Search Result
Results for "
mouse model
" in MedChemExpress (MCE) Product Catalog:
1037
Inhibitors & Agonists
6
Biochemical Assay Reagents
12
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-149464
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Ras
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Cancer
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ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model .
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- HY-P4253A
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VEGFR
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Cardiovascular Disease
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Arginyl-Glutamine TFA is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy .
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- HY-133160
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VPA-HA
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Drug Derivative
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Neurological Disease
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Valproic acid hydroxamate (VPA-HA) has shown anticonvulsant activity in a mouse neural tube defect model, without any teratogenic effects .
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- HY-122120
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AJ‐9677
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Adrenergic Receptor
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Metabolic Disease
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Rafabegron (AJ-9677) is a specific beta3-adrenoceptor agonist. Rafabegron can reduce blood glucose, insulin, FFA, and triglyceride levels in diabetic and obese mouse models .
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- HY-P3350
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Bacterial
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Infection
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LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
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- HY-P5183
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Sodium Channel
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Neurological Disease
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Hm1a is a disulfide-rich spider-venom peptide, and a NaV1.1 activator. Hm1a restores the function of inhibitory interneurons in Dravet syndrome (DS) mouse model .
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- HY-P4253
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VEGFR
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Cardiovascular Disease
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Arginyl-Glutamine is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy .
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- HY-157958
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nAChR
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Neurological Disease
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α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model .
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- HY-P991456
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Mesothelin
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Cancer
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LMB-100 is a human immunotoxin targeting MSLN/Mesothelin. LMB-100 induces systemic inflammation and CD8 T cell recruitment. LMB-100 enhances the antitumor effects of anti-PD-1 antibodies in a human peripheral blood mononuclear cell transplanted mesothelioma mouse model and a syngeneic lung adenocarcinoma mouse model expressing human mesothelin. LMB-100 can be used in mesothelioma research. Recommended isotype control: Fab fused with a fragment of Pseudomonas exotoxin A .
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- HY-156123
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Dihydrofolate reductase (DHFR)
Bacterial
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Infection
Cancer
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DHFR-IN-9 (compound 8A) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-9 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=0.25 μg/mL) and has anti-infective effects in mouse models of systemic infection and thigh infection caused by it (dose: 2.5 mg /kg, 5 mg/kg; ip). DHFR-IN-9 has stronger anticancer activity than paclitaxel (Y-B0015) in a mouse model of breast cancer (dose: 2.5 mg/kg; ip; once every 3 days) .
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- HY-176411
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VU6018042
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Potassium Channel
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Neurological Disease
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ONO-TR-772 (VU6018042) is a selective TREK inhibitor (IC50: 15 nM). ONO-TR-772 enhances recognition memory in the MK-801-stimulated NOR mouse model. ONO-TR-772 can be used in the study of diseases related to cognitive impairment .
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- HY-163076
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Apoptosis
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Others
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Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
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- HY-156122
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Dihydrofolate reductase (DHFR)
Bacterial
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Infection
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DHFR-IN-8 (compound 6r) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-8 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=15.6 ng/mL) in mouse models of systemic infection and thigh infection .
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- HY-146465
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Microtubule/Tubulin
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Cancer
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Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model .
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- HY-162315
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MAGL
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Neurological Disease
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MAGL-IN-16 (compound 27) is an oral active, selective and reversible MAGL inhibitor with the IC50 value of 10.3 nM. MAGL-IN-16 can increase the level of 2-AG and shows antidepressant effect in mouse depressed model caused by chronic restraint stress .
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- HY-156430
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MMP
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Cancer
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MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
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- HY-155079
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EGFR
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Cancer
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DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
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- HY-N7922
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Decarboxyellagic acid
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Influenza Virus
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Infection
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Urolithin M5 is a neuraminidase inhibitor that can be isolated from Ganlanye. Urolithin M5 has antiviral activity in vitro and in vivo by inhibiting the activity of viral NA. Urolithin M5 can increase the survival rate and improve pulmonary edema in pr8-infected mouse models. Urolithin M5 can be used in anti-influenza research .
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- HY-116202
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Keap1-Nrf2
Reactive Oxygen Species
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Neurological Disease
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PACA is an enhancer of nerve growth factor-induced neurite outgrowth, enhancing nerve growth factor (NGF)-induced neurite outgrowth and attenuating 6-hydroxydopamine (6-OHDA)-induced toxicity by activating the Nrf2/HO-1 pathway. PACA has neuroprotective and neurogenic activities. PACA can be used to improve dopaminergic neuron loss and motor dysfunction in MPTP mouse models of Parkinson's disease and MPP +-induced neurons .
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- HY-168300
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Reactive Oxygen Species
Apoptosis
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Inflammation/Immunology
Cancer
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Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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- HY-172672
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Orexin Receptor (OX Receptor)
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Neurological Disease
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Orexin 2 Receptor Agonist 3 is an orally active and brain-penetrant orexin receptor type-2 (OX2) agonist (EC50: 2.5 nM). Orexin 2 Receptor Agonist 3 increases wakefulness in the orexin/ataxin-3 NT1 mouse model and healthy beagle dogs. Orexin 2 Receptor Agonist 3 can be used in the study of narcolepsy .
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- HY-172671
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STING
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Cancer
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STING agonist-43 is a selective STING agonist (EC50: 20.53 μM). STING agonist-43 selectively amplifies cGAMP-dependent STING pathway activation by modulating STING oligomerization. B16.F10 has antitumor activity in a mouse melanoma model. STING agonist-43 can be used for the study of cancer immunity .
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- HY-16384
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Antibiotic L 156602; PD 124966
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Complement System
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Inflammation/Immunology
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L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH) .
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- HY-149949
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Apoptosis
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Cancer
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Anticancer agent 105 is a compound based on thienopyrimidine scaffold, with with good safety and anticancer properties. Anticancer agent 105 shows selective toxicity towards melanoma cancer, and induces apoptosis. And Anticancer agent 105 significantly inhibits the metastatic nodules, even in pulmonary metastatic melanoma mouse model .
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- HY-164102
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TNF Receptor
NF-κB
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Inflammation/Immunology
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TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
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- HY-162818
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Bacterial
Reactive Oxygen Species
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Infection
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Antibacterial agent 237 (compound Ru-8) is a bacteriostatic agent for Staphylococcus aureus, with MIC of 0.78-1.56 μg/mL. Antibacterial agent 237 destroys bacterial cell membranes, changes their permeability, and induces bacteria to produce Reactive Oxygen Species, leading to bacterial death without causing drug resistance. Antibacterial agent 237 has low hemolytic toxicity to rabbit red blood cells and Raw 264.7 cells, and has significant antibacterial effects against Staphylococcus aureus in mouse skin wound infection models and Bacillus major larvae infection models .
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- HY-10109A
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PI3K
Akt
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Inflammation/Immunology
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AS-605240 (potassium) is an orally active PI3Kγ inhibitor (IC50: 8 nM; Ki: 7.8 nM). AS-605240 (potassium) inhibits MCP-1- and CSF1-induced PKB phosphorylation (IC50 values are 0.181 and 0.550 µM, respectively). AS-605240 (potassium) reduces neutrophil recruitment in RANTES (CCL5)- and thioglycolate-induced peritonitis mouse models (EC50 values are 9.1 and 10 mg/kg, respectively). AS-605240 (potassium) ameliorates αCII-IA-induced arthritis in mice .
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- HY-155659
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Nuclear Hormone Receptor 4A/NR4A
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Neurological Disease
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4A7C-301 is a Nurr1 agonist with robust neuroprotective effects in vitro. 4A7C-301 significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models. 4A7C-301 can be used for the research of Parkinson’s disease .
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- HY-172349
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Bacterial
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Infection
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JNJ-2901 is an inhibitor of M. tuberculosis cytochrome bc1:aa3. JNJ-2901 reduces bacterial load in the acute/chronic mouse infection models of M. tuberculosis H37Rv-ΔcydAB. JNJ-2901 can be used in tuberculosis (TB) research .
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- HY-155417
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ERK
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Neurological Disease
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GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680?μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
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- HY-170446
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MyD88
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Inflammation/Immunology
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MyD88-IN-2 (compound A5S) is a Myeloid differentiation primary response 88 (MyD88) inhibitor with the Kd of 15 μM. MyD88-IN-2 shows protective effects on LPS (HY-D1056)-induced and sepsis-induced ALI mouse models .
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- HY-131598C
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6-Thioguanosine-5'-triphosphate tetrasodium
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Ras
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Inflammation/Immunology
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6-Thio-GTP (tetrasodium) is a Vav1-Rac inhibitor. 6-Thio-GTP (tetrasodium) inhibits TCR-stimulated T cell proliferation and CD28-mediated T cell survival. 6-Thio-GTP (tetrasodium) has an immunosuppressive effect in a mouse cardiac allograft transplant model and prolongs cardiac allograft survival .
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- HY-162630
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HDAC
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Inflammation/Immunology
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HDAC6-IN-44 (compound H10) is a selective HDAC6 inhibitor with an IC50 value of 8.97 nM. HDAC6-IN-44 can inhibit the idiopathic pulmonary fibrosis (IPF) phenotype and exhibits antifibrotic activity. Additionally, HDAC6-IN-44 reduces fibrogenesis in a bleomycin-induced pulmonary fibrosis mouse model and demonstrates good metabolic stability. HDAC6-IN-44 holds promise for research in the field of idiopathic pulmonary fibrosis .
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- HY-145239
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
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- HY-176404
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HSP
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Cancer
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DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
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- HY-172888
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Endogenous Metabolite
FAK
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Cancer
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SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50: 3.59 μM). SPP-037 exhibits anti-MDA-MB-231 cell migration activity by inhibiting integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used in breast cancer research .
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- HY-168009
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NLRP3-IN-45 (D6) is an inhibitor of NLRP3 inflammasome activation, inhibiting the activity of IL-1β (IC50=41.79 nM). NLRP3-IN-45 exerts its effects without affecting the initial stage of NLRP3 inflammasome activation. NLRP3-IN-45 specifically inhibits the activation of NLRP3 inflammasome in the LPS-induced acute lung injury (ALI) mouse model .
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- HY-151928
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JNK
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Neurological Disease
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JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
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- HY-155821
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NF-κB
NO Synthase
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
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- HY-155820
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NF-κB
NO Synthase
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
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- HY-P991380
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Transferrin Receptor
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Neurological Disease
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TXB4 is a brain-permeable human monoclonal antibody (mAb) targeting CD71. TXB4 prevents 6-OHDA-induced death of TH-positive neurons in the SNc in a 6-OHDA mouse model of Parkinson's disease (PD). TXB4 can be used in neurodegenerative diseases, acute brain and spinal cord injury, and depression research .
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- HY-172916
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SHP2
FGFR
p38 MAPK
ERK
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Cancer
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LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR (IC50 values are 71.6 and 8.9 nM, respectively). LC-SF-14 inhibits FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation. LC-SF-14 inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). LC-SF-14 has antitumor activity in the SNU-16 xenograft mouse model. LC-SF-14 can be used in FGFR2-driven gastric cancer research .
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- HY-P991307
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Transmembrane Glycoprotein
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Cancer
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BND-35 is a human monoclonal antibody (mAb) targeting LILRB4/ILT3/CD85k. BND-35 blocks the interaction of ILT3 with APOE and fibronectin, enhances the pro-inflammatory activity of various myeloid cells, and reverses ILT3-mediated immunosuppression of T cells by various suppressive myeloid cells. BND-35 has anti-tumor activity in the hILT3 transgenic mouse tumor model .
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- HY-172934
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Toll-like Receptor (TLR)
NO Synthase
PROTACs
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Inflammation/Immunology
Cancer
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FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8 + T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity. (Pink: target protein TLR7/8 agonist 1 ligand (HY-103698); black: linker (HY-172936); blue: FR-β ligand (HY-172935)) .
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- HY-173270
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Bacterial
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Infection
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Antibacterial synergist 3 is a dual-acting inhibitor of biofilm (IC50 of PAO1: 0.40 μM and IC50 of PA14: 1.45 μM). Antibacterial synergist 3 reduces virulence production by inhibiting the quorum sensing (QS) system and induces iron deficiency in P. aeruginosa PAO1. Antibacterial synergist 3 enhances the efficacy of Tobramycin (HY-B0441) and Ciprofloxacin (HY-B0356) in a mouse wound infection model. Antibacterial synergist 3 can be used for the research of P. aeruginosa infections .
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- HY-172941
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NOD-like Receptor (NLR)
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Neurological Disease
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VEN-02XX is an orally active and brain-permeable NLRP3 inhibitor. VEN-02XX inhibits the release of IL-1β and IL-18 (IC50 0.3 and 0.28 μM, respectively). VEN-02XX restores memory and cognition, inhibits microgliosis, and reduces neuroinflammation and tau pathology in the 5XFAD/Rubicon KO mouse model. VEN-02XX may be used in the study of Alzheimer's disease (AD) .
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- HY-109061B
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YH25448 mesylate; GNS-1480 mesylate
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EGFR
Akt
ERK
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Cancer
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Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer .
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- HY-168498
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Glutathione S-transferase
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Inflammation/Immunology
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GJG057 is a selective, orally active inhibitor for leukotriene C4 synthase (LTC4S) with an IC50 of 44 nM. GJG057 exhibits anti-inflammatory activity in mouse skin inflammation model and mouse asthma model .
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- HY-156002
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Paluratide
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Ras
ERK
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Cancer
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LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
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- HY-170994
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Imidazoline Receptor
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Neurological Disease
Inflammation/Immunology
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I2-IRs ligand-1 (Compound 12d) is an orally active and BBB-penetrable compound. I2-IRs ligand-1 has a high affinity for imidazoline I2 receptors (I2-IRs) (pKi: 9.98). I2-IRs ligand-1 can improve cognitive impairment in senescent mice and exhibits analgesic, anti-inflammatory, and neuroprotective activities. I2-IRs ligand-1 can be used for the research of Alzheimer's disease and related pain disorders .
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- HY-160587
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SRPK
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Cardiovascular Disease
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Antiangiogenic agent 5 (compound 17) has anti-angiogenic activity. Antiangiogenic agent 5 show inhibition to SRPK1, with IC50 of 1.3 nM .
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- HY-168211
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Epoxide Hydrolase
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Inflammation/Immunology
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LQ-38 is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 5.2 nM. LQ-38 exhibits anti-inflammatory activity in rat foot edema model and mouse acute pancreatitis model, exhibits analgesic effect in Acetic acid (HY-Y0319)-induced writhing mouse model .
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- HY-176149
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CaMK
MMP
AMPK
Apoptosis
Autophagy
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Cancer
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Fluoxetine-Conjugated Platinum(IV) prodrug-1 is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
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- HY-172878
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Small Interfering RNA (siRNA)
HDAC
Apoptosis
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Cancer
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HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research .
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- HY-12788
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- HY-19459A
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- HY-168719
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PPAR
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Inflammation/Immunology
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PPARγ agonist 16 (Compound 4G) is the agonist for PPARγ, that competitively binds to LBD domain of PPARγ with IC50 of 1790 nM. PPARγ agonist 16 inhibits the ear swelling in mouse model, and exhibits anti-hyperglycemic in Streptozotocin (HY-13753)-induced mouse diabetes mellitus model .
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- HY-N1419
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- HY-109010
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HM71224; LY3337641
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Btk
BMX Kinase
Toll-like Receptor (TLR)
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Metabolic Disease
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Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis .
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- HY-Y1322
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- HY-108062
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Beta-lactamase
Bacterial
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Infection
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BLI-489 is a beta-lactamase inhibitor. BLI-489 combined with Piperacillin (HY-B1923) inhibits infection caused by class A (including ultra-broad spectrum β-lactamase), Class C (AmpC) and Class D β-lactamase expressing pathogens .
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- HY-B0957
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Erythromycin ethyl succinate; EES
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Bacterial
HIV
Autophagy
Antibiotic
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Infection
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Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
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- HY-N15385
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Lipase
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Metabolic Disease
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Hericenone D is a lipase inhibitor that can be isolated and extracted from Hericium erinaceus. Hericenone D can be used in the research of obesity .
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- HY-168105
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RET
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Cancer
|
|
RET-IN-27 (compound 20p) is a potent inhibitor of RET, with IC50s of 3.6 nM, 0.1 nM, 2.1 nM, 0.3 nM for RET WT, RET V804L, RET V804M, RET M918T, respectively. RET-IN-27 plays an important role in cancer research .
|
-
- HY-169102
-
|
|
Virus Protease
|
Infection
|
|
CHIKV nsP2 protease-IN-1(compound J13) is an oral active non-structural protein 2 protease inhibitor with the EC50 of 0.39 μM aganist of CHIKV S27. CHIKV nsP2 protease-IN-1 can be used for study of Chikungunya virus .
|
-
- HY-139668
-
|
|
Neurotensin Receptor
|
Cancer
|
|
VGD071, a sortilin-targeting compound, is a promising candidate for future studies using mouse breast cancer models.
|
-
- HY-50884
-
-
- HY-118984
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
CRX-526 is a TLR4 antagonist that can block the interaction of lipopolysaccharide (LPS, HY-D1056) with the immune system, including preventing the expression of pro-inflammatory genes stimulated by LPS, as well as blocking the release of TNF-α induced by LPS. CRX-526 exhibits anti-inflammatory effects in two mouse models of colitis (namely, the dextran sodium sulfate-induced colitis model and the multidrug resistance gene 1a-deficient mouse model) .
|
-
- HY-145237
-
BM213
1 Publications Verification
|
Complement System
|
Cancer
|
|
BM213, a potent and selective agonist for C5aR1, shows antitumor activity in a mouse model of mammary carcinoma.
|
-
- HY-101459
-
-
- HY-109869
-
|
|
Orphan Receptor
|
Others
|
|
Photoregulin1 is a compound with the potential to inhibit retinitis pigmentosa that modulates gene expression in retinal cells and slows the degeneration of photoreceptors in a mouse model.
|
-
- HY-153364
-
|
|
PPAR
|
Cancer
|
|
FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
|
-
- HY-152632
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC50 values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things .
|
-
- HY-163837
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-48 (compound HD10) is a potent inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.1 nM. PD-1/PD-L1-IN-48 plays an important role in cancer research .
|
-
- HY-157839
-
|
|
α-synuclein
|
Neurological Disease
|
|
PROTAC α-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with EC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-synuclein degrader 6 plays an important role in neurodegenerative diseases (NDs) research (Blue:ubiquitin E3 ligase cereblon ligand (HY-14658), Black: linker (HY-128803); Pink: Ligand for target protein (HY-151035)) .
|
-
- HY-163192
-
|
|
ROR
|
Cancer
|
|
W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer .
|
-
- HY-161727
-
|
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis .
|
-
- HY-137922
-
|
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
SHS4121705 is an orally effective mitochondrial uncoupling agent with an IC50 of 4.3 μM in L6 myoblasts. SHS4121705 can be used in the study of non-alcoholic steatohepatitis (NASH) .
|
-
- HY-168569
-
|
|
Aminoacyl-tRNA Synthetase
|
Infection
|
|
DDD489 is a potent and selective Cryptosporidium lysyl-tRNA synthetase (CpKRS) inhibitor with IC50 values of 0.85 uM.DDD489 shows anti-cryptosporidials activity in vitro and in vivo .
|
-
- HY-123752
-
|
|
Hedgehog
Smo
|
Cancer
|
|
MS-0022 is a Smoothened (SMO) antagonist. MS-0022 can inhibit the Hedgehog (Hh) signaling pathway. MS-0022 can be used in anti-tumor research .
|
-
- HY-133898
-
|
TAK-925
|
Orexin Receptor (OX Receptor)
|
Others
|
|
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
|
-
- HY-P3163
-
|
|
PPAR
Collagen
SOD
|
Inflammation/Immunology
|
|
Hexapeptide-9 is a signaling peptide. Hexapeptide-9 can promote collagen production. Hexapeptide-9 has anti-aging activity, and can be used in cosmetic research .
|
-
- HY-163081
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
|
-
- HY-N2014
-
-
- HY-170510
-
|
|
Galectin
|
Cancer
|
|
GB2095 is a selective, orally active inhibitor for galectin-3 with Kd of 36 nM and 0.35 μM for human galectin-3 and mouse galectin-3. GB2095 exhibits antitumor efficacy in mouse models .
|
-
- HY-W587489
-
-
- HY-N0648
-
|
|
Others
|
Inflammation/Immunology
|
|
Monotropein is an iridoid glycoside isolated Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model .
|
-
- HY-P1727
-
|
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-129819
-
|
|
Bacterial
|
Infection
|
|
(Rac)-DNDI-8219 is an antituberculosis compound with potent anti-leishmanial activity. (Rac)-DNDI-8219 demonstrated superior efficacy in the Leishmania donovani mouse model. (Rac)-DNDI-8219 showed promising activity in the Leishmania infantum hamster model. (Rac)-DNDI-8219 candidate compound R-6 provided excellent oral efficacy in the same hamster model .
|
-
- HY-W764758
-
|
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
3-OH-Kynurenamine dihydroiodide is the dihydroiodide form of 3-OH-Kynurenamine (HY-156908). 3-OH-Kynurenamine dihydroiodide is an activator for aryl hydrocarbon receptor (AhR), and thus regulates the immune response. 3-OH-Kynurenamine dihydroiodide upregulates the expressions of Ido1 and Tgfb1, ameliorates the skin inflammation in psoriasis mouse model and kidney damage in nephrotoxic lupus mouse model .
|
-
- HY-170794
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
ALT-007 is an orally effective serine palmitoyltransferase (SPT) inhibitor. SPT is the rate-limiting enzyme for the de novo synthesis of ceramide. In a mouse model of age-related sarcopenia, ALT-007 can effectively restore the muscle mass and function impaired by aging. ALT-007 may enhance protein homeostasis in Caenorhabditis elegans and mouse models of aging and age-related diseases and play the role of a ceramide inhibitor .
|
-
- HY-167676
-
|
|
DNA/RNA Synthesis
|
Inflammation/Immunology
|
|
Cofpropamine, a caffeine derivative that inhibits polyadenylation, enhances the inhibitory effect of cyclophosphamide (HY-17420) in rat adjuvant arthritis and mouse collagen arthritis models .
|
-
- HY-117951
-
|
|
Beta-lactamase
|
Infection
|
|
ANT431 is a metallo-β-lactamase inhibitor that also restores the effectiveness of Meropenem (HY-13678) in a mouse thigh Escherichia coli infection model .
|
-
- HY-B1899S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Apoptosis
|
Others
|
|
Taurodeoxycholic acid-d5 is the deuterium labeled Taurodeoxycholic acid (HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
|
-
- HY-P1727A
-
|
|
YAP
|
Cancer
|
|
Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-120016
-
|
|
Glucocorticoid Receptor
|
Neurological Disease
|
|
RU 43044 is a glucocorticoid receptor antagonist. RU 43044 shows an antidepressant-like effect, probably via an inhibition of enhanced prefrontal dopaminergic neurotransmission in these mouse models .
|
-
- HY-163729
-
-
- HY-173030
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, DOR and KOR with Ki of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models .
|
-
- HY-P99590A
-
|
RAP-011
|
TGF-beta/Smad
|
Cardiovascular Disease
|
|
Sotatercept (mIgG2a) has direct cardioprotective actions, which reduces right ventricular (RV) remodeling and improves function in a pulmonary artery banding (PAB) mouse model .
|
-
- HY-139716
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
|
-
- HY-169779
-
|
|
p62
|
Cancer
|
|
PTX80 is an antagonist of p62 with an IC50 value of 31.18 nM. PTX80 reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model .
|
-
- HY-153650
-
-
- HY-153521
-
|
|
BCL6
|
Cancer
|
|
CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
|
-
- HY-12182
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-155146
-
|
|
Necroptosis
|
Cancer
|
|
Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
|
-
- HY-17035
-
|
|
Parasite
Antibiotic
Bacterial
|
Infection
|
|
Doramectin is a derivative of Ivermectin (HY-15310). Doramectin is a potent antiparasitic antibiotic. Doramectin is an active compound against S.mansoni in an NMRI mouse infection model .
|
-
- HY-N2195
-
|
(+)-Nootkatone
|
Interleukin Related
TNF Receptor
|
Neurological Disease
|
|
Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects . Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease .
|
-
- HY-P2287
-
|
|
CRFR
|
Neurological Disease
|
|
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an EC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive agent in the mouse model .
|
-
- HY-147784
-
|
|
Btk
|
Cancer
|
|
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
|
-
- HY-P99578
-
|
HL036337; HBM9036
|
TNF Receptor
|
Inflammation/Immunology
|
|
Tanfanercept (HL036337) is an TNF-α receptor fusion protein that targets TNF-α. Tanfanercept is effective in ameliorating corneal erosions in a dry eye (DE) mouse model .
|
-
- HY-164781
-
-
- HY-163984
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 240 (compound 62-7c) is an antibacterial agent that can target multidrug-resistant (MDR) MRSA strains. Antibacterial agent 240 showed high biosafety and potent anti-infection activity in mouse pneumonia and mouse wound models of MRSA infection .
|
-
- HY-172970
-
|
|
CDK
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib (HY-50898) in the NCI-N87 xenograft mouse model produces a synergistic therapeutic effect .
|
-
- HY-151066
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMS-1233 is an orally active inhibitor for programmed cell death-ligand 1 (PD-L1), with IC50 of 14.5 nM. BMS-1233 promotes cell death of HepG2 in a Jurkat T cell and HepG2 cell co-culture model, exhibits antitumor activity against melanoma in mouse model .
|
-
- HY-161736
-
|
|
CDK
|
Cancer
|
|
ARN25499 (compound 15) is a CDC42 inhibitor. ARN25499 can be used in cancer-related research .
|
-
- HY-153254
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus .
|
-
- HY-163719
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy .
|
-
- HY-163849
-
|
|
Others
|
Inflammation/Immunology
|
|
Mizoribine prodrug-1 (compound 18) is a oral active ester-based mizoribine (HY-17470) prodrug. Mizoribine prodrug-1 displays a inhibition of IL-2 production .
|
-
- HY-132924
-
-
- HY-162554
-
|
|
CD73
|
Inflammation/Immunology
Cancer
|
|
CD73-IN-15 (compound 12f) is a potent inhibitor of CD73, with the IC50 of 60 nM. CD73-IN-15 plays an important role in cancer research .
|
-
- HY-156800
-
|
|
Phospholipase
|
Others
|
|
PDDC is a compound used to inhibit Alzheimer's disease. It is a nSMase2 inhibitor that can inhibit tau-induced nSMase2 activity and ceramide elevation, and slow the spread of tau in mouse models.
|
-
- HY-111258
-
-
- HY-153996
-
|
|
Deubiquitinase
|
Cancer
|
|
CT1113 is a potent USP28 and USP25 inhibitor. CT1113 decreases the MYC level in vivo，exhibits anti-tumor activity in mouse pancreatic cancer CDX model .
|
-
- HY-136447
-
ASP4132
1 Publications Verification
|
AMPK
|
Cancer
|
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
|
-
- HY-P1787
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (4-10) is an epitope for the polyclonal anti-Aβ(1-42) antibody, reduces amyloid deposition in a transgenic Alzheimer disease mouse model .
|
-
- HY-125850
-
-
- HY-124378
-
|
|
MAGL
|
Inflammation/Immunology
|
|
MAGL-IN-17 (Compound ) is an inhibitor for MAGL with a Ki of 0.4 μM. MAGL-IN-17 inhibits mouse MAGL and rat MAGL with IC50 of 0.18 and 0.24 μM. MAGL-IN-17 exhibits anti-inflammatory activity in mouse experimental autoimmune encephalitis models .
|
-
- HY-12182A
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-16706
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-120924
-
-
- HY-153670
-
|
|
CCR
|
Cancer
|
|
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
|
-
- HY-162042
-
|
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 14 (compound 32) is an orally active AMPK activator. AMPK activator 14 decreases fasted glucose and insulin levels in a db/db mouse model of Type II diabetes .
|
-
- HY-128901
-
|
F 14679 fumarate
|
5-HT Receptor
|
Neurological Disease
|
|
F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress .
|
-
- HY-P10850
-
|
|
TNF Receptor
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model .
|
-
- HY-131420
-
|
Aseanostatin P1; Isotetradecanoic acid
|
Biochemical Assay Reagents
|
Others
|
|
12-Methyltridecanoic acid is a methylated fatty acid that has been found in milk. 12-Methyltridecanoic acid (200 μM) reduces angiogenesis and corneal opacity in alkaline or Pseudomonas aeruginosa-induced ocular mouse models.
|
-
- HY-170409
-
|
|
Trk Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
|
-
- HY-168625
-
|
|
Molecular Glues
|
Inflammation/Immunology
|
|
VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc. .
|
-
- HY-145521
-
|
5(S)-Hydroxy-6E,8Z,11Z-eicosatrienoic acid
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
5(S)-HETrE is a metabolite of the ω-6 fatty acid γ-linolenic acid. 5(S)-HETrE can be elevated in serum levels in an obesity mouse model .
|
-
- HY-P3341
-
-
- HY-W096171
-
|
3-Hydroxy-D-tyrosine
|
Carboxypeptidase
|
Neurological Disease
|
|
D-Dopa is a non-competitive, allosteric inhibitor for glutamate carboxypeptidase II (GCPII) with an IC50 of 200 nM. D-Dopa exhibits good pharmacokinetic characteristics, and low blood-brain barrier permeability in mouse model .
|
-
- HY-U00442
-
CTX1
1 Publications Verification
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system .
|
-
- HY-111209
-
|
S14161
|
PI3K
|
Cancer
|
|
Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research .
|
-
- HY-15782
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
YH16899 binds Lysyl-tRNA synthetase (KRS), and inhibits membrane translocation of KRS. YH16899 impares the interaction of KRS with 67LR. YH16899 inhibits tumor metastasis in mouse models .
|
-
- HY-13646C
-
|
HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride
|
P-glycoprotein
|
Cancer
|
|
Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models .
|
-
- HY-W151617A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Desethoxy Quetiapine dihydrochloride (Compound 28) is an antagonist for dopamine D2 receptor with an IC50 of 1330 nM. Desethoxy Quetiapine dihydrochloride antagonises Apomorphine (HY-12723)-induced climbing and swimming disruption in mouse models .
|
-
- HY-150233
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .
|
-
- HY-167855
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
MRS4833 (compound 15) is an orally active, potent, competitive P2Y14R antagonist with an of IC50 of 5.92 nM for hP2Y14R and an IC50 of 4.8 nM for mP2Y14R. MRS4833 reduces airway eosinophilia in a protease-mediated asthma model and reverses chronic neuropathic pain in a mouse CCI model .
|
-
- HY-169092
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
PF-07957472 (Compound 4) is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor. PF-07957472 shows cytopathic effect in SARS-CoV-2 infected NHBE cells (EC50 = 13.9 nM). PF-07957472 shows antiviral effect in a mouse-adapted model of COVID-19 infection model .
|
-
- HY-173425
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
STING-IN-15 (compound 66) is a potent STING inhibitor. STING-IN-15 inhibits human STING and mouse STING with IC50s of 116 and 96.3 nM, respectively. STING-IN-15 significantly alleviates tissue injury and inflammation in TREX1 D18N mouse model .
|
-
- HY-118696
-
|
|
GABA Receptor
|
Neurological Disease
|
|
MGAT2-IN-5 (Compound 17b) is a selective inhibitor for mouse GABA transit protection subsidity 2 (mGAT2) with an IC50 of 45 μM. MGAT2-IN-5 exhibits anticonvulsive efficacy in audiogenic seizure (AGS) susceptible frings mouse model with an ED50 of 20.4 mg/kg .
|
-
- HY-163069
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-43 (compound A11) is an orally active and potent antitubercular agent. Antitubercular agent-43 shows highly metabolic stability against human and mouse cytochrome P450 enzymes. Antitubercular agent-43 exhibits bactericidal efficacy in acute TB infection mouse model .
|
-
- HY-19606
-
|
Antibiotic MI 43-37F11
|
Interleukin Related
NO Synthase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cytogenin (Antibiotic MI 43-37F11) is an orally active antineoplastic antibiotic. Cytogenin regulates the inflammatory cytokine, reduces the levels of iNOS, NO and IL-6 in mouse macrophages, and exhibits antidiabetic efficacy in mice. Cytogenin inhibits growth of Ehrlich ascites tumor in mouse model .
|
-
- HY-169832
-
|
|
Drug Intermediate
|
Others
|
|
Sulfanegen is a 3-mercaptopyruvate prodrug and cyanide antidote. Sulfanegen converts toxic cyanide into a relatively non-toxic substance. Sulfanegen, alone or in combination with Cobinamide, has detoxification effect in mouse models of cyanide poisoning .
|
-
- HY-168147
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp-1-IN-24 (compund 7) is an ENPP1 inhibitor that, in combination with anti-PD-1 antibodies, achieves 77.7% tumor growth inhibition and improves survival in mouse models .
|
-
- HY-124733A
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism .
|
-
- HY-155163
-
-
- HY-112330
-
|
|
PKA
|
Neurological Disease
|
|
4-Cyano-3-methylisoquinoline is an inhibitor for protein kinase A (PKA) with an IC50 of micromolar level. 4-Cyano-3-methylisoquinoline reverses morphine tolerance in mouse model .
|
-
- HY-149539
-
|
|
FLT3
RET
|
Cancer
|
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
|
-
- HY-136527
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .
|
-
- HY-401913
-
|
|
Phosphodiesterase (PDE)
|
Infection
Cancer
|
|
Endo CNTinh-03 is inhibitor for the elevation of cAMP and cGMP induced by agonist, such as G protein-coupled receptors, adenylate cyclase, and guanylate cyclase (IC50 is 4 μM). Endo CNTinh-03 inhibits cholera toxin- and Escherichia coli (STa) toxin- induced CFTR chloride current, ameliorates secretory diarrhea in mouse models, and prevents cyst growth in polycystic kidney disease model .
|
-
- HY-16706A
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-N7000
-
-
- HY-N2556
-
|
|
Others
|
Inflammation/Immunology
|
|
Tirucallol, a tetracyclic triterpene, is isolated from Euphorbia lacteal latex. Tirucallol has topical anti-inflammatory effect. Tirucallol can suppress ear edema in the mouse model and inhibit nitrite production in lipopolysaccharide-stimulated macrophages .
|
-
- HY-145704
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria .
|
-
- HY-126379
-
|
|
Apoptosis
|
Cancer
|
|
CDDO-2P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-2P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model .
|
-
- HY-105321A
-
|
PBT 2 hydrochloride
|
Bacterial
|
Neurological Disease
|
|
PBT 1033 hydrochloride is an orally active copper/zinc ionophore. PBT 1033 hydrochloride restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria .
|
-
- HY-N3312
-
|
|
Endogenous Metabolite
|
Infection
|
|
Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-164484
-
|
|
Raf
|
Cancer
|
|
IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
|
-
- HY-106892
-
|
348U87
|
DNA/RNA Synthesis
|
Infection
|
|
BW 348U87 is an inhibitor for ribonucleotide reductase, which exhibits synergistic effect with Acyclovir (HY-17422), potentiate the antiviral activity of Acyclovir against herpes simplex virus (HSV) in athymic nude mouse model .
|
-
- HY-170833
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Anticonvulsant agent 8 (compound D4) is an anticonvulsant agent that inhibits GABAA currents with ED50 values of 2.23 and 24.60 mg/kg in the maximum electroshock (MES) and pentylenetetrazol (PTZ) tests in mouse models, respectively .
|
-
- HY-105296
-
|
|
Sigma Receptor
mAChR
|
Cancer
|
|
Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
|
-
- HY-161065
-
|
|
Bacterial
|
Infection
|
|
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection .
|
-
- HY-N8730
-
|
|
Others
|
Neurological Disease
|
|
7,8,3 ',4 '-Tetramethoxyflavone is an extract
isolated from natural pomegranate juice and seeds. 7,8,3 ',4' -Tetramethoxyflavone has a protective effect on the neurotoxicity of
paraquat-induced Parkinson's disease mouse model .
|
-
- HY-153189
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research .
|
-
- HY-15324
-
|
P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
|
Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
|
Cancer
|
|
PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
|
-
- HY-162892
-
|
|
Epigenetic Reader Domain
|
Cancer
|
BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model .
|
-
- HY-15323
-
|
P505-15 Hydrochloride
|
Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
|
Cancer
|
|
PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
|
-
- HY-170436
-
|
|
Photosensitizer
Apoptosis
|
Cancer
|
|
NFh-NMe-2 is a photosensitizer, that interacts with nitroreductase, generates singlet oxygen in tumor cells, exhibits cytotoxicity in cancer cells, and induces apoptosis. NFh-NMe-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-148258
-
-
- HY-146054
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model .
|
-
- HY-144265
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect .
|
-
- HY-B1252B
-
-
- HY-172759
-
|
|
Wee1
|
Cancer
|
|
PKMYT1-IN-9 is a highly selective and orally active PKMYT1 inhibitor (IC50: 4.4 nM). PKMYT1-IN-9 shows more selective for PKMYT1 than WEE1 (IC50: 32.4 μM). PKMYT1-IN-9 exhibits antitumor activity .
|
-
- HY-161297A
-
-
- HY-145272
-
|
|
ELOVL
|
Neurological Disease
|
|
ELOVL1-IN-3 (Compound 22) is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD) [1].
|
-
- HY-B0478
-
|
AF-1161
|
5-HT Receptor
|
Neurological Disease
|
|
Trazodone hydrochloride (AF-1161) is a serotonin receptor antagonist and reuptake inhibitor with anti-neuroinflammatory effects. Trazodone hydrochloride can be used for research in major depressive disorder and also holds potential for studies related to sleep disorders .
|
-
- HY-149700
-
|
|
ROCK
MMP
STAT
|
Others
|
|
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model .
|
-
- HY-B1252BR
-
|
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
Cefalonium (dihydrate) (Standard) is the analytical standard of Cefalonium (dihydrate). This product is intended for research and analytical applications. Cefalonium dihydrate is a cephalosporin antibiotic. Cefalonium (dihydrate) is effective against Staphylococcus aureus. Cefalonium (dihydrate) has anti-inflammatory and antibacterial activities .
|
-
- HY-145119
-
|
|
SARS-CoV
|
Infection
|
|
GS-621763 is an orally available precursor to GS-441524 that exhibits anti-SARS-CoV-2 viral activity in mice. GS-621763 reduces viral load to undetectable levels in ferrets infected with SARS-CoV-2 .
|
-
- HY-145280A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active .
|
-
- HY-145280
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active .
|
-
- HY-N6790
-
-
- HY-118282
-
|
|
PGE synthase
|
Endocrinology
|
|
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice .
|
-
- HY-114360A
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
|
-
- HY-N0109
-
|
Rhodioloside
|
PINK1/Parkin
mTOR
Apoptosis
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
|
-
- HY-N0648R
-
|
|
Others
|
Inflammation/Immunology
|
|
Monotropein (Standard) is the analytical standard of Monotropein. This product is intended for research and analytical applications. Monotropein is an iridoid glycoside isolated Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model .
|
-
- HY-173080
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 267 (Compound h19) is a pleuromutilin derivative with a potent antibacterial activity on Gram-positive bacteria. Antibacterial agent 267 shows an antibacterial activity in methicillin-resistant Staphylococcus aureus (MRSA)-infected mouse models .
|
-
- HY-114952
-
|
|
Acyltransferase
|
Cardiovascular Disease
|
|
SM-32504 is an effective ACAT inhibitor that can significantly reduce serum cholesterol levels in mouse models fed with high-fat and high-cholesterol diets. SM-32504 can be used for research on hypercholesterolemia and atherosclerosis .
|
-
- HY-123059
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
(Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease .
|
-
- HY-172937
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 13 (compound MR3) is potent ERα degrader with an IC50 of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .
|
-
- HY-148772
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
PTC258 is a specific and orally active splicing modulator of Elongator complex protein 1 gene (ELP1). PTC258 increases the expression of ELP1 in vitro and in vivo. PTC258 is well tolerated in mouse model .
|
-
- HY-129228
-
|
|
Parasite
|
Infection
|
|
Lychnopholide is a sesquiterpene lactone derived from the Asteraceae, Lychnopholide exhibits anti-trypanosomal activity against Trypanosoma cruzi. lychnopholide encapsulated in nanocapsules reduces its toxicity to mammalian cells. Lychnopholide ameliorates Chagas disease in mouse models .
|
-
- HY-172371
-
|
|
Reactive Oxygen Species
|
Others
|
|
Hypoxystat increases the affinity of hemoglobin for oxygen and reduces the release of oxygen to tissues, thereby inducing the tissue hypoxia. Hypoxystat alleviates the mitochondrial disease Leigh syndrome in Ndufs4 knockout mouse models. Hypoxystat exhibits orally activity .
|
-
- HY-162144
-
|
|
Bacterial
|
Infection
|
|
BDM91288 is an orally active AcrB efflux pump inhibitor of pyridinium piperazine. BDM91288 can enhance the in vivo efficacy of levofloxacin (HY-B0330) in the treatment of Klebsiella pneumoniae pulmonary infection in mouse models .
|
-
- HY-108194
-
|
|
Biochemical Assay Reagents
|
Others
|
|
CGP 46700 (Compound 49) is an orally active iron chelator, that exhibits high affinity for iron, removes iron from ferritin and human serum transferrin. CGP 46700 promotes iron excretion in a mouse iron overload model .
|
-
- HY-111145
-
|
|
Androgen Receptor
|
Cancer
|
|
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
|
-
- HY-135115
-
|
3,4-DHPEA-EA
|
α-synuclein
HDAC
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasma leptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
|
-
- HY-169927
-
|
|
Ferroptosis
|
Inflammation/Immunology
|
|
Ferroptosis-IN-16 (Compound 13l) is a specific inhibitor for ferroptosis with an EC50 of 0.7 nM and 0.9 nM in ES-2 cell and LX-2 cell. Ferroptosis-IN-16 ameliorates Acetaminophen (HY-66005)-induced acute liver injury in mouse model, and exhibits good metabolic stability in mouse liver microsomes .
|
-
- HY-149430
-
|
|
Amyloid-β
|
Neurological Disease
|
|
YIAD-0205 is an orally available Aβ(1?42) aggregation inhibitor. YIAD-0205 demonstrated in vivo efficacy in an AD transgenic mouse model with five familial AD mutations (5XFAD) .
|
-
- HY-170806
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .
|
-
- HY-105321
-
|
PBT 2
|
Bacterial
|
Neurological Disease
|
|
PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria .
|
-
- HY-169918
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-34 (compound A8) is a phenyl urea SHP2 inhibitor with anti-cancer activity. SHP2-IN-34 significantly suppresses tumor growth in CT26 mouse model .
|
-
- HY-P5907
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-161759
-
|
|
Histone Methyltransferase
|
Metabolic Disease
|
|
MS152 is an oral bioactive inhibitor of EHMT2/G9a. MS152 reactivats maternally silenced Prader-Willi syndrome (PWS) genes in brain and liver tissues of PWS mouse models .
|
-
- HY-163149
-
|
|
HBV
|
Infection
|
|
AB-452, a Dihydroquinolizinone (DHQ) analogue, is a potent and orally active HBV RNA destabilizer. AB-452 inhibits PAPD5/7 proteins in vitro with good in vivo efficacy in a chronic HBV mouse model .
|
-
- HY-13762
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-159881
-
|
|
Mitophagy
|
Metabolic Disease
|
|
SHS206 (compound 6n) is an orally active mitochondrial uncoupler that reduces hepatic triglyceride levels. SHS206 exhibits in vivo efficacy in the GAN mouse model and shows inhibitory effects on metabolic dysfunction-associated steatohepatitis (MASH) .
|
-
- HY-13762A
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
|
-
- HY-124628
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
|
-
- HY-163386
-
|
|
Biochemical Assay Reagents
|
Others
|
|
HFTC-HClO 1 is a stable and sensitive ratiometric probe, which images the endogenous HClO. HFTC-HClO 1 exhibits a main emission peak at 579 nm. HFTC-HClO-1 visualizes HClO generated in the rheumatoid arthritis mouse model .
|
-
- HY-161864
-
|
|
STAT
|
Inflammation/Immunology
|
|
STAT3-IN-29 (Compound B20) is an inhibitor for STAT3. STAT3-IN-29 inhibits the proliferation of HaCaT cell with IC50 of 0.09 µM, ameliorates the IMQ-induced psoriasis in mouse models .
|
-
- HY-114409
-
|
|
Galectin
|
Cancer
|
|
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model .
|
-
- HY-124733
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism .
|
-
- HY-131004
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
|
-
- HY-106431
-
|
Olpadronate; OLP
|
Others
|
Metabolic Disease
Cancer
|
|
Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid also prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis .
|
-
- HY-126328
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis .
|
-
- HY-127093
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Sedecamycin is an antibiotic, which exhibits antibacterial activity against gram-positive bacteria. Sedecamycin inhibits Treponema hyodysenteriae, with MIC of 0.78 to 12.5 µg/ml. Sedecamycin exhibits protective and therapeutic effect against the swine dysentery in mouse models .
|
-
- HY-155250
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis .
|
-
- HY-162239
-
|
|
Others
|
Cancer
|
|
Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
|
-
- HY-D2376
-
|
|
Fluorescent Dye
|
Cancer
|
|
BH-Vis is a two-photon fluorescent probe that inhibits cell plasma membrane (CPM). BH-Vis has great potential to accurately identify pyroptosis at the cellular level during AAA development in the mouse abdominal aortic aneurysm AAA model .
|
-
- HY-148839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research .
|
-
- HY-165603
-
|
|
Liposome
VEGFR
FGFR
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Si5-N14 is a key component of siloxane-incorporated lipid nanoparticles (SiLNP), possessing pro-vascular repair and anti-tumor activities. In the transgenic GFP mouse model, Si5-N14 can mediate CRISPR-Cas9 editing. In the Lewis lung carcinoma (LLC) tumor-bearing mouse model, Si5-N14 can knock out the expression of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) to exert an anti-tumor effect. In a mouse model of lung injury induced by viral infection, the delivery of Fibroblast Growth Factor-2 (FGF-2) mRNA via Si5-N14 can promote vascular repair, increase blood oxygen levels, and improve lung function. Si5-N14 shows promise for research in the fields of oncology, pneumonia, and cardiovascular diseases .
|
-
- HY-117709
-
|
|
HDAC
|
Neurological Disease
|
|
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .
|
-
- HY-163763
-
|
|
G2A (GPR132)
|
Neurological Disease
|
|
T-10418 is an agonist for G2 accumulation protein (G2A) (also known as G protein-coupled receptor GPR132) with an EC50 of 0.82 μM. T-10418 exhibits a sensitizing effect on mouse primary sensory neurons. T-10418 exhibits good pharmacokinetic characteristics, and no obvious toxicity (at 100 μM) in mouse models .
|
-
- HY-172453
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
XW-032 is an apo-IDO1 inhibitor, with an IC50 of 21 nM. XW-032 (TGI = 63%) exhibits potent in vivo anti-tumor efficacy in the CT26 syngeneic mouse model and is expected to be applied in the research of the field of cancer .
|
-
- HY-P1728
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-137992
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (HY-108345)-induced lung fibrosis mouse model. Aucuparin has anti-inflammatory activity and can inhibit the activation of inflammatory factors by TGF-β .
|
-
- HY-172105
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-NASH agent 2 (compound 21) is an inhibitor of de novo adipogenesis activity and α-SMA gene expression. Anti-NASH agent 2 improves hepatic steatosis, edema, inflammatory infiltrates, and liver fibrosis in NASH mouse models .
|
-
- HY-143464
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease .
|
-
- HY-P10432
-
|
|
Formyl Peptide Receptor (FPR)
|
Others
Inflammation/Immunology
|
|
SHAAGtide is a FPRL1 activator. SHAAGtide has anti-inflammatory activity, mediates its biological activity via FPR2 and is used to reduce the expression of inflammatory cytokines in mouse models. SHAAGtide can be used in the study of diseases such as lung inflammation and fibrosis .
|
-
- HY-169201
-
|
|
Keap1-Nrf2
|
Cancer
|
|
Nrf2 activator-12 (compund 10v) potently activates Nrf2 (EC50=83.5 nM) and exhibits promising pharmacological properties, reversing disease progression and alleviating demyelination in an experimental autoimmune encephalomyelitis mouse model .
|
-
- HY-153482
-
|
|
Small Interfering RNA (siRNA)
|
Cancer
|
|
ATU027 is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
|
-
- HY-A0143
-
-
- HY-153482A
-
|
|
Small Interfering RNA (siRNA)
|
Cancer
|
|
ATU027 sodium is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 sodium has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
|
-
- HY-125850R
-
|
|
Drug Metabolite
HIV
Interleukin Related
|
Infection
Inflammation/Immunology
Cancer
|
|
Berberrubine (chloride) (Standard) is the analytical standard of Berberrubine (chloride). This product is intended for research and analytical applications. Berberrubine chloride is an orally active metabolite of berberine. Berberrubine chloride alleviates mucosal lesions and inflammation in mouse colitis models. Berberrubine chloride has anti-inflammatory, anti-tumor, and antiviral activities .
|
-
- HY-162650
-
|
|
ClpP
|
Cancer
|
|
SL44 is an agonist for human caseinolytic protease P (HsClpP), with an EC50 of 1.30 μM. SL44 inhibits the proliferation of LM3 with an IC50 of 3.1 μM. SL44 induces apoptosis in HCC cells, through the degradation of respiratory chain complex subunits. SL44 exhibits antitumor efficacy in mouse models without obvious toxicity (LD50=400 mg/kg). SL44 exhibits good pharmacokinetic characters in rat models .
|
-
- HY-P10914
-
|
|
MDM-2/p53
Autophagy
|
Inflammation/Immunology
Cancer
|
|
D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
|
-
- HY-158160
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
|
-
- HY-16634
-
|
|
MDM-2/p53
|
Cancer
|
|
MI-888 (TFA) is an orally active MDM2-p53 interaction inhibitor with a Ki of 0.44 nM. MI-888 (TFA) can achieve rapid, complete, and sustained tumor regression in a xenograft mouse model of cancer .
|
-
- HY-111054A
-
|
MDCG sodium
|
Endogenous Metabolite
|
Others
|
|
N-methyl-N-dithiocarboxyglucamine (MDCG) sodium mobilizes and promotes excretion of metallothionein-bound 109Cd in mouse model. N-methyl-N-dithiocarboxyglucamine significantly lowers the Cd content of both the liver and kidney, which is organs most susceptible to Cd-induced toxicity .
|
-
- HY-12788A
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(S)-PF-04449613 is the left-handed isomer of PF-04449613 (HY-12788). PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM. PF-04449613 improves motor learning ability in a mouse model .
|
-
- HY-163159
-
-
- HY-17035R
-
|
|
Parasite
Antibiotic
Bacterial
|
Infection
|
|
Doramectin (Standard) is the analytical standard of Doramectin. This product is intended for research and analytical applications. Doramectin is a derivative of Ivermectin (HY-15310). Doramectin is a potent antiparasitic antibiotic. Doramectin is an active compound against S.mansoni in an NMRI mouse infection model .
|
-
- HY-156111
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
|
-
- HY-161952
-
|
|
SHP2
|
Cancer
|
|
JAB-3312 is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. JAB-3312 has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
|
-
- HY-148230
-
|
|
Interleukin Related
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Others
|
|
TFEB Decoy ODN sodium is a synthetic oligonucleotide with a hairpin ring structure, which were designed to inhibit Transcription factor EB (TFEB). TFEB decoy ODN inhibited fibrosis and autophagy in a UUO mouse model. The TFEB decoy ODNs also showed anti-inflammatory effects.
|
-
- HY-W016794
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
NSC3852 exhibits anti-proliferative activity against cancer cell MCF-7. NSC3852 promotes the ROS generation, DNA damage, and apoptosis in MCF-7. NSC3852 exhibits anti-tumor against leukemia in mouse model
|
-
- HY-P10435
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
|
-
- HY-116266
-
|
|
5-HT Receptor
|
Others
|
|
RS 67333 is a 5-HT4R agonist with stress-preventive activity. RS 67333 attenuates stress-induced body weight changes and prevents depression- and anxiety-like behaviors in two mouse strains tested in different stress models.
|
-
- HY-B0702
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-168169
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-10 (compound 7) is an inhibitor of MAO-A/B with IC50 of 424.1 nM and 177.9 nM, respectively. hMAO-B-IN-10 exerts a certain neuroprotective effect in MPTP (HY-15608)-induced mouse PD model. .
|
-
- HY-157136
-
|
|
CRM1
COX
c-Myc
Survivin
|
Cancer
|
|
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
|
-
- HY-169994
-
-
- HY-163006
-
|
|
EGFR
c-Met/HGFR
|
Cancer
|
|
EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
|
-
- HY-163396
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
|
-
- HY-16160
-
|
|
Autophagy
ICMT
|
Cancer
|
|
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research .
|
-
- HY-149666
-
|
|
DGK
|
Cancer
|
|
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.09 (DGKα) and 0.006 μM (DGKζ) .
|
-
- HY-142221
-
|
|
PD-1/PD-L1
|
Cancer
|
|
ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC50 value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections .
|
-
- HY-149667
-
|
|
DGK
|
Cancer
|
|
BMS-332 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.005 (DGKα) and 0.001 μM (DGKζ) .
|
-
- HY-155109
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-114 is a potent stimulator of interferon genes (STING) agonist. Antitumor agent-114 activates immunity and reduces tumor volume in a mouse model of breast cancer. Antitumor agent-114 can be used for immunity and cancer diseases research .
|
-
- HY-158093
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages .
|
-
- HY-155642
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
PU-48 is a potent urea transporters A (UT-A) inhibitor (IC50=0.32 μM). PU-48 has a good diuretic effect in mouse models, and shows little or no cytotoxicity. PU-48 has the potential to be developed as a diuretic .
|
-
- HY-10596
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model .
|
-
- HY-B0149S3
-
|
Cyclocapron-13C2,15N
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
|
-
- HY-156881
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
Apoptosis
|
Cancer
|
|
PARG-IN-4 (Formula (A)) is an orally available PARG inhibitor (EC50=1.9 nM) with cell membrane permeability. PARG-IN-4 can effectively inhibit tumor growth in mouse models. PARG-IN-4 can be used in cancer research .
|
-
- HY-100827
-
|
LF22-0542
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
|
-
- HY-124875
-
|
HIF inhibitor 64B
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
|
|
Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .
|
-
- HY-114977
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Avenanthramide A is a phytoalexin, which can be found in oats (Avena sativa L.). Avenanthramide A targets the RNA helicase DDX3, leads to mitochondrial swelling and increased ROS production, and induces apoptosis in CRC cells. Avenanthramide A exhibits antitumor efficacy in mouse model. Avenanthramide A orally active .
|
-
- HY-169310
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
|
-
- HY-N2909
-
|
|
NF-κB
RIP kinase
Mixed Lineage Kinase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models .
|
-
- HY-P99351
-
|
Anti-MMP9 Reference Antibody (andecaliximab)
|
MMP
|
Cancer
|
|
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-168045
-
|
|
HBV
DNA/RNA Synthesis
|
Infection
|
HBV-IN-48 is an HBV inhibitor. HBV-IN-48 has antiviral activity against HBV in HepDE19 cells, with an EC50 value of 0.005 μM. HBV-IN-48 can reduce serum HBV DNA levels in mouse models of HBV infection .
|
-
- HY-N2195R
-
|
(+)-Nootkatone (Standard)
|
Interleukin Related
TNF Receptor
|
Neurological Disease
|
|
Nootkatone (Standard) is the analytical standard of Nootkatone. This product is intended for research and analytical applications. Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects[1]. Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease[2].
|
-
- HY-16726
-
|
CG100649
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-168489
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
OBI-992 drug-linker is a drug-linker conjugate composed of a TOP I inhibitor Exatecan (HY-13631) and a linker. OBI-992 drug-linker exhibits antitumor property in mouse models and can be used for synthesis of ADC OBI-992 .
|
-
- HY-14833
-
|
TP300
|
Topoisomerase
|
Cancer
|
|
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
|
-
- HY-P1728A
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-122989
-
|
|
DYRK
|
Inflammation/Immunology
|
|
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models .
|
-
- HY-135217
-
|
|
Apoptosis
|
Cancer
|
|
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-108678
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Neurological Disease
|
|
TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models .
|
-
- HY-162573
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
|
-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-126242S
-
|
|
JAK
|
Inflammation/Immunology
|
|
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model .
|
-
- HY-173117
-
|
|
CaMK
|
Cardiovascular Disease
Cancer
|
|
RA306 is an orally active CAMK2 inhibitor. RA306 can block the PEAK1/CAMK2 signaling pathway. RA306 inhibits the proliferation, migration, and invasion of breast cancer cells and has anti-tumor activity. In addition, RA306 can improve dilated cardiomyopathy in mice and can be used in the research of heart diseases .
|
-
- HY-P1120
-
|
|
Formyl Peptide Receptor (FPR)
PERK
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
WKYMVm is a selective formylpeptide receptor 2 (FPR2) agonist. WKYMVm has a powerful anti-inflammatory effect that can reduce lung injury and spinal cord injury. WKYMVm ameliorates obesity by regulating lipid metabolism and leptin signaling. WKYMVm is involved in the regulation of immune cells by activating FPRs. WKYMVm can promote the chemotactic migration of immune cells and inhibit the apoptosis of phagocytes. In addition, WKYMVm may play a favorable or unfavorable role in tumors, depending on the type of tumor .
|
-
- HY-149035
-
|
|
Others
|
Cancer
|
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
|
-
- HY-24504
-
-
- HY-176163
-
|
|
HSV
|
Infection
|
|
HSV-1-IN-2 (compound 5i) is a potent Herpes simplex virus type 1 (HSV-1) inhibitor with an EC50 of 1.95 μM. HSV-1-IN-2 inhibits apoptosis and improves herpes encephalitis model mouse survival .
|
-
- HY-117366
-
|
|
PKC
|
Cancer
|
|
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
|
-
- HY-N2707
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Cancer
|
|
6-Deoxyjacareubin is a natural xanthone, that can be isolated from the leaves of Vismia latifolia. 6-Deoxyjacareubin protects against non-apoptotic cell death by inhibiting ROS production. 6-Deoxyjacareubin ameliorates neurodegeneration in a mouse model of familial amyotrophic lateral sclerosis (ALS) .
|
-
- HY-106781A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
OPC 4392 hydrochloride is an agonist for presynaptic dopamine receptor and an antagonist for postsynaptic D2 receptor. OPC 4392 reverses the Reserpine (HY-N0480)-induced dopamine accumulation, inhibits Apomorphine (HY-12723)-induced stereotypic and climbing behaviors in mouse models .
|
-
- HY-123891
-
|
|
EGFR
|
Cancer
|
|
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
|
-
- HY-162790
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SARS-CoV-2-IN-95 (Compound 10) is an inhibitor for SARS-CoV-2 PLpro with an IC50 of 0.39 μM. SARS-CoV-2-IN-95 exhibits antiviral activity in mouse SARS-CoV-2-infected model .
|
-
- HY-136990
-
|
|
Others
|
Cancer
|
|
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
|
-
- HY-168331
-
|
|
FXR
|
Others
|
|
FXR agonist 10 (Compound 27) is an agonist for FXR with an EC50 of 14.26 μM. FXR agonist 10 upregulates the expression of SHP and BSEP proteins, downregulates the expression of NTCP and CYP7A1 proteins. FXR agonist 10 ameliorates the ANIT-induced cholestasis in mouse model .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613); EP-100
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-114483
-
AES-135
1 Publications Verification
|
HDAC
|
Cancer
|
|
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM .
|
-
- HY-149708
-
|
|
ICMT
|
Others
|
|
UCM-13207 (compound 21) is a selective ICMT inhibitor that ameliorates basic progeria-like features. UCM-13207 can improve the survival rate of LmnaG609G/G609G mice in the mouse premature aging model .
|
-
- HY-131902
-
|
|
MALT1
|
Cancer
|
|
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse .
|
-
- HY-132166
-
|
IDRX-42
|
c-Kit
PDGFR
c-Fms
FLT3
Src
|
Cancer
|
|
M4205 is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. M4205 exhibits antitumor efficacy in xenograft mouse models .
|
-
- HY-161519
-
|
|
Pyruvate Kinase
|
Inflammation/Immunology
|
|
PKM2 activator 7 (Compd B4) is a PKM2 activator with the AC50 of 0.144 μM. PKM2 activator 7 suppresses DSS (HY-116282C)-induced colitis by inhibiting T cell growth in mouse colitis model .
|
-
- HY-156681A
-
|
|
PI3K
|
Cancer
|
|
(S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
|
-
- HY-116504
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
|
-
- HY-170570
-
|
|
LXR
Stearoyl-CoA Desaturase (SCD)
Fatty Acid Synthase (FASN)
|
Cancer
|
|
PFM046 is the antagonist for liver X receptor (LXR), that inhibits the activation of LXRα and LXRβ with IC50 of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models .
|
-
- HY-129331
-
|
|
Antibiotic
Bacterial
Fungal
|
Infection
Cancer
|
|
Neothramycin A is an antibiotic, which can be isolated from Streptomyces. Neothramycin A exhibits board spectrum antimicrobial activity, inhibits Staphylococcus aureus, Klebsiella pneumoniae, Escherichia coli W677, and Saccharomyces cerevisia with MIC of 25-50 μg/mL. Neothramycin A exhibits antitumor efficacy against leukemia in mouse models .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-117862
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
TASP0412098 is an orally available, potent and selective CRTH2/DP2 antagonist with high binding affinity (IC50 2.1 nM) and functional activity (IC50 12 nM). TASP0412098 has the potential to suppress asthma in mouse and guinea pig bronchial asthma models .
|
-
- HY-147936
-
|
|
MMP
|
Inflammation/Immunology
|
|
TP0556351 is a potent and selective matrix metalloproteinase-2 (MMP2) inhibitor with an IC50 value of 0.2 nM. TP0556351 reduces the amount of collagen in the lungs of a Bleomycin-induced pulmonary fibrosis mouse model. TP0556351 can be used for researching idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-153468
-
|
|
Sodium Channel
TRP Channel
|
Cancer
|
|
ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy exhibits low nanomolar cytotoxicity in ERα+ breast cancer cell lines (IC50 = 5-25 nM) through induction of necrosis. ErSO-TFPy exhbits antitumor efficacy in mouse models .
|
-
- HY-W753791
-
|
|
TNF Receptor
JNK
|
Neurological Disease
Inflammation/Immunology
|
|
(±)-Perillaldehyde has an antidepressant effect by modulating the olfactory nervous system in a mouse model of stress-induced depression. (±)-Perillaldehyde also has anti-inflammatory activity, inducing JNK activation in RAW264.7 cells and inhibiting the expression of TNF-α, with an IC50 of 171.7 μM .
|
-
- HY-138007
-
|
|
ROR
PPAR
LXR
|
Metabolic Disease
Inflammation/Immunology
|
|
SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models .
|
-
- HY-N15497
-
|
|
Reactive Oxygen Species
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Terpestacin is found in Phoma exigua var. heteromorpha. Terpestacin binds to UQCRB to inhibit the production of mitochondrial ROS and HIF-1α. Terpestacin inhibits tumor angiogenesis in the FM3A breast cancer cell xenograft mouse model. Terpestacin has antitumor activity and phytotoxicity .
|
-
- HY-160021
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
|
-
- HY-120777
-
|
|
Bacterial
|
Others
|
|
GSK729 is a THPP inhibitor with the activity of inhibiting EchA6 and inhibiting Mycobacterium tuberculosis. GSK729 can selectively pull down EchA6 in a stereospecific manner, inhibit its activity, inhibit fatty acid synthesis of Mycobacterium tuberculosis, and has a bactericidal effect in a mouse chronic tuberculosis infection model.
|
-
- HY-173601
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK3-IN-17 is an orally active JAK3 inhibitor (IC50: 14.56 nM). JAK3-IN-17 inhibits the production of IL-2 and IL-6 in a DNCB-induced mouse atopic dermatitis model and exhibits anti-inflammatory activity .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-121365
-
|
|
Bacterial
|
Infection
|
|
Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
|
-
- HY-152293
-
|
|
VEGFR
ERK
|
Cancer
|
|
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-168731
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-25 (Compound 6e) is the orally active inhibitor for hAChE and eqBChE with IC50 of 7.9 nM and 0.79 nM. AChE/BChE-IN-25 exhibits antioxidant activity, that scavenges free radical with IC50 of 22.91 μM. AChE/BChE-IN-25 exhibits neuroprotective effects by reducing mitochondrial and cellular oxidative stress in the Drosophila Alzheimer's disease model. AChE/BChE-IN-25 ameliorates Scopolamine (HY-N0296)-induced spatial and cognitive memory impairment in mouse model .
|
-
- HY-N0830
-
-
- HY-114360AS1
-
|
|
Isotope-Labeled Compounds
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Taurohyodeoxycholic acid-d4 (sodium) is a deuterated labeled Taurohyodeoxycholic acid (sodium) . Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
|
-
- HY-142520
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .
|
-
- HY-N0830B
-
|
|
Biochemical Assay Reagents
HSP
Endogenous Metabolite
|
Cancer
|
|
Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
|
-
- HY-W016868
-
|
|
Hydroxycarboxylic Acid Receptor (HCAR)
|
Metabolic Disease
|
|
3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity .
|
-
- HY-N3312R
-
|
|
Endogenous Metabolite
|
Infection
|
|
Matairesinol (Standard) is the analytical standard of Matairesinol. This product is intended for research and analytical applications. Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-172115
-
|
|
TrxR
Apoptosis
|
Cancer
|
|
BGC4 is a biphenyl-based gold(III) complex. BGC4 inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity (IC50 for MDA-MB-231 is 5.4 μM), and induces apoptosis. BGC4 exhibits antitumor efficacy in mouse models .
|
-
- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
|
NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
|
-
- HY-156920
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
Cancer
|
|
VDX-111 is an analog of vitamin D. VDX-111 exhibits cytotoxicity in ovarian cancer cells through upregulation of RIPK1/RIPK3 pathway and induction of necroptosis. VDX-111 promotes expressions of cytokines and exhibits antitumor activity in mouse model .
|
-
- HY-P10414A
-
|
KP1 (human) hydrochloride
|
TGF-beta/Smad
p38 MAPK
|
Inflammation/Immunology
|
|
Klotho-derived peptide 1 (KP1 human) hydrochloride blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
|
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-155556
-
|
|
ClpP
|
Cancer
|
|
ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
|
-
- HY-120041
-
|
|
IRAK
|
Cancer
|
|
ND-2158 is a competitive IRAK4 inhibitor, with the Ki of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo .
|
-
- HY-170361
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
MTHFD2-IN-5 (Compound 16e) is a selective inhibitor for MTHFD2 with an IC50 of 66 nM. MTHFD2-IN-5 inhibits the proliferation of MOLM-14 with a GI50 of 720 nM. MTHFD2-IN-5 exhibits antitumor efficacy in mouse models .
|
-
- HY-P10414
-
|
KP1 (human)
|
TGF-beta/Smad
p38 MAPK
|
Inflammation/Immunology
|
|
Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
|
-
- HY-170850
-
|
|
Kinesin
|
Cancer
|
|
MKLP2-IN-1 (compound 12a) is an inhibitor of MKLP2 with good oral bioavailability. MKLP2-IN-1 inhibits the microtubule-stimulated ATPase activity of recombinant MKLP2 in vitro and suppresses tumor growth in a mouse Calu-6 lung cancer model .
|
-
- HY-168327
-
|
|
FXR
|
Inflammation/Immunology
|
|
LH10 is a fexaramine-based agonist for FXR with an EC50 of 0.14 μM. LH10 exhibits liver protection efficacy, ameliorates the alpha naphthylisothiocyanate (ANIT)-induced cholestasis, APAP (HY-66005)-induced acute liver injury and non-alcoholic steatohepatitis (NASH) in mouse models .
|
-
- HY-169420
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
IL-6-IN-1 (Compound 22) inhibits the release of IL-6 with an IC50 of 1.065 μM. IL-6-IN-1 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced acute lung injury in mouse model .
|
-
- HY-13508
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .
|
-
- HY-176141
-
|
|
Trace Amine-associated Receptor (TAAR)
|
Neurological Disease
|
|
ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research .
|
-
- HY-P10019
-
|
|
GCGR
|
Neurological Disease
|
|
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
|
-
- HY-P2032
-
|
|
Endogenous Metabolite
|
Infection
Cancer
|
|
Cyclochlorotine is a mycotoxin that can be extracted from the yellow rice infectant Penicillium islandicum Sopp. Cyclochlorotine promotes glycogenolysis, inhibits glycogen synthesis, affects fat synthesis and protein synthesis in liver cells. Cyclochlorotine exhibits chronic toxicity in liver that induces liver fibrosis and cirrhosis in mouse models. Cyclochlorotine exhibits carcinogenicity .
|
-
- HY-N0109R
-
|
Rhodioloside (Standard)
|
Prolyl Endopeptidase (PREP)
mTOR
Apoptosis
PINK1/Parkin
|
Cancer
|
|
Salidroside (Standard) is the analytical standard of Salidroside. This product is intended for research and analytical applications. Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
|
-
- HY-123334
-
|
|
Porcupine
Wnt
|
Cancer
|
|
GNF-1331 (compound 19) is a potent, selective and orally bioavailable porcupine inhibitor (IC50=12 nM). GNF-1331 blocks Wnt ligand secretion and subsequent Wnt signaling activity, and induces significant antitumor effects in the mouse MMTV-WNT1 xenograft tumor model .
|
-
- HY-101096
-
|
MK-8998; CX-8998; JZP385
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-120027
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Kribb3 is an inhibitor for microtubule. KRIBB3 inhibits the proliferation of cancer cells with GI50 of 0.2-2.5 μM, arrests cell cycle at G2/M phase, and induces apoptosis in HCT-116. Kribb3 exhibits antitumor activity in mouse models .
|
-
- HY-157847
-
|
|
STAT
|
Cancer
|
|
Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
|
-
- HY-170453
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
|
-
- HY-117985A
-
|
DA-1229 hydrochloride
|
Dipeptidyl Peptidase
|
Metabolic Disease
Endocrinology
|
|
Evogliptin hydrochloride (DA-1229 hydrochloride) is an orally available DPP4 inhibitor with significant and durable hypoglycemic effects in mouse models. Evogliptin hydrochloride also inhibits the generation of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin hydrochloride can be used in the research of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-14849
-
|
Razupenem; SM 216601; SMP 601
|
Antibiotic
Bacterial
|
Others
|
|
PTZ601 (SMP 601) is an antibiotic, which inhibits the gram-positive bacteria, including the Vancomycin (HY-B0671)-resistant Enterococcus faecium (VREF) and Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA). PTZ601 exhibits antimicrobial activity in infected mouse models .
|
-
- HY-W091169
-
|
2-((Methylamino)methyl)phenol hydrochloride
|
Reactive Oxygen Species
|
Cardiovascular Disease
Inflammation/Immunology
|
|
N-Methyl-2-HOBA (2-((Methylamino)methyl)phenol) hydrochloride is a methylated form of the isoketal scavenger 2-HOBA (HY-34350). N-Methyl-2-HOBA hydrochloride can be used as a negative control for the activity of 2-HOBA in a mouse model of hypertension .
|
-
- HY-148923
-
|
|
STAT
|
Cancer
|
|
MC0704 is a STAT3 inhibitor with an IC50 value of 2.13 μM. MC0704 induces cell apoptosis and cell cycle arrest. MC0704 shows antitumor activity in mouse breast cancer models. MC0704 can be used for the research of metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-168563
-
|
|
Cholinesterase (ChE)
FAAH
|
Neurological Disease
|
|
BuChE-IN-15 (compound D12) is a selective BuChE/FAAH dual inhibitor with and show IC50 values of 81 and 400 nM for hBuChE and hFFAH, respectively. BuChE-IN-15 possesses good BBB penetration, and shows neuroprotection.BuChE-IN-15 can be used for study of Alzheimer .
|
-
- HY-163534
-
|
|
PD-1/PD-L1
|
Cancer
|
PD-1/PD-L1-IN-43 (compound Z13) is a small-molecule inhibitors targeting the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-43 exhibites potent in vivo antitumor efficacy against B16-F10 melanoma. PD-1/PD-L1-IN-43 inhibits tumor growth by blocking the interaction between PD-1 and PD-L1. PD-1/PD-L1-IN-43 can be used in anti-tumor studies .
|
-
- HY-147429
-
|
Abx MCP; RG6006
|
Bacterial
Antibiotic
|
Infection
|
|
Zosurabalpin is a polypeptide antibiotic targeting LPS transporter (LptB2FGC complex), which can block the transport of LPS and lead to endotoxin accumulation in cells, and has shown excellent antibacterial activity against Carbapenem-resistant Acinetobacter baumanni (CRAB) .
|
-
- HY-148625
-
-
- HY-173317
-
|
|
STING
Interleukin Related
|
Inflammation/Immunology
|
|
STING-IN-13 is a selective STING inhibitor. STING-IN-13 can effectively inhibit downstream signaling of the STING pathway and inhibit STING-mediated inflammation. STING-IN-13 has low toxicity and can be used to study STING-related inflammatory and autoimmune diseases .
|
-
- HY-15582
-
|
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
|
-
- HY-159937
-
|
|
Wee1
CDK
|
Cancer
|
|
PKMYT1-IN-7 (compound 7) is an orally active PKMYT1 inhibitor with IC50 values of 1.6 nM and 0.06 μM against of PKMYT1 and pCDK1, respectively. PKMYT1-IN-7 suppresses the phosphorylation of CDK1 at T14 and Y15. PKMYT1-IN-7 shows anticancer activity both < and < .
|
-
- HY-117356B
-
|
|
P2Y Receptor
NF-κB
ERK
|
Cardiovascular Disease
|
|
MRS2693 trisodium is a selective P2Y6 agonist with an EC50 value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model .
|
-
- HY-B1606
-
|
Chlorthymol; 6-Chlorothymol
|
GABA Receptor
Bacterial
|
Neurological Disease
Inflammation/Immunology
|
|
Chlorothymol (Chlorthymol) is a potent GABAA receptor subunit LGC-37 positive modulator. Chlorothymol is an effective anticonvulsant. Chlorothymol is protective in several mouse seizure assays, including the 6-Hz 44-mA model of pharmacoresistant seizures. Chlorothymol possess GABAergic, membrane-modifying, antioxidant and topical antiseptic properties .
|
-
- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
|
-
- HY-169074
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-N-methylpiperazine is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-N-methylpiperazine can be used to synthesize PROTAC MLKL Degrader-2 (HY-169072) to exhibit antinecroptotic activity on human cell lines and effectively degrade MLKL in the HT-29 xenograft mouse model .
|
-
- HY-114196
-
|
ZGN-1061
|
MetAP
|
Metabolic Disease
|
|
Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells .
|
-
- HY-N0830A
-
|
|
HSP
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Palmitic acid calcium is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid calcium is used to establish a cell steatosis model .
|
-
- HY-10834
-
|
|
β-catenin
|
Cancer
|
|
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway. β-catenin-IN-6 inhibits human colorectal cancer cells proliferation, as well as in a β-catenin/RK3E mouse model .
|
-
- HY-168212
-
-
- HY-162632
-
|
|
Akt
CXCR
|
Inflammation/Immunology
|
|
Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC50 of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models .
|
-
- HY-169057
-
|
|
IRAK
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
BI1543673 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. BI1543673 can reduce the inflammatory response stimulated by TLR4 and TLR7/8 in human lung tissue. BI1543673 can decrease inflammatory signaling in a mouse model of lung inflammation induced by LPS .
|
-
- HY-A0143A
-
|
DGLA sodium; all-cis-8,11,14-Eicosatrienoic acid sodium
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid (DGLA; all-cis-8,11,14-Eicosatrienoic acid) sodium is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid (sodium) attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-145830
-
|
|
Adenylate Cyclase
|
Neurological Disease
|
|
AC1-IN-1 is a potent and selective Adenylyl cyclase type 1 (AC1) inhibitor with an IC50 of 0.54 µM. AC1-IN-1 displays modest antiallodynic effects in a mouse model of inflammatory pain. AC1-IN-1 has CNS activity .
|
-
- HY-13762S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-158766
-
|
3-Succinylated cholic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
3-sucCA (3-Succinylated cholic acid) is a microbial derived bile acid. 3-sucCA is a lumen-restricted metabolite and alleviates alleviates MAFL-MASH progression in mouse models by reshaping the gut microbiota, especially by promoting the growth of Akkermansia muciniphila. 3-sucCA levels are lower in patients with biopsy-proven MAFLD .
|
-
- HY-136181A
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-170506
-
|
|
Others
|
Inflammation/Immunology
|
|
KB-208 is a phagocytosis inhibitor that improves immune thrombocytopenia (ITP) in mouse models at a dose of 1 mg/kg. KB-208 does not affect other blood parameters and does not elevate serum toxicity biomarkers. KB-208 can be used in immunology research .
|
-
- HY-106431R
-
|
Olpadronate (Standard); OLP (Standard)
|
Others
|
Metabolic Disease
Cancer
|
|
Olpadronic acid (Standard) is the analytical standard of Olpadronic acid. This product is intended for research and analytical applications. Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid also prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis .
|
-
- HY-120633
-
|
|
LPL Receptor
|
|
|
BMS-986104 is a potent and selective S1P1 receptor modulator. BMS-986104 is effective in a mouse EAE model, which is comparable to FTY720. Mechanistically, BMS-986104 exhibites excellent remyelinating effects on lysophosphatidylcholine (LPC)-induced demyelination in a three-dimensional brain cell culture assay.
|
-
- HY-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-148178
-
|
|
Parasite
|
Infection
|
|
MMV688533 is an antimalarial agent with rapid anti-plasmodial activity and effective single-dose activity against Plasmodium falciparum infection in humanized mouse models. MMV688533 can inhibit the activity of asexual blood stage parasites with an IC50 value of 1.3 nM. MMV688533 exhibits excellent pharmacokinetic properties and safety .
|
-
- HY-148838
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research .
|
-
- HY-120118
-
|
ML246
|
DNA/RNA Synthesis
|
Cancer
|
|
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models .
|
-
- HY-136181
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- HY-169853
-
|
|
VISTA
|
Inflammation/Immunology
|
|
M351-0056 is the agonist for the immune checkpoint protein VISTA, that reduces the secretion of VISTA-induced cytokines, promotes the T-cell proliferation induced by VISTA, and exhibits immunomodulatory activity. M351-0056 ameliorates Imiquimod (HY-B0180)-induced psoriatic dermatitis in mouse models .
|
-
- HY-170434
-
|
|
Bcl-2 Family
Caspase
|
Cancer
|
|
Bfl-1-IN-6 (Compound 20) is an orally active inhibitor for Bcl-2 related protein A1 (BFL1) with an IC50 of 19 nM. Bfl-1-IN-6 stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor efficacy in mouse models .
|
-
- HY-164285
-
|
|
ADC Cytotoxin
N-myristoyltransferase
|
Cancer
|
|
MYX1715 is an inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. MYX1715 inhibits the proliferation of LU0884 and LU2511 with IC50 values of 44 nM and 9 nM. MYX1715 exhibits antitumor efficacy against neuroblastoma and gastric cancer in mouse models. MYX1715 can be used as ADC toxin .
|
-
- HY-168733
-
|
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
|
LDHA-IN-9 (Compound 1g) is an inhibitor for LDH-A with an IC50 of 25 nM. LDHA-IN-9 inhibits the proliferation of DLD-1 cell (GI50 of 27 μM) through apoptosis induction. LDHA-IN-9 exhibits antitumor activity in mouse model without significant toxicity (25 mg/kg) .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-P99604
-
|
AZD-1061; COV2-2130
|
SARS-CoV
|
Infection
|
|
Cilgavimab (AZD-1061; COV2-2130) is a human SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection .
|
-
- HY-155681
-
|
|
PD-1/PD-L1
Monoamine Oxidase
|
Cancer
|
|
SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%) .
|
-
- HY-W112239
-
|
|
Reactive Oxygen Species
Fluorescent Dye
|
Cancer
|
|
BDPI is the a BODIPY derivative. BDPI reveals a high O2 quantum yield and exhibits phototoxicity that inhibits HeLa with an IC50 of 0.6 µg/mL. BDPI nanoarticles can be taken up by HeLa, producing fluorescence signals in the cells, and can be used as cell imaging agent. BDPI nanoarticles exhibit antitumor efficacy in mouse models .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-139915
-
|
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-155740
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability .
|
-
- HY-170760
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 258 (Compound 11e) is an antibacterial agent, that destory the bacteria cell membrane, and inhibits various gram-positive bacteria (MIC for Staphylococcus aureus is 1-2 μg/mL). Antibacterial agent 258 exhibits low hemolytic activity and low cytotoxicity. Antibacterial agent 258 exhibits anti-infectious efficacy in mouse models .
|
-
- HY-105321R
-
|
PBT 2 (Standard)
|
Bacterial
|
Neurological Disease
|
|
PBT 1033 (Standard) is the analytical standard of PBT 1033. This product is intended for research and analytical applications. PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria .
|
-
- HY-B1864C
-
|
Ksg sulfate
|
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
|
-
- HY-149631
-
|
|
HDAC
|
Cancer
|
|
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
|
-
- HY-149950
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 106 (compound 10ic) is an anticancer agent that induces apoptosis in B16-F10 melanoma cells. Anticancer agent 106 also potently inhibits metastatic nodules in a mouse model of lung metastatic melanoma. Anticancer agent 106 can be used in the study of cancer, especially lung metastatic melanoma .
|
-
- HY-170503
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-20 (Compound A49) is an inhibitor for methionine adenosyltransferase 2A (MAT2A) with an IC50 ≤50 nM. MAT2A-IN-20 inhibits human UGT1A1 with an IC50 of 28.45 μM. MAT2A-IN-20 exhibits antitumor in mouse models .
|
-
- HY-164799
-
|
|
FXR
|
Inflammation/Immunology
|
|
FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models .
|
-
- HY-P1709
-
|
|
Bacterial
|
Infection
|
|
Protactin is a pentapeptide lactone produced by Streptomyces cucumeris strain L703-4 (ATCC 53784) with significant antioxidant properties. Protactin can be converted to actinomycin Zp by ferrocyanide oxidation. Actinomycin Zp exhibits potent antibacterial activity in vitro and has significant antitumor effects against P-388 leukemia in a mouse model .
|
-
- HY-117985
-
|
DA-1229
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
Inflammation/Immunology
|
|
Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-150307
-
|
|
Protein Arginine Deiminase
|
Inflammation/Immunology
|
|
KP-302 (compound 23) is a selective inhibitor of protein arginine deaminase PAD2 with a Ki of 60 μM. KP-302 also reversed physical disability in the EAE mouse model of multiple sclerosis (MS) and eliminated T cell infiltration in the brain. KP-302 has the potential to be a disease-modifying agent for MS .
|
-
- HY-163760
-
|
|
HuR
MMP
|
Cancer
|
|
ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .
|
-
- HY-172870
-
-
- HY-162901
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3-IN-48 is an NLRP3 inhibitor. NLRP3-IN-48 targets the NLRP3 protein, affecting the assembly of the NLRP3 inflammasome and thereby inhibiting its activation. NLRP3-IN-48 has anti-inflammatory activity in a mouse model of acute colitis induced by DSS .
|
-
- HY-168329
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
TGR5 agonist 7 (Compound 22-Na) is a gut-restricted, orally active agonist for G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 < 1 μM. TGR5 agonist 7 exhibits blood glucose lowering effect in mouse model, and can be used in diabete research .
|
-
- HY-170523
-
|
|
SARS-CoV
DNA Methyltransferase
|
Infection
|
|
RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models .
|
-
- HY-159088
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
|
-
- HY-12797
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
GF 15 is an inhibitor of centrosomal clustering during cell mitosis, with an EC50 value of 900 nM for inducing multipolar spindles. GF 15 is a derivative of griseofulvin that inhibits tubulin polymerization at concentrations above 25 μM. GF 15 inhibits tumor growth and significantly prolongs survival in mouse xenograft models of human colon cancer and multiple myeloma .
|
-
- HY-100443
-
|
PX-102
|
FXR
|
Cancer
|
|
PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy .
|
-
- HY-159886
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
MG-C-30 is an orally active agonist for CD27 with an EC50 of 0.84 μM. MG-C-30 activates NK cells and T cell co-stimulatory signals, and enhances immune response. MG-C-30 exhibits antitumor efficacy in mouse EG7-OVA model .
|
-
- HY-161768
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC50 of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model .
|
-
- HY-170396
-
|
|
BCRP
|
Inflammation/Immunology
|
|
ABCG2-IN-4 (Compound K31) is an orally active inhibitor for ABCG2, which reduces the release of Protoporphyrin IX (PPIX) (HY-B1247) from erythrocytes into plasma, and prevents the reduces phototoxicity. ABCG2-IN-4 exhibits anti-inflammatory and antioxidant activity in mouse models .
|
-
- HY-12768B
-
|
BLZ945 dihydrochloride
|
c-Fms
|
Neurological Disease
Cancer
|
|
Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
|
-
- HY-160514
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LXQ46 is an orally active inhibitor for protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 0.190 μM. LXQ46 enhances insulin and leptin signaling pathways in insulin-resistant C2C12. LXQ46 ameliorates type 2 diabetes and increases insulin tolerance in mouse models .
|
-
- HY-18112
-
|
|
Beta-secretase
|
Neurological Disease
|
|
AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research .
|
-
- HY-172087
-
|
|
VD/VDR
|
Inflammation/Immunology
|
|
VDR agonist 3 (Compound E15) is a potent vitamin D receptor (VDR) agonist. VDR agonist 3 can effectively inhibit HSC activation through VDR. VDR agonist 3 significantly reduces liver fibrosis without causing hypercalcemia in a CCl4-induced mouse liver fibrosis model .
|
-
- HY-B0702R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline (Standard) is the analytical standard of Nicergoline. This product is intended for research and analytical applications. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-122664
-
|
|
BRK
|
Cancer
|
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
- HY-169411
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-77 (Compound H7) is a non-competitive inhibitor for α-glucosidase with an IC50 of 1.25 μM. α-Glucosidase-IN-77 lowers blood glucose levels, improves glucose tolerance, regulates intestinal microbiota, and exhibits hepatoprotective effect in mouse type 2 diabetes model .
|
-
- HY-117839
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
|
-
- HY-170780
-
|
|
Parasite
Dihydroorotate Dehydrogenase
|
Infection
|
|
DSM1465 (Compound 82) is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 value of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites with an EC50 value of 1.4 nM. DSM1465 shows potent in vivo activity in the humanized P. falciparum mouse model .
|
-
- HY-B1864B
-
|
Ksg hydrochloride hydrate
|
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
|
-
- HY-135432
-
|
APD334 arginine
|
LPL Receptor
|
Inflammation/Immunology
|
|
Etrasimod arginine is an orally available S1P receptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4 +CD45RB high T cell-transferred mouse colitis model .
|
-
- HY-110216
-
|
|
CRAC Channel
|
Inflammation/Immunology
|
|
5J-4 is a potent CRAC inhibitor. 5J-4 decreases the numbers of infiltrated mononuclear cell into the CNS, and significantly decreases the population of infiltrated CD4+ population. 5J-4 reduces the symptoms and delayed the onset of EAE (experimental autoimmune encephalomyelitis) in mouse model of inflammation .
|
-
- HY-B1864A
-
|
Ksg hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
|
-
- HY-163803
-
|
|
HDAC
DNA Methyltransferase
|
Cancer
|
|
CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models .
|
-
- HY-P991310
-
|
LT3015; LT-3000
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Lpathomab (LT3015; LT-3000) is a human IgG1 monoclonal antibody (mAb) targeting LPA. Lpathomab reduces the release of IL-8 and IL-6 cytokines in SKOV3 cells and blocks LPA-triggered tumor cell migration. Lpathomab reduces neovascularization in Matrigel plug and CNV models. Lpathomab inhibits brain injury in the CCI mouse model. Lpathomab can be used in the study of brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-139815
-
|
|
HDAC
|
Cancer
|
|
ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
|
-
- HY-123439
-
|
|
Others
|
Neurological Disease
|
|
FTY720-C2 is a derivative of FTY72 (HY-12005). FTY720-C2 promotes the expression of brain-derived neurotrophic factor (BDNF) and glial cell-derived neurotrophic factor (GDNF) in multiple system atrophy (MSA) models, without causing immunosuppression. FTY720-C2 improves motor dysfunction and reduces the levels of insoluble alpha-synuclein (αSyn) in MSA mouse models. FTY720-C2 is blood-brain barrier penetrate .
|
-
- HY-173024
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
|
-
- HY-122906
-
|
|
c-Fms
|
Inflammation/Immunology
|
|
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis .
|
-
- HY-135217R
-
|
|
Apoptosis
|
Cancer
|
|
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-158812
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
Eicosapentaenoyl-L-carnitine chloride is a long-chain acylcarnitine composed of Eicosapentaenoic Acid (HY-B0660) and L-Carnitine (HY-B0399). The levels of Eicosapentaenoyl-L-carnitine chloride are increased in the eyes of mice fed a diet high in n-3/n-6 polyunsaturated fatty acids (PUFAs) in a mouse model of myopia induced by out-of-focus lenses .
|
-
- HY-169347
-
|
LC-05-004
|
Molecular Glues
Casein Kinase
|
Cancer
|
|
dCK1α-2 is an orally active CK1α molecular glue degrader that targets p53 pathway-related targets. dCK1α-2 exhibits anti-tumor efficacy in mouse models and can increase the expression of p53-related genes. .
|
-
- HY-149417
-
|
|
HDAC
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research .
|
-
- HY-172953
-
|
|
Parasite
|
Infection
|
|
Insecticidal agent 24 is an orally active pyridylspiroindoline frontrunner. Insecticidal agent 24 has antiplasmodial activity (Pf NF54 IC50: 0.08 μM). Insecticidal agent 24 inhibits hERG activity (IC50: 6.5 μM). Insecticidal agent 24 reduces parasitemia in a humanized immunodeficient NSG mouse Plasmodium falciparum infection model .
|
-
- HY-170575
-
|
|
Bacterial
|
Infection
|
|
Pks13-IN-1 (Compound 44) is an orally active inhibitor for Mycobacterium tuberculosis Polyketide synthase 13 (Pks13). Pks13-IN-1 inhibits M. tuberculosis strain H37Rv with a MIC of 0.07 μM. Pks13-IN-1 exhibits antibacterial efficacy in mouse model .
|
-
- HY-B0702S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-121490
-
|
|
Apoptosis
|
Cancer
|
|
IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
|
-
- HY-123033A
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-162882
-
|
|
Xanthine Oxidase
Reactive Oxygen Species
|
Metabolic Disease
|
CC15009 is a xanthine oxidoreductase (XOR) inhibitor, with an IC50 value of 0.237 nM. CC15009 can inhibit the oxidative subtype of XOR, thereby reducing the production of the byproduct ROS and exhibiting antioxidant activity. CC15009 has demonstrated a good dose-dependent uric acid-lowering effect in two different mouse models of hyperuricemia induced by XOR substrates .
|
-
- HY-125650
-
|
PUM
|
Antibiotic
DNA/RNA Synthesis
Bacterial
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Pseudouridimycin (PUM) is an antibiotic that selectively inhibits bacterial RNA polymerase (RNAP), with an IC50 of about 0.1 μM and MICs of 4-6 μg/mL. Pseudouridimycin is a C-nucleoside analogue that's effective against both Gram-negative and Gram-positive bacteria. Pseudouridimycin inhibits bacterial growth in vitro and shows activity in a mouse model of purulent streptococcal peritonitis .
|
-
- HY-12300A
-
|
CFI-400945 hydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model .
|
-
- HY-170398
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
ZG297 is an agonist for Staphylococcus aureus ClpP (SaClpP ) with an EC50 of 0.26 μM. ZG297 degrades SaFtsZ, inhibits the bacterial cell division, thereby exhibiting antistaphylococcal activity, that inhibits S. aureus 8325-4 strains and MRSA strains with MIC of 0.063-256 μg/mL. ZG297 exhibits anti-infectious efficacy in mouse models .
|
-
- HY-16726R
-
|
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-170936
-
|
|
FAK
Hippo (MST)
YAP
|
Cancer
|
|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
|
-
- HY-154313
-
|
Clospirazine
|
Ras
|
Cancer
|
|
Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
|
-
- HY-170363
-
|
|
Proteasome
Parasite
|
Infection
|
|
Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, inibits T. b. brucei, T. b. gambiense and T. b. rhodesiense with EC50s of 157 nM, 220 nM and 156 nM, respectively. Proteasome-IN-6 exhibits antitrypanosomal activity in mouse model .
|
-
- HY-117985B
-
|
DA-1229 tartrate
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
Inflammation/Immunology
|
|
Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-149105
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor. FSH receptor antagonist 1 exhibits an IC50 of 28 nM on a cell line expressing the human FSH receptor. FSH receptor antagonist 1 significantly inhibits follicle growth and ovulation in an ex vivo mouse model .
|
-
- HY-164587
-
|
|
DOCK
|
Metabolic Disease
|
|
E197 is the inhibitor for DOCK5 that destroys the podosome belt structure of osteoclasts, thereby inhibiting the bone resorption (IC50=3.44 μM in human osteoclast). E197 inhibits the Rac in DOCK5 expressing HEK293 cell with an IC50 of 36 μM. E197 prevents the bone loss in mouse ovariectomized models .
|
-
- HY-162255
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer .
|
-
- HY-114977R
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Avenanthramide A (Standard) is the analytical standard of Avenanthramide A. This product is intended for research and analytical applications. Avenanthramide A is a phytoalexin, which can be found in oats (Avena sativa L.). Avenanthramide A targets the RNA helicase DDX3, leads to mitochondrial swelling and increased ROS production, and induces apoptosis in CRC cells. Avenanthramide A exhibits antitumor efficacy in mouse model. Avenanthramide A orally active .
|
-
- HY-123033
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-149352
-
|
|
Thymidylate Synthase
|
Cancer
|
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
|
-
- HY-P991464
-
|
|
TNF Receptor
|
Cancer
|
|
IBI37G5 is a human monoclonal antibody (mAb) targeting TNFRSF18/GITR/CD357. IBI37G5 has anti-tumor activity in MC38 and B16F10 mouse tumor models. IBI37G5 can be used in the study of cancer immunity .
|
-
- HY-D2620
-
|
|
Photosensitizer
Reactive Oxygen Species
Ferroptosis
|
Cancer
|
|
CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC50 of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models .
|
-
- HY-146407
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity .
|
-
- HY-138131
-
|
|
SOD
|
Neurological Disease
|
|
SOD1-Derlin-1 inhibitor-1 (compound 56-20) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-1 inhibits SOD1 G93A-Derlin-1 complex with an IC50 value of 7.11 μM. SOD1-Derlin-1 inhibitor-1 can be used for the research of amyotrophic lateral sclerosis .
|
-
- HY-123982
-
|
|
SOD
|
Neurological Disease
|
|
SOD1-Derlin-1 inhibitor-2 (compound 56-59) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-2 attenuates the interactions between Derlin-1 and SOD1 mut. SOD1-Derlin-1 inhibitor-2 can be used for the research of amyotrophic lateral sclerosis (ALS) .
|
-
- HY-W115718
-
|
|
Dopamine β-hydroxylase
|
Neurological Disease
|
|
Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) .
|
-
- HY-173312
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 49 is an orally active antimalarial compound. Antimalarial agent 49 inhibits growth of Pf3D7 and PfK1 strains (IC50: 0.84 μM and 0.4 μM respectively). Antimalarial agent 49 has antimalarial activity and inhibits the development of P. berghei liver stages. Antimalarial agent 49 can be used in the study of Plasmodium infection .
|
-
- HY-161905
-
|
|
Parasite
|
Infection
|
|
ML471 is an oral active parasite tyrosyl-tRNA synthetase (PfTyrRS) inhibitor and can be used for study of malaria .
|
-
- HY-W613220
-
-
- HY-168782
-
|
|
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Resolvin D2 n-3 DPA is a specialized proresolving mediator (SPM). Resolvin D2 n-3 DPA (1 nM) can reduce the chemotaxis and adhesion of human neutrophils induced by TNF-α. Resolvin D2 n-3 DPA (100 ng/mouse; intravenous injection) can reduce neutrophil infiltration in the peritoneum and the levels of IL-6 and the chemokine (C-C motif) ligand 2 (CCL2) in a mouse model of inflammation induced by zinc oxide .
|
-
- HY-168998
-
|
|
Fungal
Casein Kinase
|
Infection
|
|
Yck2-IN-1 (Compound 2a) is an inhibitor of the fungal Candida albicans Yck2 kinase. It exhibits an IC50 of approximately 80 nM against Yck2 and a MIC80 of 12.5 µM against C. albicans, with good metabolic stability (66% remaining in mouse liver microsomes). In a mouse model of drug-resistant candidiasis, Yck2-IN-1 significantly reduced fungal burden in the kidneys. Yck2-IN-1 holds promise for research in the field of antifungal infection .
|
-
- HY-125172
-
|
Polyglutamine Aggregation inhibitor III
|
Huntingtin
|
Others
|
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s=25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2 transgenic mouse model of Huntington's disease.
|
-
- HY-N13866
-
|
|
Others
|
Cancer
|
|
Cucumarioside A2-2 is a triterpene glycoside with antitumor activity. Cucumarioside A2-2 can induce mouse macrophage polarization toward the M1 phenotype. Cucumarioside A2-2 pretreated macrophages can effectively and selectively target and kill multiple types of cancer cells. Cucumarioside A2-2-induced M1 macrophages can effectively target and penetrate tumor tissues and improve the survival rate of mice in an allogeneic model. Exogenous activation of Cucumarioside A2-2 provides a useful model for the subsequent development of antitumor cell immunosuppression .
|
-
- HY-161892
-
|
|
FABP
|
Metabolic Disease
Inflammation/Immunology
|
|
FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC50 of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models .
|
-
- HY-170492
-
|
|
Epoxide Hydrolase
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
sEH inhibitor-19 (Compound (R)-14i) is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 1.2 nM. sEH inhibitor-19 inhibits the expression of TNF-α and IL-6, exhibits anti-inflammatory activity in mouse acute pancreatitis or Carrageenan (HY-125474)-induced edema models .
|
-
- HY-126850
-
|
|
EGFR
|
Cancer
|
|
4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline, HY-N0565) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates .
|
-
- HY-135953
-
|
|
Apoptosis
|
Cancer
|
|
CDDO-3P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-3P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model . CDDO-3P-Im is a orally active necroptosis inhibitor that can be used for the research of ischemia/reperfusion (I/R) .
|
-
- HY-170395
-
|
|
RSV
DNA/RNA Synthesis
|
Infection
|
|
GHP-88309 is a broad-spectrum, orally active antiviral agent targeting paramyxoviruses, that targets the viral polymerase, interupts the viral RNA synthesis, and inhibits respiratory syncytial virus (RSV), measles virus (MeV), and canine distemper virus (CDV) with EC50 of 0.06-1.2 μM. GHP-88309 exhibits anti-infectious efficacy in mouse models .
|
-
- HY-123522
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo .
|
-
- HY-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-160061
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
|
-
- HY-155850
-
|
|
Pyruvate Kinase
|
Neurological Disease
|
|
CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction .
|
-
- HY-15079
-
|
GYKI-53773; LY-300164
|
iGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity . Talampanel (IVAX) has neuroprotective effects in rodent stroke models . Talampanel attenuates caspase-3 dependent apoptosis in mouse brain .
|
-
- HY-167935
-
|
|
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
|
LCC-12 formic is a dimer of metformin that targets mitochondrial copper(II), leading to a decrease in the NAD(H) pool and modulation of inflammatory responses. LCC-12 formic reduces inflammation in mouse models of bacterial and viral infections. LCC-12 formic also serves as a tool for investigating metabolic diseases through its effects on cell plasticity and epigenetic programming.
|
-
- HY-103370
-
|
BA 7602-06
|
Chloride Channel
|
Inflammation/Immunology
|
|
Talniflumate (BA 7602-06) is the proagent of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase . Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome .
|
-
- HY-146086
-
|
|
Keap1-Nrf2
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
|
|
Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model .
|
-
- HY-P3291
-
|
ZP7570
|
GCGR
|
Metabolic Disease
|
|
Dapiglutide (ZP7570) is a long-acting glucagon-like peptide-1 receptor 1R (GLP-1R)/Glucagon-like peptide-2 receptor (GLP-2R) dual agonist. Dapiglutide alleviates intestinal dysfunction in a mouse short bowel model and has anti-obesity effects .
|
-
- HY-161663
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
|
-
- HY-W641445
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
ELP-004 is a TRPC channel inhibitor and inhibtis TRPC channel-mediated Ca 2+ entry. ELP-004 is an osteoclast inhibitor and inhibits osteoclast differentiation. ELP-004 inhibits basal Ca 2+ and related NFATc1 translocation in inflammatory osteoclastogenesis. ELP-004 reduces bone erosion in a mouse model of rheumatoid arthritis .
|
-
- HY-114180
-
|
RU320521
|
Cyclic GMP-AMP Synthase
|
Metabolic Disease
|
|
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS) .
|
-
- HY-129752
-
|
|
Antibiotic
|
Cancer
|
|
Piperafizine B exhibits slightly cytotoxicity in moser cells, P388 cells and Vincristine (VCR) (HY-N0488)-resistant P388 cells (IC50s is 23.8, 22.6 and 23.7 μg/mL, respectively). Piperafizine B exhibits synergistic effects with Vincristine, enhances the VCR-induced cytotoxicity and ameliorates the leukemia in mouse model .
|
-
- HY-139562
-
|
|
FXR
|
Metabolic Disease
|
|
BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
|
-
- HY-12098
-
|
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-164909
-
|
|
PANK
|
Inflammation/Immunology
|
|
PZ-3022 is an orally active and allosteric PanK activator that counteracts C3-CoA inhibition. PZ-3022 increases hepatic CoASH and C2-CoA and decreases C3-CoA in the propionic acidemia mouse model. PZ-3022 can be used for research of mitochondrial defect in propionic acidemia .
|
-
- HY-125650A
-
|
PUM TFA
|
Antibiotic
DNA/RNA Synthesis
Bacterial
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Pseudouridimycin (PUM) TFA is an antibiotic that selectively inhibits bacterial RNA polymerase (RNAP), with an IC50 of about 0.1 μM and MICs of 4-6 μg/mL. Pseudouridimycin TFA is a C-nucleoside analogue that's effective against both Gram-negative and Gram-positive bacteria. Pseudouridimycin TFA inhibits bacterial growth in vitro and shows activity in a mouse model of purulent streptococcal peritonitis .
|
-
- HY-111193
-
|
3-Chloroprocainamide
|
NF-κB
Apoptosis
|
Cancer
|
|
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
|
-
- HY-19345
-
|
NSC13316
|
p38 MAPK
|
Cancer
|
|
Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways . Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model . Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell .
|
-
- HY-164284
-
|
|
Sodium Channel
|
Neurological Disease
|
|
LK-2 is an antagonist for ASIC1a with a Kd of 1.9 μM. LK-2 reduces glutamate-induced ASIC1a current-enhancement with an IC50 of 6.6 μM. LK-2 exhibits neuroprotective efficacy in mouse ischemic stroke model, with improved motor and coordination skills. LK-2 is blood-brain barrier (BBB) penetrable .
|
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
|
-
- HY-163766
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Antiproliferative agent-51 (Compound 18h) exhibits inhibitory efficacy against estrogen receptor α (ERα) mediated transcription, with an IC50 of 1.6 nM. Antiproliferative agent-51 inhibits the proliferation of cancer cell ZR-75, with an IC50 of 0.031 μM. Antiproliferative agent-51 exhibits antitumor efficacy in mouse models .
|
-
- HY-117818
-
|
Antibiotic DC 116
|
Antibiotic
|
Cancer
|
|
Sapurimycin is an antitumor antibiotic isolated from Streptomyces DO-116 and belongs to the capramycin family. Sapurimycin exhibits potent activity against Gram-positive bacteria and exhibits significant antitumor effects against leukemia P388 and sarcoma 180 in mouse models. In vitro studies have shown that Sapurimycin can induce single-strand breaks in supercoiled plasmid DNA .
|
-
- HY-19345A
-
|
NSC13316 dihydrochloride
|
p38 MAPK
|
Cancer
|
|
Vacquinol-1 (NSC13316) dihydrochloride is a MKK4-specific activator that activates MAPK pathways . Vacquinol-1 dihydrochloride specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model . Vacquinol-1 dihydrochloride also induces apoptosis in hepatocellular carcinoma (HCC)cell .
|
-
- HY-164123
-
|
|
Bacterial
|
Infection
|
|
Antibiofilm agent-9 (Compound 4) is a pyrrolomycin derivative with antibacterial activity. Antibiofilm agent-9 inhibits Bacillus anthracis with MIC of 0.031 μg/mL. Antibiofilm agent-9 exhibits antibiofilm activity with 84% biofilm inhibition (24 h, 8.0 μg/mL). Antibiofilm agent-9 exhibits a good pharmacokinetic characters in mouse model .
|
-
- HY-170874
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
|
-
- HY-N1181
-
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-N3005
-
|
|
Apoptosis
Autophagy
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
|
Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
|
-
- HY-108420
-
|
|
CDK
|
Cancer
|
|
INK4C-IN-2 (Compound 40) is the inhibitor for INK4C (also known as p18) and the activator for CDK4/6. INK4C-IN-2 increases the number and expansion capacity of mouse and human hematopoietic stem cells (HSCs) with EC50 of 5.21 nM, promotes the self-renewal and multilineage differentiation of HSCs. INK4C-IN-2 improves the expansion and long-term hematopoietic reconstruction ability of HSCs in mouse bone marrow transplantation model .
|
-
- HY-170362
-
|
|
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC50 of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models .
orally active, THP-1, C57Bl/6 mouse, orally active
|
-
- HY-117049
-
|
|
CDK
DYRK
|
Neurological Disease
|
|
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) . Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model .
|
-
- HY-162641
-
|
|
IRAK
NF-κB
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-147736
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
|
-
- HY-172454
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-36 (Compound B8) is an allosteric inhibitor of SHP2, with an IC50 value of 9.0 nM. In addition, its IC50 for p-ERK is 40 nM. SHP2-IN-36 also exhibited significant antitumor activity in the KYSE520 xenograft mouse model. SHP2-IN-36 can be used for research in the field of anti-tumor .
|
-
- HY-143905
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-136360
-
MI-3454
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
|
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .
|
-
- HY-158148
-
|
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
|
|
CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC50 of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable .
|
-
- HY-122611
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-145405
-
|
|
Liposome
|
Others
|
|
C12-200 is a type of ionizable cationic lipid and helper lipid commonly used for mRNA delivery. In the hemophilia B mouse model, mRNA encoding human erythropoietin (EPO) and coagulation factor IX (FIX) can be successfully delivered and expressed using C12-200. C12-200 is utilized in research related to hemophilia B .
|
-
- HY-W092043
-
|
|
PROTAC Linkers
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR4-IN-C34-C2-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34 (HY-107575). TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-143904
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-161620
-
|
|
IRAK
|
Inflammation/Immunology
|
|
DW18134 is an inhibitor for interleukin receptor-associated kinase 4 (IRAK 4) with an IC50 of 11.2 nM. DW18134 inhibits phosphorylation of IRAK4 and IKK, downregulates the secretion of TNF-α and IL-6. DW18134 attenuates the Lipopolysaccharides (HY-D1056)-induced peritonitis and DSS-induced colitis in mouse models, and protects the intestinal barrier function .
|
-
- HY-168930
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 25 (Compound 29) is an orally active Autotaxin inhibitor with an IC50 of 1.08 nM. ATX inhibitor 25 exhibits excellent in vitro metabolic stability, with a t1/2 of more than 170 minutes. In the bleomycin (HY-108345)-induced pulmonary fibrosis mouse model, orally administered ATX inhibitor 25 shows anti-fibrotic effects .
|
-
- HY-P10360
-
|
|
α-synuclein
|
Neurological Disease
|
|
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .
|
-
- HY-111066
-
|
|
Dopamine Receptor
|
Others
|
|
JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
|
-
- HY-119311
-
|
|
PPAR
|
Metabolic Disease
|
|
Pioglitazone ketone is an active metabolite of the PPARγ agonist Pioglitazone (HY-13956). Formation of pioglitazone ketone occurs primarly through cytochrome P450 (CYP) isoform CYP2C8-mediated metabolism of pioglitazone. Pioglitazone ketone (100 mg/kg in the diet) reduces blood glucose levels in a KKAy mouse model of type 2 diabetes.
|
-
- HY-169904
-
|
|
SOD
|
Neurological Disease
|
|
AKV-9 is the inhibitor for mutated Cu/Zn superoxide dismutase (SOD1), that inhibits SOD1-induced protein aggregation and exhibits protective efficacy against SOD1-induced cytotoxicity in PC-12 with an EC50 of 0.3 μM. AKV-9 ameliorates amyotrophic lateral sclerosis in mouse models and extends their lifespan .
|
-
- HY-123033B
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside tartrate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-121600
-
|
|
Cannabinoid Receptor
|
|
|
GAT229 is a CB1 positive allosteric modulator (PAM) that effectively reduces intraocular pressure (IOP) in high IOP mouse models and enhances CB1 receptor-mediated IOP-lowering effects. A 0.2% GAT229 solution or 10 mg/kg of GAT229 alone significantly reduces IOP. GAT229 is promising for research related to glaucoma and elevated intraocular pressure .
|
-
- HY-147735
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-123033C
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside malate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-168927
-
|
|
Apoptosis
Pyroptosis
|
Cancer
|
|
Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model .
|
-
- HY-172170
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-39 (Compound 14) is a reversible inhibitor for LSD1 with an IC50 of 0.18 μM. LSD1-IN-39 exhibits broad-spectrum anti-proliferative activity against cancer cells, inhibits the cell migration of HepG2 and inhibits the epithelial-mesenchymal transition. LSD1-IN-39 exhibits antitumor activity in mouse models .
|
-
- HY-123033D
-
|
|
Endogenous Metabolite
Sirtuin
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside (triflate), an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside (triflate) is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside (triflate) reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-122611A
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
|
-
- HY-161767
-
|
|
Molecular Glues
|
Cancer
|
|
JWJ-01-306 is a molecular glue that targets the C2H2 zinc finger transcription factor ZBTB11. JWJ-01-306 degrades ZBTB11, reduces the oxidative phosphorylation (OXPHOS) and tricarboxylic acid (TCA) cycle, and inhibits the proliferation of KAS-resistant PDAC cells. JWJ-01-306 exhibits good pharmacokinetic characteristics in mouse model .
|
-
- HY-B0217
-
|
NTZ; NSC 697855
|
Parasite
Influenza Virus
Autophagy
|
Infection
Cancer
|
|
Nitazoxanide (NTZ), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans. Nitazoxanide inhibits Giardia lamblia trophozoite proliferation in axenic culture with an IC50 of 2.4 μM . Nitazoxanide can be used for the research of parasitic gastroenteritis. Nitazoxanide shows anti-Japanese encephalitis virus (JEV) activity in a mouse model .
|
-
- HY-163768
-
|
|
β-catenin
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-172 (Compound 28) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 3.92 μM. Antitumor agent-172 exhibits high affinity to β-catenin with Kd of 82 nM. Antitumor agent-172 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
|
-
- HY-150639
-
|
|
Raf
|
Cancer
|
|
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
|
-
- HY-163673
-
|
|
Glucocorticoid Receptor
Drug-Linker Conjugates for ADC
|
Inflammation/Immunology
|
|
Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models .
|
-
- HY-170846
-
|
|
FGFR
VEGFR
Bcr-Abl
FLT3
Cytochrome P450
|
Inflammation/Immunology
|
|
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model .
|
-
- HY-144898
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
SB-216 is an BBB-penetrable tubulin polymerization inhibitor. SB-216 can inhibit the proliferation and migration, and induce apoptosis and cell cycle arrest of tumor cells. SB-216 has good in vivo metabolic stability and low toxicity, but its oral bioavailability is limited. SB-216 has antitumor activity and can be used in the research of tumors such as melanoma .
|
-
- HY-129115
-
|
|
Reactive Oxygen Species
Caspase
|
Others
|
|
S1QEL1.1 is a small molecule inhibitor that specifically inhibits the generation of superoxide and hydrogen peroxide at the IQ site during reverse electron transfer in mitochondrial respiratory chain complex I (Complex I), with an IC50 of 0.07 μM. S1QEL1.1 can significantly reduce the activation of cysteine-aspartic protease (caspase) triggered by endoplasmic reticulum stress. S1QEL1.1 helps to decrease excessive proliferation of stem cells by inhibiting the Reactive Oxygen Species signaling pathway initiated by endoplasmic reticulum stress .
|
-
- HY-146186
-
|
|
JAK
|
Cancer
|
|
JAK2 JH2 binder-1 (compound 11) is a potent and selective JAK2 JH2 binder, with a Kd of 37.1 nM. JAK2 JH2 binder-1 has the potential for various myeloproliferative neoplasms research .
|
-
- HY-163527
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-155993
-
|
|
PARP
|
Cancer
|
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
|
-
- HY-N0656
-
|
|
Bacterial
DNA/RNA Synthesis
Nuclear Factor of activated T Cells (NFAT)
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Usnic acid is a secondary metabolite of lichens with a unique dibenzofuran skeleton. Usnic acid inhibits DNA/RNA synthesis and has antibacterial activity. Usnic acid induces cell cycle arrest and apoptosis and has anticancer activity. Usnic acid inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1. Usnic acid has antioxidant and anti-inflammatory activities by inhibiting lipid peroxidation and myeloperoxidase .
|
-
- HY-161665
-
|
|
iGluR
|
Neurological Disease
|
|
BDZ-P7 inhibits AMPA receptor GluA2, GluA1/2, GluA2/3, and GluA1 subunit with IC50s of 3.03 μM, 3.14 μM, 3.19 μM, 3.2 μM. BDZ-P7 has neuroprotective effect and reinstates locomotor abilities in a mouse model of Parkinson’s disease .
|
-
- HY-155572
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator-8 (compound 10e) is a Nrf2 activator (EC50=37.9 nM). Nrf2 activator-8 exhibits remarkable antioxidant and anti-inflammatory effects in BV-2 microglial cells. Nrf2 activator-8 can significantly restore spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation .
|
-
- HY-151462
-
RP-6685
1 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-147410
-
|
ION-363
|
DNA/RNA Synthesis
Others
|
Neurological Disease
|
|
Ulefnersen (ION363) is an Antisense Oligonucleotide (ASO) directed against the 6th intron of the fused-in sarcoma (FUS) transcript to silence FUS in a non-allele-specific manner. Ulefnersen can reduce postnatal levels of FUS protein in the brain and spinal cord in disease-relevant mouse model of ALS-FUS , delaying motor neuron degeneration. Ulefnersen can be used in the research of Amyotrophic Lateral Sclerosis (ALS) .
|
-
- HY-176410
-
|
|
IRAK
|
Cancer
|
|
IRAK1/4/pan-FLT3 Kinase-IN-2 (compound 27) is a potent IRAK1/4 and FLT3 dual inhibitor with IC50s of 10, 0.7, and <0.5 nM. IRAK1/4/pan-FLT3 Kinase-IN-2 extends acute myeloid leukemia model mouse survival .
|
-
- HY-W743888
-
|
6-Allyl-6-nor-LSD
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
AL-LAD (6-Allyl-6-nor-LSD) is an activator for 5-HT2A receptor with Ki of 3.4-8.1 nM. AL-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with absolute affinitiesK0.5 of 189 nM and 12.3 nM. AL-LAD acts as psychoactive substance in mouse model .
|
-
- HY-168734
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model .
|
-
- HY-13954
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
|
-
- HY-145245
-
-
- HY-162616
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
|
-
- HY-107811A
-
|
|
Autophagy
α-synuclein
Apoptosis
Monoamine Oxidase
Mitosis
|
Neurological Disease
Cancer
|
|
Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol hydrochloride can induce cell mitosis, Autophagy and Apoptosis. Harmol hydrochloride promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol hydrochloride has anti-tumor, anti-depressant and anti-aging activities. Harmol hydrochloride improves motor impairment in a mouse Parkinson's disease model .
|
-
- HY-W757743
-
|
ACP-196-d3
|
Isotope-Labeled Compounds
|
Others
|
|
Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
|
-
- HY-N0421R
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-169265
-
|
|
Bcl-2 Family
|
Others
|
|
BRD-K20733377 is an inhibitor for Bcl-2, and exhibits selective cytotoxicity against senescent cells, that inhibits the viability of Etoposide (HY-13629)-induced IMR-90 senescent cell with an IC50 of 10.7 μM. BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21 and KI67 in aged mouse model .
|
-
- HY-159700
-
|
|
Liposome
|
Infection
|
|
AA3-DLin is an ionizable cationic lipid with a pKa value of 5.8. AA3-DLin is used to delivery mRNA combined with lipid nanoparticles (LNPs). AA3-DLin LNP COVID-19 vaccines encapsulating SARS CoV-2 spike mRNAs successfully induces strong immunogenicity in a BALB/c mouse model .
|
-
- HY-112863
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt inhibitor 3 is an orally active and potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor. RORγt inhibitor 3 shows high binding affinity and inhibitory activity of Th17 cell differentiation. RORγt inhibitor 3 also shows efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models .
|
-
- HY-P10559
-
|
|
Bacterial
|
Infection
|
|
(RXR)4XB is a cell-penetrating peptide, that binds the phosphorodiamidate morpholino oligomers (PMOs), forms peptide-conjugated PMOs (PPMOs), and improves the delivery of PMO into bacterial cells. (RXR)4XB-PMO conjugate prevents the formation of biofilms, inhibits Pseudomonas aeruginosa with MIC50 of 0.5 to 16 μM, and reduces the bacterial burden in mouse acute pneumonia models .
|
-
- HY-156633
-
|
PC14586
|
MDM-2/p53
|
Cancer
|
|
Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
|
-
- HY-138657
-
|
|
Phosphatase
|
Cancer
|
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model .
|
-
- HY-135317
-
|
CA-4948
|
IRAK
Apoptosis
FLT3
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib exhibits antitumor activity in mouse model
|
-
- HY-155971
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model .
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-14342
-
MK-5046
2 Publications Verification
|
Bombesin Receptor
|
Metabolic Disease
|
|
MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
- HY-107811
-
Harmol
1 Publications Verification
|
Autophagy
α-synuclein
Apoptosis
Monoamine Oxidase
Mitosis
|
Neurological Disease
Cancer
|
|
Harmol is an orally active β-carboline alkaloid. Harmol is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model .
|
-
- HY-147410A
-
|
ION-363 sodium
|
Others
DNA/RNA Synthesis
|
Neurological Disease
|
|
Ulefnersen sodium (ION363) is an Antisense Oligonucleotide (ASO) directed against the 6th intron of the fused-in sarcoma (FUS) transcript to silence FUS in a non-allele-specific manner. Ulefnersen sodium can reduce postnatal levels of FUS protein in the brain and spinal cord in disease-relevant mouse model of ALS-FUS , delaying motor neuron degeneration. Ulefnersen sodium can be used in the research of Amyotrophic Lateral Sclerosis (ALS) .
|
-
- HY-148948
-
|
|
NAMPT
|
Neurological Disease
|
|
NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity .
|
-
- HY-151933
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
|
-
- HY-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-153255
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-13 (Compound 36) is an orally active BACE1 inhibitor with an IC50 value of 2.9 nM. BACE1-IN-13 is highly potent in hAβ42 cell (IC50 = 1.3 nM). BACE1-IN-13 has cardiovascularly safty and elicits sustained Aβ42 reduction in mouse and dog animal models .
|
-
- HY-170616
-
|
|
Fungal
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
JH-FK-08 is an inhibitor for the serine/threonine-specific phosphatase calcineurin. JH-FK-08 exhibits antifungal activity that inhibits C. neoformans with MIC80 of 0.8 µg/mL. JH-FK-08 exhibits immunosuppressive activity and inhibits the IL-2 expression with an IC50 of 42.6 nM. JH-FK-08 exhibits anti-infectious activity in mouse models .
|
-
- HY-N11499
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models .
|
-
- HY-161523
-
|
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
|
|
XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model .
|
-
- HY-103171
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50=3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model .
|
-
- HY-147301B
-
|
AP1189 methanesulfonate
|
Melanocortin Receptor
ERK
|
Inflammation/Immunology
|
|
Resomelagon methanesulfonate (AP1189 methanesulfonate) is the methanesulfonate salt form of Resomelagon (HY-147301). Resomelagon methanesulfonate is an orally active melanocortin receptor (MR) agonist. Resomelagon methanesulfonate induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon methanesulfonate exhibits anti-inflammatory activity in mouse peritonitis and peritonitis model. Resomelagon methanesulfonate can be used for obesity and chronic inflammation research .
|
-
- HY-165245
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
|
-
- HY-168485
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARα/δ agonist 3 (Compound 8) is the orally active agonist for PPAR, that activates PPARα, PPARδ and PPARγ with EC50s of 5.6, 3.4 and 1278 nM, respectively. PPARα/δ agonist 3 exhibits anticholestatic activity in mouse ANIT- or CDCA (HY-76847)-induced cholestatic liver disease models .
|
-
- HY-160186
-
|
|
Cytochrome P450
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
|
|
20-SOLA is an orally active 20-HETE antagonist. 20-SOLA greatly ameliorates changes in blood pressure and renal injury associated with a Streptozotocin (STZ) (HY-13753)-diabetic mouse model. 20-SOLA facilitates the restoration of coronary collateral growth (CCG) after ischemic injury. 20-SOLA can be studied for research in cardiovascular diseases and diabetes .
|
-
- HY-157442
-
-
- HY-137655
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
BMS-P5 is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model .
|
-
- HY-118338
-
|
|
Parasite
|
Infection
|
|
WRR-483 is an analog of K11777, an inhibitor of cruzain, used to inhibit the proliferation of Trypanosoma cruzi in cell culture. WRR-483 can eradicate parasitic infection in an acute Chagas disease mouse model. WRR-483 is an irreversible cysteine protease inhibitor that shows pH-dependent high affinity and potent trypanocidal activity against cruzain and T. cruzi infection, and is expected to inhibit Chagas disease.
|
-
- HY-125279
-
|
|
Parasite
|
Inflammation/Immunology
|
|
OAT-2068 is a selective, high activity and orally active inhibitor of mouse chitotriosidase (mCHIT1) (IC50=29 nM) and displays 143-fold selectivity over m AMCase (IC50=4170 nM). OAT-2068 displays a good pharmacokinetic profile and is an ideal tool to study the role of CHIT1 in biological systems, including animal models of human diseases .
|
-
- HY-168012
-
|
|
Ras
Phosphatase
|
Cancer
|
|
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
|
-
- HY-161723
-
|
|
Dopamine Transporter
CDK
|
Neurological Disease
|
|
LH2-051 is a lysosome-enhancing lead compound, which promotes the lysosome biogenesis and the Aβ aggregate clearance through dopamine transporter-cyclin-dependent kinase 9-transcription factor EB (DAT-CDK9-TFEB) pathway. LH2-051 exhibits good pharmacokinetic characteristics in mouse models. LH2-051 is potential for ameliorating Aleheimer’s Disease .
|
-
- HY-113365
-
|
4-Cholesten-3-one
|
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
Cholestenone (4-cholesten-3-one) is an orally available antimicrobial agent that is metabolized primarily in the liver as an intermediate oxidation product of cholesterol. Cholestenone inhibits human dermal fibroblast migration and fights Helicobacter pylori infection in vitro and in mouse models by inhibiting cholesterol-α-D-glucopyranoside (CGL). Cholestenone also alleviates metabolic disorders caused by obesity in db/db mice .
|
-
- HY-155532
-
|
|
Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-170993
-
|
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
Antimicrobial agent-39 (Compound 8i) is an antibiotic that targets 50S ribosomal subunit and inhibits bacterial protein synthesis. Antimicrobial agent-39 disrupts bacterial cell membranes, leads to leakage of cell contents, thereby exhibiting board-spectrum actibacterial activity. Antimicrobial agent-39 targets organic cation transporters (OCTs), accumulates in infected kidneys, thereby ameliorating pyelonephritis in mouse models .
|
-
- HY-47888
-
|
|
Integrin
|
Inflammation/Immunology
|
|
PLN-1474 (compound 1) is an orally active and selective ανβ1 integrin inhibitor with an IC50 value of <50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or researching a fibrotic or cirrhotic disease or disorder.
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-170309
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
NZ-804 is an orally active inhibitor for SARS-CoV-2 main protease Mpro with an IC50 of 8.9 nM. NZ-804 inhibits the SARS-CoV-2 replication in HeLa-hACE2 cell with an EC50 of 14 nM. NZ-804 exhibits board-spectrum antiviral activity aganst multiple CoVs. NZ-804 diminishes virus replication in mouse and hamster model .
|
-
- HY-162004
-
|
|
NF-κB
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model .
|
-
- HY-161779
-
|
|
Molecular Glues
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models .
|
-
- HY-13440
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AMG 511
2 Publications Verification
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PI3K
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Cancer
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AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
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- HY-157088
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Caspase
Apoptosis
Cyclophilin
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Others
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C105SR is a cyclophilin D (CypD) inhibitor targeting to peptidyl-prolylcis-trans isomerase (PPIase). C105SR inhibits mitochondrial permeability transition opening (mPTP) with an IC 50 of 5 nM. C105SR inhibits hypoxia and reoxygenation inudced hepatocyte apoptosis and increases the level of calcium retention capacity (CRC). C105SR exhibits hepaprotective effect in ischaemia-reperfusion injury (IRI) mouse model .
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- HY-168328
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NF-κB
Interleukin Related
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Inflammation/Immunology
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FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
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- HY-169937
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Epigenetic Reader Domain
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Cancer
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(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
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- HY-P10826
-
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1 inhibitory peptide C8 is inhibits PD-1/PD-L1 interaction, promotes the activation of CD8+ and CD4+ T cells, and increases the IFN-γ secretion. PD-1/PD-L1 inhibitory peptide C8 exhibits antitumor efficacy in mouse model .
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- HY-128423AS
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Acetylisovaleryltylosin-d9
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Isotope-Labeled Compounds
Apoptosis
Antibiotic
NF-κB
Bacterial
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Others
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Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9) is the deuterium labeled Tylvalosin (HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
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- HY-110077
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API-1
1 Publications Verification
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Akt
Apoptosis
Caspase
PARP
|
Cancer
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API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model .
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- HY-171590
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Salt-inducible Kinase (SIK)
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Inflammation/Immunology
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SIK2-IN-3 is an orally active SIK1/2 selective inhibitor (IC50: 0.128/0.084 μM). SIK2-IN-3 inhibits CRTC3 phosphorylation and myeloid cell pro-inflammatory cytokine production. SIK2-IN-3 ameliorates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model .
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- HY-149426
-
|
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Sirtuin
|
Inflammation/Immunology
|
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SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .
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- HY-146462
-
|
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Apoptosis
ROS Kinase
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Cancer
|
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
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- HY-164546
-
|
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STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
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- HY-19443
-
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Histamine Receptor
Lipoxygenase
|
Inflammation/Immunology
|
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UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guinea pigs. UCB-35440 can be used for research on asthma and skin inflammation .
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- HY-116447
-
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Mitochondrial Metabolism
Apoptosis
|
Cancer
|
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Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
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- HY-131328
-
|
LOXO-305
|
Btk
|
Cancer
|
|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
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- HY-162280
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PROTACs
RANKL/RANK
Nuclear Factor of activated T Cells (NFAT)
Btk
|
Cancer
|
|
PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .
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-
- HY-18329
-
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MDM-2/p53
STAT
Apoptosis
|
Cancer
|
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TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models .
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-
- HY-B0596
-
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TA-0910
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Thyroid Hormone Receptor
Apoptosis
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Neurological Disease
Endocrinology
|
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Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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- HY-155238
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GABA Receptor
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Neurological Disease
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E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
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- HY-121856
-
|
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Others
|
Inflammation/Immunology
|
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Flumizole, a derivative of substituted 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles, was synthesized and evaluated for its immunoregulatory and anti-inflammatory properties in animal models such as rat adjuvant-induced arthritis and mouse oxazolone-induced contact sensitivity assays. This compound class combines structural elements from flumizole and levamisole, aiming to enhance therapeutic efficacy. Symmetrically substituted 5,6-diaryl compounds with specific alkyl heteroatom or halogen substitutions showed optimal potency in the arthritis model. However, variations in activity were less consistent in the contact sensitivity assay. Flumizole and related compounds demonstrate potential as dual-action agents, targeting inflammation and immune modulation, offering promise for therapeutic development in immune-related disorders .
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-
- HY-168207
-
|
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Toll-like Receptor (TLR)
NF-κB
|
Inflammation/Immunology
|
|
TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury .
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-
- HY-162680
-
|
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Influenza Virus
|
Infection
|
|
OSC-GCDI(P) is a broad-spectrum orally active anti-influenza virus agent that exhibits significant inhibitory effects against both wild-type and Oseltamivir (HY-13317) resistant (H275Y) influenza virus strains in mouse infection models. OSC-GCDI(P) is capable of preventing not only wild-type influenza viruses but also OS-resistant variants with NA(H275Y) .
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- HY-149092
-
|
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TAM Receptor
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Cancer
|
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Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
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-
- HY-123429
-
|
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Antibiotic
|
Infection
|
|
CK0683A is a novel biaminourea antibiotic with antiplaque effects and demonstrated efficacy in experimental mouse dental disease models. A 12-week study in beagles compared its efficacy in terms of plaque and gingivitis reduction, staining potential, and safety. Dogs were selected as the study subjects because the onset and progression of canine periodontal disease is similar to that of humans. As a positive control for plaque and gingivitis reduction and staining, chlorhexidine acetate was selected because it is effective in both humans and dogs.
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-
- HY-16622B
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
GSK 1842799 hydrochloride is a selective S1P1 receptor agonist with potent agonist activity and exceptional selectivity over S1P3. GSK 1842799 hydrochloride demonstrates good oral bioavailability and rapid conversion to its active phosphorylated form. GSK 1842799 hydrochloride significantly reduces blood lymphocyte counts in vivo following oral administration. GSK 1842799 hydrochloride has shown efficacy comparable to FTY720 in the mouse EAE model of multiple sclerosis.
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- HY-P10913
-
|
|
Bacterial
|
Infection
|
|
HYNIC-UBI29-41 is composed of a bifunctional chelator HYNIC and an antimicrobial peptide UBI 29-41. HYNIC-UBI29-41 retains the antibacterial properties of UBI 29-41, and exhibits good affinity to Gram-positive and Gram-negative bacteria. HYNIC-UBI29-41 can be used as an imaging agent for bacterial infection detection in mouse models, when labeled with the radioactive element technetium (99mTc) .
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-
- HY-153598
-
|
|
PROTACs
RIP kinase
|
Cancer
|
|
LD4172 is a PROTAC degrader for RIP kinase (RIPK1) with DC50 in nanomolare levels. LD4172 induces apoptosis in cell B16F10 with combination of TNF-α. LD4172 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170613); Black: linker (HY-W012241); Blue: ligand for E3 ligase VHL (HY-112078))
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- HY-11046A
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
KRP-109 is a neutrophil elastase (NE) inhibitor with activity in reducing lung inflammation. KRP-109 improves survival in mouse models and reduces the number of neutrophils and inflammation in the alveolar walls. KRP-109 significantly reduced cell and neutrophil counts in bronchoalveolar lavage fluid, as well as cytokine levels such as interleukin 1β and macrophage inflammatory protein 2. KRP-109 can be used in the research of severe pneumonia .
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-
- HY-15344
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
Metabolic Disease
|
|
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
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-
- HY-105395
-
|
|
Influenza Virus
|
Infection
|
|
BCX-1898, a cyclopentane derivative, is an orally active and selective influenza virus neuraminidase inhibitor. BCX-1898 has antiviral activity with EC50s of <0.01-21 μM on influenza A (H1N1, H3N2, and H5N1) and influenza B viruses replication in MDCK cells. BCX-1898 shows protection against the mouse influenza model .
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-
- HY-171191
-
|
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
c-Met/HGFR
|
Cancer
|
|
REGN5093-M114 is a bispecific antibody-drug conjugate (ADC) that targets two epitopes of the MET receptor tyrosine kinase inhibits the proliferation of NSCLC cells, exhibits antitumor efficacy in mouse models. REGN5093-M114 is composed of the human monoclonal anti-MET antibody Davutamig (HY-P990073) and the tubulin-inhibiting linker-payload (HY-148528) .
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-
- HY-N14354
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Ferrocin B is an iron-containing cyclic decapeptide antibiotic found in the bacterium Pseudomonas fluorescens YK-310, exhibiting strong antibacterial activity primarily against Gram-negative bacteria, with particularly potent inhibitory effects on Pseudomonas aeruginosa. In a mouse infection model, Ferrocin B shows a half effective dose (ED50) of 0.593 mg/kg against P. aeruginosa. Ferrocin B holds potential for research in the field of anti-infective therapies .
|
-
- HY-120356
-
|
TAI-95
|
Apoptosis
NEKs
|
Cancer
|
|
T-1101 (TAI-95) is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 induces apoptosis in Huh-7. T-1101 exhibits antitumor efficacy in mouse models .
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-
- HY-118912
-
|
|
MDM-2/p53
|
Inflammation/Immunology
Cancer
|
|
BMH-9 (Compound Z54) is a modulator for nuclear receptor subfamily 2, group F, member 6 (NR2F6) (also known as nuclear orphan receptor Ear2) . BMH-9 is an activator for p53 signaling pathway through interaction with DNA. BMH-9 inhibits proliferation of human cancer cells, exhibits antitumor efficacy in NOD-SCID mouse models .
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-
- HY-172550
-
|
|
HCN Channel
|
Neurological Disease
|
|
MS7710 is a brain-penetrant inhibitor targeting the hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. MS7710 reduces the Ih current and decreases the activity of ventral tegmental area (VTA) dopamine neurons by inhibiting HCN channels. MS7710 can effectively improve social interaction deficits and reward-related cognitive flexibility in the chronic social defeat stress (CSDS) mouse model. MS7710 is promising for research of depression .
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-
- HY-P10439
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
CVRARTR is a programmed cell death ligand-1 (PD-L1) antagonist with a KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and T cell proliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model. CVRARTR can be used in melanoma research .
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-
- HY-A0143S
-
|
DGLA-d6; all-cis-8,11,14-Eicosatrienoic acid-d6
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
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-
- HY-162830
-
|
|
Lipoxygenase
Monoamine Oxidase
|
Neurological Disease
|
|
5-LOX/MAOs-IN-1 (compound 3) is a 5-LOX/MAOs inhibitor and a potent free radical scavenger with antioxidant properties. 5-LOX/MAOs-IN-1 also showed neuroprotective activity in oxidative stress-damaged cell models and can activate the neurogenesis microenvironment of adult mouse neural stem cells. 5-LOX/MAOs-IN-1 can be used for the study of neurodegenerative diseases .
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-
- HY-110243
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
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-
- HY-111751
-
|
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iGluR
|
Neurological Disease
|
|
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models .
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-
- HY-19620A
-
|
LMI070 hydrochloride; NVS-SM1 hydrochloride
|
DNA/RNA Synthesis
Potassium Channel
|
Cancer
|
|
Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
|
-
- HY-19620
-
|
LMI070; NVS-SM1
|
DNA/RNA Synthesis
Potassium Channel
|
Cancer
|
|
Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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-
- HY-167715
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Traxanox is an orally available diuretic that enhances phagocytosis of yeast granules by mouse peritoneal macrophages and rat peritoneal polymorphonuclear leukocytes in vitro.
Traxanox inhibits IgE-mediated histamine release and cyclic AMP phosphodiesterase
activity.Traxanox exhibits anti-inflammatory activity, as it inhibits the anaphylactoid reaction and reduces pleural fluid accumulation in experimental models of inflammation. Traxanox also demonstrates a synergistic effect when combined with hydrocortisone or indomethacin in suppressing adjuvant arthritis in rats.
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-
- HY-172874
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
TDO-IN-2 is an orally active TDO inhibitor (IC50: 1.25 μM). TDO-IN-2 has antitumor activity in the Hepa1-6 hepatocellular carcinoma allograft mouse model. TDO-IN-2 has synergistic effects with the PD-1/PD-L1 inhibitor BMS-202 (HY-19745) and can be used to study tumor immune tolerance .
|
-
- HY-101855
-
|
Anle138b
|
Amyloid-β
|
Neurological Disease
|
|
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
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-
- HY-112828
-
|
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DAGL
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
LEI105 is a potent, highly selective and reversible dual diacylglycerol lipase (DAGL)-α/DAGL-β inhibitor. LEI105 reduces 2-arachidonoylglycerol levels in Neuro2A cells. LEI105 also reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model. LEI105 is promising for research of diseases, such as obesity, related metabolic disorders and neuroinflammation .
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-
- HY-173474
-
|
|
Estrogen Receptor/ERR
Androgen Receptor
|
Cancer
|
|
ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
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-
- HY-161936
-
|
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Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Z21115 is an orally active inhibitor for phosphodiesterase 4 (PDE4), that inhibits PDE4D7 with IC50 of 10.5 nM. Z21115 inhibits Lipopolysaccharide (HY-D1056)-induced expression of IL-6, TNF-α and iNOS. Z21115 exhibits anti-inflammatory activity in DSS (HY-116282)-induced mouse colitis models without significant toxicity (1 g/kg) .
|
-
- HY-15131
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
PNRI-299 is a selective AP-1 transcription inhibitor with an IC50 of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model .
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-
- HY-161383
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
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-
- HY-144126
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
|
-
- HY-144643
-
|
|
Fungal
HDAC
Cytochrome P450
|
Inflammation/Immunology
|
|
CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis .
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-
- HY-150109
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia .
|
-
- HY-N0747
-
-
- HY-162578
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes .
|
-
- HY-W127408
-
|
|
Biochemical Assay Reagents
Endogenous Metabolite
|
Others
|
|
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
|
-
- HY-17600
-
|
ACP-196
|
Btk
|
Cancer
|
|
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-123479
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Antibiotic
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Infection
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CK0492B is a novel biaminourea antibiotic that has antiplaque properties in vitro and has shown efficacy in an experimental mouse dental disease model. A 12-week study in beagles compared its efficacy in reducing plaque and gingivitis, staining potential, and safety. Dogs were selected as the study subjects because the onset and progression of canine periodontal disease are similar to humans. Chlorhexidine acetate was selected as a positive control for plaque and gingivitis reduction and staining because it is effective in both humans and dogs.
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- HY-156103
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Huntingtin
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Neurological Disease
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mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitory activity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy .
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- HY-136927
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STING
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Inflammation/Immunology
Cancer
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MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
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- HY-147008
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Epigenetic Reader Domain
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Cancer
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XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC) .
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- HY-169078
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Histone Methyltransferase
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Cancer
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ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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- HY-143286
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PROTACs
FLT3
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Cancer
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PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
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- HY-103370R
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BA 7602-06 (Standard)
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Chloride Channel
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Inflammation/Immunology
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Talniflumate (Standard) is the analytical standard of Talniflumate. This product is intended for research and analytical applications. Talniflumate (BA 7602-06) is the proagent of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase . Talniflumate is an orally active Ca2+-activated Cl- channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome .
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- HY-107592
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IKK
STAT
Apoptosis
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Inflammation/Immunology
Cancer
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ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
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- HY-139602
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Flavivirus
Dengue Virus
Virus Protease
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Infection
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(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
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- HY-B1864AR
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Ksg hydrochloride (Standard)
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Antibiotic
Bacterial
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Infection
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Kasugamycin (Ksg) hydrochloride (Standard) is the analytical standard of Kasugamycin hydrochloride (HY-B1864A). This product is intended for research and analytical applications. Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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- HY-162011
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EBI2/GPR183
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Inflammation/Immunology
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GPR183 antagonist-2 (compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduces paw and joint swelling and gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases .
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- HY-B0217R
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Parasite
Influenza Virus
Autophagy
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Infection
Cancer
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Nitazoxanide (Standard) is the analytical standard of Nitazoxanide. This product is intended for research and analytical applications. Nitazoxanide (NTZ), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans. Nitazoxanide inhibits Giardia lamblia trophozoite proliferation in axenic culture with an IC50 of 2.4 μM . Nitazoxanide can be used for the research of parasitic gastroenteritis. Nitazoxanide shows anti-Japanese encephalitis virus (JEV) activity in a mouse model .
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- HY-117133
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SF0166
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Integrin
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Metabolic Disease
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Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
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- HY-115893A
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CDK
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Cancer
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P18IN005 hydrochloride is a novel inhibitor of p18, exhibiting potent activity in negatively regulating haematopoietic stem cell (HSC) self-renewal. P18IN005 hydrochloride has been shown to be more effective than p27 in inhibiting HSC self-renewal in mouse models. P18IN005 hydrochloride promotes the expansion of functional HSCs in short-term cultures. P18IN005 hydrochloride serves as a valuable tool for dissecting the signaling pathways involved in stem cell self-renewal.
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- HY-15186
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GDC-0068; RG7440
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Organoid
Akt
Apoptosis
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Cancer
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Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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- HY-14162
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FLAP
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Inflammation/Immunology
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AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB4 and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma .
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- HY-124954
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Cannabinoid Receptor
TNF Receptor
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Neurological Disease
Inflammation/Immunology
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MN-25 (compound 4a) is an orally active indolpyridone that serves as a novel cannabinoid ligand. MN-25 has Ki of 245 nM and 11 nM for CB1 and CB2. MN-25 has CB2 agonist activity and inhibits TNF-R release in human peripheral blood mononuclear cells in vitro with an IC50 of 33 μM. MN-25 shows efficacy in a mouse acute inflammation model at oral doses up to 50 mg/kg >[1].
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- HY-164595
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Hippo (MST)
Apoptosis
AMPK
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Metabolic Disease
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IHMT-MST1-39 is an orally active inhibitor for MST kinase, with IC50 of 42 nM and 109 nM, for MST1 and MST2. IHMT-MST1-39 activates the AMPK signaling pathway in liver cells, reduces apoptosis of pancreatic β-cells. IHMT-MST1-39 ameliorates diabetes in Streptozotocin (HY-13753)-induced type 1 diabetes (T1D) mouse models .
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- HY-161629
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Toll-like Receptor (TLR)
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Cancer
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TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
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- HY-18676B
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OSU-T315 analog
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Integrin
Autophagy
Apoptosis
Caspase
PDHK
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Cancer
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ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models .
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- HY-147136
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YAP
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Cancer
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MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model .
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- HY-100009
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Flufenamic acid butyl ester; Butyl flufenamate
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COX
Prostaglandin Receptor
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Inflammation/Immunology
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Ufenamate (Flufenamic acid butyl ester) is an anthranilic acid-based anti-inflammatory drug that can be used in the study of skin diseases such as acute and chronic eczema, contact dermatitis, diaper dermatitis, miliary rashes and atopic dermatitis. Ufenamate has a certain photoprotective effect, reduces the degree of skin erythema and swelling in the photoaging model, downregulates the expression level of COX-2 and can promote the healing of mouse skull defects by secreting BMP2 .
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- HY-155313
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Drug-Linker Conjugates for ADC
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Cancer
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β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
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![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.eu/product_pic/hy-155313.gif)
- HY-133012
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TRP Channel
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Neurological Disease
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GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
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- HY-123033AR
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Sirtuin
Endogenous Metabolite
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Neurological Disease
Metabolic Disease
Cancer
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Nicotinamide riboside (chloride) (Standard) is the analytical standard of Nicotinamide riboside (chloride). This product is intended for research and analytical applications. Nicotinamide riboside Chloride, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
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- HY-173433
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Epigenetic Reader Domain
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Cancer
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JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)) .
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- HY-170594
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Atg7
Autophagy
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Cancer
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Antitumor agent-192 (Compound 2f) is a β-carboline antitumor agent. Antitumor agent-192 induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. Antitumor agent-192 has an IC50 of less than 5 μM for human tumor cell lines and significantly inhibits tumor development and reduces tumor weight in a mouse colorectal cancer model transplanted with allografts [1].
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- HY-158062
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PROTACs
DNA/RNA Synthesis
Apoptosis
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Cancer
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LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research . (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
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- HY-P1416
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Wnt
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Cancer
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Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
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- HY-101447
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EPH 116
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Src
Apoptosis
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Cancer
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SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
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- HY-P10872
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SARS-CoV
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Infection
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P315V3 is an pan inhibitor for coronavirus, that inhibits SARS-CoV-2 prototypePT, Delta, BA.1 and BA.4 strain with IC50s of 10.9, 8.9, 8.6, and 2.7 nM. P315V3 exhibits cytotoxicity in Vero cell with CC50 of 4.3 μM. P315V3 exhibits anti-infectious efficacy in mouse models .
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- HY-157317
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Apoptosis
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Cancer
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Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
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- HY-168861
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Beta-lactamase
Bacterial
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Infection
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NDM-1 inhibitor-8 (Compound 18b) is the covalent inhibitor for new delhi metallo-β-lactamase-1 (NDM-1) with an IC50 of 7.03 μM. NDM-1 inhibitor-8 inhibits the drug resistant strains, exhibits synergistic antibacterial effect with the use of Meropenem (HY-13678). NDM-1 inhibitor-8 exhibits anti-infectious activity in mouse models .
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- HY-15186C
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GDC-0068 tosylate; RG7440 tosylate
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Organoid
Akt
Apoptosis
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Cancer
|
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Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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-
- HY-145253
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PROTAC Linkers
Toll-like Receptor (TLR)
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Inflammation/Immunology
|
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Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
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- HY-Y0546
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Endogenous Metabolite
Photosensitizer
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Cancer
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Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
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- HY-170382
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
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- HY-129510
-
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EGFR
Mitosis
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Cancer
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4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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-
- HY-13496
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c-Fms
|
Inflammation/Immunology
Cancer
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JNJ-28312141 is an inhibitor for colony-stimulating factor-1 receptor (CSF-1R or FMS), with an IC50 of 0.69 nM. JNJ-28312141 inhibits proliferation of BDBM, MV-4-11, M-o7e, TF-1 with an IC50s of 2.6, 21, 41 and 150 nM, respectively. JNJ-28312141 exhibits anti-inflammatory activity in mouse arthritis model .
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- HY-P991455
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TNF Receptor
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Cancer
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PTX-35 is a human IgG monoclonal antibody (mAb) targeting TNFRSF25. PTX-35 reduces the suppressive activity of regulatory T cells and enhances CD4+ T cell effector responses in a mouse melanoma model. PTX-35 can be used in Islet cell transplant rejection and Solid tumours research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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- HY-169120
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Telomerase
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Cancer
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FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
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- HY-18956A
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(E/Z)-Sephin1 hydrochloride; (E/Z)-IFB-088 hydrochloride
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Phosphatase
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Neurological Disease
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(E/Z)-Icerguastat hydrochloride ((E/Z)-Sephin1 hydrochloride) is a selective inhibitor with activity that prolongs the phosphorylation effects of eIF2α. (E/Z)-Icerguastat hydrochloride protects cells from defects in proteostasis. (E/Z)-Icerguastat hydrochloride was shown to significantly extend the survival of infected prion mice in a mouse model. (E/Z)-Icerguastat hydrochloride effectively reduces PrPSc expression and prion sequence activity in various neuronal cell lines persistently infected with different prion strains .
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- HY-13442C
-
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B1939 (mesylate) (purity>99%, single impurity ≤ 0.15%); E7389 (mesylate) (purity>99%, single impurity ≤ 0.15%); ER-086526 (mesylate) (purity>99%, single impurity ≤ 0.15%)
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Microtubule/Tubulin
Apoptosis
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Cancer
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Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) is an inhibitor for microtubule. Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) exhibits antitumor efficacy in mouse model .
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- HY-173016
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Opioid Receptor
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Neurological Disease
|
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HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .
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- HY-P991481
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CCR
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Cancer
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S-531011 is a human IgG1 monoclonal antibody (mAb) targeting CCR8. S-531011 reduces tumor-infiltrating CCR8+ Tregs and has anti-tumor activity in CT26.WT and EMT6 tumor-bearing mouse tumor models. S-531011 can be used in the study of cancer immunity. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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- HY-161539
-
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Opioid Receptor
|
Neurological Disease
|
|
KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
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-
- HY-P99623
-
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MGD006; S80880
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CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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-
- HY-112584
-
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6-Methoxynicotinamide
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Amine N-methyltransferase
|
Metabolic Disease
|
|
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
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-
- HY-160998
-
|
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CCR
|
Inflammation/Immunology
|
|
YM-344031 is an orally active antagonist for CCR3. YM-344031 inhibits binding of Eotaxin-1 and RANTES to CCR3, with IC50 of 3.0 and 16.3 nM. YM-344031 inhibits ligand-induced rise in intracellular Ca [2+] and the ligand-induced chemotaxis. YM-344031 inhibits eotaxin-1-induced changes in eosinophil morphology in macaques blood, and prevents allergic skin reactions in a mouse allergy model .
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- HY-139061
-
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LPL Receptor
ROCK
|
Cancer
|
|
Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
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-
- HY-169919
-
|
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Histone Demethylase
Fungal
|
Infection
|
|
HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model .
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- HY-N14035
-
|
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ATP Citrate Lyase
|
Cardiovascular Disease
Metabolic Disease
|
|
Garcinia cambogia extract contains several active compounds, including hydroxycitric acid (HCA) (an ECC inhibitor), xanthones, benzophenones, hydroxycitric acid (an ATP-citrate lyase inhibitor). Garcinia cambogia extract lowers the body weight gain, visceral fat accumulation, blood and hepatic lipid concentrations, and plasma insulin and leptin levels in a high-fat diet (HFD)-induced obesity mouse model. Garcinia cambogia extract is promising for research of fatty liver, dyslipidemia, hyperinsulinemia and hyperleptinemia rendered by HFD .
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- HY-137655A
-
|
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Protein Arginine Deiminase
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Cancer
|
|
BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model .
|
-
- HY-171793
-
|
|
PPAR
|
Metabolic Disease
|
|
DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes .
|
-
- HY-134914
-
|
|
Antibiotic
Parasite
|
Infection
|
|
Fosmidomycin is an orally active antibiotic, which exhibits antimalarial activity through inhibition of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DOXP reductoisomerase). Fosmidomycin inhibits P. falciparum strains 3D7, HB3, Dd2 and A2, with IC50s of 150, 71, 170 and 150 ng/mL, respectively. Fosmidomycin exhibits synergistic effect with Clindamycin (HY-B1455), and ameliorates malaria in mouse model .
|
-
- HY-145254
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
|
-
- HY-163538
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
|
-
- HY-160939
-
|
|
MAP3K
|
Neurological Disease
Inflammation/Immunology
|
|
ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model .
|
-
- HY-117985S
-
|
DA-1229-d9
|
Isotope-Labeled Compounds
Autophagy
Dipeptidyl Peptidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Evogliptin-d9 (DA-1229-d9) is deuterium labeled Evogliptin. Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-171317
-
|
|
Bacterial
|
Infection
|
|
SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide (HY-B0276), enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models. SMARt751 can cross blood brain barrier .
|
-
- HY-167706
-
|
|
GPR35
|
Inflammation/Immunology
|
|
Diethyl-Lodoxamide is a highly potent GPR35 agonist with potential to inhibit inflammatory bowel disease. Diethyl-Lodoxamide activates GPR35 in humans, mice and rats, showing similar EC50 values. Diethyl-Lodoxamide can alleviate the clinical symptoms of DSS-induced inflammatory bowel disease in mouse models, and the effect is better than the traditional drug 5-ASA. The pharmaceutical properties of Diethyl-Lodoxamide have been optimized to better meet the requirements of drug design .
|
-
- HY-169059
-
|
|
Ferroptosis
|
Inflammation/Immunology
|
|
Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
|
-
- HY-N0841
-
|
Dihydrobrusatol; NSC310616
|
Parasite
NF-κB
p38 MAPK
Phosphatase
Apoptosis
|
Infection
Cancer
|
|
Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
|
-
- HY-173062
-
|
|
Epigenetic Reader Domain
c-Myc
|
Others
|
|
BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models .
|
-
- HY-B0596A
-
|
TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-126287
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
|
-
- HY-N3980R
-
|
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-P99056
-
|
PF 05082566
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Utomilumab (PF 05082566) is a fully human IgG2 agonist monoclonal antibody that selectively binds to 4-1BB/CD137. Utomilumab can be used in the research of tumors such as follicular and other CD20 + non-Hodgkin lymphomas .
|
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-155780
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-16911
-
|
API-1252; Debio 1452
|
Bacterial
Antibiotic
|
Infection
|
|
AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ⩽0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
|
-
- HY-170497
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
|
-
- HY-145255
-
|
|
PROTAC Linkers
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
|
-
- HY-P991233
-
|
|
EGFR
|
Cancer
|
|
BAT1006 is a monoclonal antibody targeting HER2 extracellular domain II with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) for the study of HER2-positive locally advanced/metastatic solid tumors. BAT1006 has an approximately 5-fold enhanced ADCC effect compared to pertuzumab (HY-P9912) and exhibits potent anti-tumor activity in the HER2-positive Calu-3 xenograft mouse model .
|
-
- HY-162596
-
|
BA-1049
|
ROCK
|
Neurological Disease
|
|
NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice .
|
-
- HY-169002
-
|
|
Phosphatase
|
Cancer
|
|
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
|
-
- HY-149677
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
|
-
- HY-161954
-
|
|
HDAC
|
Cancer
|
|
HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC50: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer .
|
-
- HY-P1416A
-
|
|
Wnt
|
Cancer
|
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-161515
-
|
|
NAMPT
Epigenetic Reader Domain
|
Cancer
|
|
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
|
-
- HY-138671
-
|
|
Bacterial
|
Infection
|
|
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
|
-
- HY-170027
-
|
|
HIF/HIF Prolyl-Hydroxylase
AMPK
|
Cancer
|
|
LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-172881
-
|
|
Pyruvate Kinase
|
Cancer
|
|
PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research .
|
-
- HY-B0380B
-
|
GIC-1001
|
Biochemical Assay Reagents
|
Others
|
|
Trimebutine 3-TCBS (GIC-1001) is an innovative formulation designed to release hydrogen sulfide (H2S) in vivo. This compound combines trimebutine with an H2S-releasing antagonist (phenyl 3-thiocarbamate) and exhibits enhanced anti-nociceptive effects in a mouse colonic distension model, superior to conventional trimebutine. GIC-1001 can reduce visceral pain and discomfort associated with lumen distension in a dose-dependent manner, showing potential superiority .
|
-
- HY-P990025
-
|
ARGX-117
|
Complement System
|
Inflammation/Immunology
|
|
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .
|
-
- HY-122611R
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-135317F
-
|
CA-4948 phosphate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib phosphate exhibits antitumor activity in mouse model .
|
-
- HY-173005
-
|
|
PI3K
Akt
GSK-3
Apoptosis
|
Cardiovascular Disease
|
|
JZ19 reduces the LDH and ROS levels, and exhibits antioxidant activity against oxygen-glucose deprivation (OGD)-induced cardiomyocyte injury. JZ19 reverses Isoproterenol (HY-B0468)-induced cardiomyocyte hypertrophy and apoptosis through PI3K-AKT-GSK3β signaling pathway. JZ19 alleviates Isoproterenol (HY-B0468)-induced heart failure in mouse models .
|
-
- HY-168952
-
|
|
STING
IFNAR
Interleukin Related
|
Inflammation/Immunology
|
|
GHN105 is an orally active inhibitor for STING that inhibits STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. GHN105 reduces the IFN-β, IL-6 and CXCL10 levels in serum, and alleviates colitis in DSS (HY-116282)-induced acute colitis mouse model. GHN105 exhibits good pharmacokinetic parameters in mice with an oral bioavailability of 43% and a half-life of 1.1 hours .
|
-
- HY-173276
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor. After being orally administered at a dose of 50 mg/kg in a mouse model, it can reduce the level of plasma neurofilament light chain (NfL). SARM1-IN-4 prevents programmed axonal degeneration by inhibiting the NAD+ hydrolase activity of SARM1, and it can be used in research related to neurodegenerative diseases and neurological disorders (such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathies, etc.).
|
-
- HY-110155
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
|
-
- HY-160962
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
SM1044 is a dihydroartemisinin (DHA) dimer. SM1044 activates caspase, induces apooptosis in RL95-2 and KLE cells. SM1044 inhibits proliferations of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, AN3CA, with IC50 < 3.6 μM . SM1044 inhbits tumor growth in RL95-2 xenograft mouse model .
|
-
- HY-12700
-
|
|
Trace Amine-associated Receptor (TAAR)
|
Neurological Disease
|
|
RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages .
|
-
- HY-160912
-
|
|
ELOVL
|
Cancer
|
|
ELOVL6-IN-5 (compound B) is an inhibitor of the elongase enzyme of long-chain fatty acid family 6 (ELOVL6). ELOVL6 is a rate-limiting enzyme for the elongation of saturated and monounsaturated long-chain fatty acids and is an effective target for inhibiting diabetes. ELOVL6-IN-5 reduces hepatic fatty acid levels in a mouse model of diet-induced obesity (DIO). However, ELOVL6 inhibition by ELOVL6-IN-5 did not improve insulin resistance .
|
-
- HY-161996
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Inflammation/Immunology
|
IDO1-IN-25 is a dual inhibitor of IDO1/TDO2, with IC50 values of 0.17 μM and 3.2 μM, respectively. IDO1-IN-25 can effectively inhibit the production of NO in RAW264.7 cells stimulated by lipopolysaccharide (LPS). IDO1-IN-25 can exert anti-inflammatory effects in a mouse ear edema acute inflammation model induced by croton oil .
|
-
- HY-14687
-
|
(rac)-BMN-673; (rac)-LT-673
|
PARP
|
Cancer
|
|
(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models .
|
-
- HY-120387
-
|
|
ROS Kinase
Anaplastic lymphoma kinase (ALK)
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
SMU-B is the orally active inhibitor for ALK (IC50<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC50=1.87 nM) and AXL (IC50=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC50s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models .
|
-
- HY-170336
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for ERα with DC50 of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model . (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))
|
-
- HY-135317E
-
|
CA-4948 maleate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model .
|
-
- HY-18187
-
|
|
Apoptosis
|
Cancer
|
|
Ki 23057 is a competitive, orally active inhibitor for tyrosine kinase, which inhibits the phosphorylation of K-samII/FGF-R2, VEGF-R1, VEGF-R2, PDGF-Rβ and c-Kit, with IC50s of 88, 69, 83, 100 and 480 nM. Ki 23057 inhibits the proliferation of sclerogastric cancer cells OCUM-2MD3 and OCUM-8, and induces apoptosis. Ki 23057 exhibits antitumor efficacy in mouse models .
|
-
- HY-163616
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
|
-
- HY-173293
-
|
|
ASK1
|
Inflammation/Immunology
|
|
ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM . In an experimental mouse model of liver injury induced by Acetaminophen (HY-66005), ASK1-IN-8 can significantly reduce the plasma alanine transaminase (ALT) level, protecting the liver . ASK1-IN-8 can be used in research related to liver diseases .
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-
- HY-117622
-
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IRAK
|
Inflammation/Immunology
Cancer
|
|
ND-2110 is a selective IRAK4 inhibitor (Ki: 7.5 nM). ND-2110 binds to the ATP pocket of IRAK4. ND-2110 targets
the subset of activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL) cell lines with MYD88 L265P mutations,. ND-2110 inhibits LPS-induced TNF production, alleviates collagen-induced arthritis, and blocks gout formation in mouse models .
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-
- HY-155195
-
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|
FLT3
|
Cancer
|
|
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
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-
- HY-N1486R
-
|
|
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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-
- HY-100546
-
|
|
Histone Demethylase
|
Infection
Metabolic Disease
Cancer
|
|
GSK-LSD1 is a LSD1 inhibitor. GSK-LSD1 reduces food intake and body weight, and improves insulin sensitivity and glycemic control in mouse models of obesity. GSK-LSD1 also ameliorates NAFLD. GSK-LSD1 inhibits SARS-CoV-2-triggered cytokine release in COVID-19 PBMCs. GSK-LSD1 also inhibits cancer growth and metastasis .
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-
- HY-143286A
-
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|
PROTACs
FLT3
|
Cancer
|
|
PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader，with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells，can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
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-
- HY-124623
-
|
|
Parasite
|
Infection
|
|
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
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-
- HY-161630
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
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-
- HY-135317C
-
|
CA-4948 tosylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model .
|
-
- HY-170774
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cardiovascular Disease
|
|
Hypoxia inducer-1 (Compound N6) is an orally active hypoxia activated nitric oxide (NO) donor compound. Hypoxia inducer-1 exhibits highly selective NO release under hypoxic conditions and inhibits hypoxia-induced apoptosis, necrosis, and the increase in ROS levels. Hypoxia inducer-1 regulates vascular dilation and has a protective effect in a mouse model of myocardial hypoxia injury. Hypoxia inducer-1 can be used in the research of coronary heart disease .
|
-
- HY-159962
-
|
|
Glutaminase
|
Metabolic Disease
|
|
TGase2-IN-1 (Compound 22) is an orally active inhibitor for TGase2 with an IC50 of 1.12 μM. TGase2-IN-1 inhibits TGase2 in human retinal microvascular endothelial cells with an IC50 of 0.07 μM. TGase2-IN-1 exhibits 74.6% oral bioavailability. TGase2-IN-1 inhibits retinal vascular leakage in mouse Streptozotocin (HY-13753)-induced diabetic model .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-161520
-
|
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
|
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model .
|
-
- HY-162645
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
|
-
- HY-B0722
-
|
|
Endogenous Metabolite
Reactive Oxygen Species
|
Metabolic Disease
Cancer
|
|
Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
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-
- HY-153896
-
|
|
c-Met/HGFR
|
Cancer
|
|
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
|
-
- HY-170495
-
|
|
HDAC
Apoptosis
Interleukin Related
|
Inflammation/Immunology
|
|
HDAC6 degrader-5 (Compound 6) exhibits inhibitory and degradation activity against HDAC6, with an IC50 of 4.95 nM and a DC50 of 0.96 nM. HDAC6 degrader-5 inhibits the release of TNF-α, IL-1β and IL-6, blocks the hepatocyte apoptosis. HDAC6 degrader-5 exhibits anti-inflammatory activity in mouse APAP (HY-66005)-induced liver injury models .
|
-
- HY-161072
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
CSC-6 is a NLRP3 inhibitor. CSC-6 can significantly inhibit IL-1β secreted by PMATHP-1 cells with an IC50 value of 2.3 μM. CSC-6 specifically binds NLRP3 and inhibits NLRP3 activation by blocking ASC oligomerization during NLRP3 assembly. CSC-6 effectively reduces the symptoms of NLRP3 overactivation-mediated sepsis and gout in mouse models .
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-
- HY-103171R
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BAY 60-6583 (Standard) is the analytical standard of BAY 60-6583. This product is intended for research and analytical applications. BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50?= 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model .
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-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
- HY-147696
-
|
|
HSP
AMPK
Reactive Oxygen Species
|
Cancer
|
|
SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
|
-
- HY-161631
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
|
-
- HY-170796
-
|
|
Amylases
|
Metabolic Disease
|
|
α-Amylase-IN-11 (compound C5f) is an α-Amylase inhibitor (IC50=0.56 μM) that can reduce the sugar level in vivo. α-Amylase-IN-11 has a moderate inhibitory effect on α-glucosidase (α-glucosidase), with IC50=11.03 μM. α-Amylase-IN-11 can significantly reduce the glucose concentration in a mouse model and has the potential for use in diabetes research .
|
-
- HY-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
|
-
- HY-160843
-
|
|
Apoptosis
|
Cancer
|
|
N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
|
-
- HY-148794
-
|
IkT-148009
|
c-Met/HGFR
Bcr-Abl
|
Neurological Disease
Cancer
|
|
Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD .
|
-
- HY-117088
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
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-
- HY-135317B
-
|
CA-4948 hydrochloride
|
IRAK
FLT3
Apoptosis
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317). Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib hydrochloride inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib hydrochloride exhibits antitumor activity in mouse model .
|
-
- HY-170568
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
|
-
- HY-173075
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Cancer
|
|
Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-168709
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC50 of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model .
|
-
- HY-161834
-
|
|
Pyroptosis
Aquaporin
NOD-like Receptor (NLR)
p38 MAPK
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
RG100204 is a selective, orally available inhibitor of the aquaporin AQP9. RG100204 directly inhibits AQP9 channel function, preventing the transmembrane transport of water, glycerol, and H 2O 2. RG100204 reduces the activation of the NLRP3 inflammasome and p38 MAPK signaling pathways, thereby alleviating inflammation and pyroptosis. RG100204 reduces multi-organ dysfunction in a mouse sepsis model and shows glucose-regulating effects in diabetic db/db mice .
|
-
- HY-B1864BR
-
|
Ksg hydrochloride hydrate (Standard)
|
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate (Standard) is the analytical standard of Kasugamycin hydrochloride hydrate (HY-B1864B). This product is intended for research and analytical applications. Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
|
-
- HY-135317D
-
|
CA-4948 mesylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model .
|
-
- HY-168729
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 256 (Compound C09) is an inhibitor for type I signal peptidase (SPase I). Antibacterial agent 256 inhibits gram-positive bacteria, that inhibits S. aureus ATCC 29213, E. faecium QF31, E. faecalis SF23-1 and S. suis P1/7, with MIC of 1-16 μg/mL. Antibacterial agent 256 exhibits cytotoxicity in cancer cell HEp-2 and Caco-2 with CC50 of 14.65 μg/mL and 21.93 μg/mL. Antibacterial agent 256 exhibits a hemolytic activity on mouse RBCs, with an HC50 of 13.29 μg/mL. Antibacterial agent 256 ameliorates the MRSA skin infection in mouse model .
|
-
- HY-151563A
-
|
|
Deubiquitinase
|
Cancer
|
|
OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
|
-
- HY-118899
-
|
|
Endogenous Metabolite
|
Cancer
|
|
XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
|
-
- HY-W010649
-
|
|
HSP
Epigenetic Reader Domain
ATP-binding cassette (ABC) transporters
Bacterial
Fungal
Antibiotic
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-163765
-
|
|
PI4K
Potassium Channel
|
Infection
|
|
Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models .
|
-
- HY-132192
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
|
-
- HY-14342A
-
|
|
Bombesin Receptor
|
Metabolic Disease
|
|
(R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
- HY-P991328
-
|
|
Notch
|
Cancer
|
|
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
|
-
- HY-19109
-
|
|
Leukotriene Receptor
|
Others
|
|
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
|
-
- HY-107811R
-
|
|
Apoptosis
Monoamine Oxidase
Autophagy
α-synuclein
Mitosis
|
Neurological Disease
Cancer
|
|
Harmol (Standard) is the analytical standard of Harmol (HY-107811). This product is intended for research and analytical applications. Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model .
|
-
- HY-N0352
-
|
|
Parasite
|
Infection
|
|
Tuberostemonine is a stenine alkaloid that can be isolated from Stemona tuberosa and Stemona sessifolia. Tuberostemonine is an antimalarial agent that has inhibitory activity against Ferredoxin-NADP + reductases (FNRs) from Plasmodium falciparum (PfFNR). Tuberostemonine can reduce the number of citric acid-induced coughs in guinea pigs. Tuberostemonine decreases bronchoalveolar lavage fluid (BALF), neutrophil and macrophage infiltration and reduces peribronchial and perivascular inflammatory cell infiltration in mouse model of acute lung inflammation. Tuberostemonine has a level of activity as a feeding deterrent .
|
-
- HY-114622
-
|
API-1252 tosylate; Debio 1452 tosylate
|
Bacterial
Antibiotic
|
Infection
|
|
AFN-1252 (API-1252) tosylate is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 tosylate exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 tosylate exhibits typical MIC90 values of 0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 tosylate is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
|
-
- HY-117694
-
|
|
CGRP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
MK-8825 is an orally active, potent and selective CGRP receptor antagonist, which shows concentration-dependent inhibition of Capsaicin (HY-10448)-evoked dermal blood flow with an EC50 value of about 7.4 μM. MK-8825 inhibits CGRP-induced spontaneous nociceptive facial grooming behaviors, neuronal activation in the trigeminal nucleus, and systemic release of pro-inflammatory cytokines in a mouse model of acute orofacial masseteric muscle pain. MK-8825 is promising for research of acute migraine .
|
-
- HY-157892
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 38 is an orally active antimalarial agent, which inhibits Plasmodium falciparum D6 strain, Chloroquine (HY-17589A)-sensitive Thai strain and Chloroquine-resistant FcB1 strain and K1 strain, with IC50s of 0.5, 13, 1 and 13 μM, respectively. Antimalarial agent 38 is non-cytotoxic for mammalian cells MCR58 (IC50 >140 μM). Antimalarial agent 38 improves the survival rate of Plasmodium yoelii nigeriensis infected mouse model .
|
-
- HY-148813
-
|
|
PROTACs
STAT
|
Cancer
|
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155781
-
|
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COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
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-
- HY-132192A
-
|
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PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
|
-
- HY-154851
-
|
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GSK-3
CDK
Tau Protein
|
Neurological Disease
|
|
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
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-
- HY-120356A
-
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TAI-95 tosylate
|
NEKs
Apoptosis
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Cancer
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|
T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models .
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-
- HY-149948
-
|
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Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
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-
- HY-176457
-
|
|
Small Interfering RNA (siRNA)
MDM-2/p53
PROTACs
|
Cancer
|
|
ZS3-046 is a TAF1 PROTAC degrader. ZS3-046 promotes the ubiquitination and degradation of TAF1. ZS3-046 activates p53 and induces apoptosis in acute myeloid leukemia (AML) cells. ZS3-046 has antitumor activity in an AML tumor xenograft mouse model. (Target protein ligand (HY-176467); CRBN ligase (HY-41547); Linker (HY-176469); CRBN ligase + Linker (HY-176450)) .
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- HY-111310
-
ML351
1 Publications Verification
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Lipoxygenase
|
Neurological Disease
Metabolic Disease
|
|
ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2 . ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D .
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- HY-17600R
-
|
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Btk
|
Cancer
|
|
Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-146755
-
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Trk Receptor
|
Cancer
|
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
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- HY-172409
-
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Cannabinoid Receptor
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
CB1R antagonist 2 (Compound 11g) is the antagonist for cannabinoid receptor 1 (CB1R), that inhibits MAPK/NF-κB signaling pathway and exhibits anti-inflammatory activity. CB1R antagonist 2 inhibits LPS (HY-D1056)-induced IL-6, IL-1β and TNF-α expressions in RAW264.7. CB1R antagonist 2 ameliorates OVA-induced allergic rhinitis in mouse models .
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-
- HY-159925
-
|
|
Cyclic GMP-AMP Synthase
|
Infection
Inflammation/Immunology
|
|
QKY-613 is a prodrug that enhances immune surveillance by targeting nucleic acid modification pathways. QKY-613 promotes the selective incorporation of 6mdA (N6-methyldeoxyadenosine) into viral DNA, enhancing the phase separation potential of DNA, thereby increasing the activation of cGAS and strengthening host immune surveillance. In virus-infected mouse models, QKY-613 significantly reduced mortality in aged mice. QKY-613 holds promise for research on nucleic acid modification-based immune surveillance mechanisms .
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-
- HY-170583
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
hAChE-IN-10 (Compound ET11) is the inhibitor for human acetylcholinesterase (AChE) with an IC50 of 6.34 nM. hAChE-IN-10 scavenges free radicals, and exhibits antioxidant activity. hAChE-IN-10 exhibits metal chelating activity, inhibits Cu 2+-induced Aβ1-42 aggregation, reduces the formation of amyloid plaques, and exhibits neuroprotective activity. hAChE-IN-10 ameliorates the Scopolamine (HY-N0296)-induced cognitive impairment in mouse models .
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-
- HY-163512
-
|
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HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body .
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-
- HY-162829
-
|
|
URAT1
GLUT
|
Metabolic Disease
|
|
hURAT1 inhibitor 1 (compound 27b) is an isomarine-based, orally active dual hURAT1/GLUT9 inhibitor with IC50s of 0.16 μM and 4.47 μM, respectively, and has anti-hyperuricemia effects. hURAT1 inhibitor 1 showed significant uric acid-lowering activity in a hyperuricemia mouse model (10 mg/kg dose). hURAT1 inhibitor 1 had no significant in vitro cytotoxicity or in vivo hepatotoxicity and showed good PK characteristics .
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-
- HY-163481
-
|
|
Bacterial
|
Infection
|
|
Antibiofilm agent-6 (Compound 26c) is a quorum sensing inhibitor with strong antibiofilm effects that can inhibit the fluorescence intensity of PAO1-lasB-gfp and PAO1-pqsA-gfp in a concentration-dependent manner. Antibiofilm agent-6 can inhibit the production of pyocyanin and rhamnolipid. Antibiofilm agent-6 aids helps ciprofloxacin (HY-B0356) effectively eliminate the living bacteria in a mouse model infected with P. aeruginosa PAO1 .
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-
- HY-17638A
-
|
DSP-3235 (sebacate); KGA-3235 (sebacate); GSK-1614235 (sebacate)
|
SGLT
|
Neurological Disease
|
|
Mizagliflozin sebacate (DSP-3235 sebacate) is a sodium-glucose cotransporter inhibitor with activity in improving vascular cognitive impairment caused by small vessel disease. Mizagliflozin sebacate improves blood flow and reverses vascular cognitive impairment by inhibiting neuronal SGLT1 activity. Mizagliflozin sebacate also showed the ability to increase the survival rate of IL-1β-treated PC12HS cells. Mizagliflozin sebacate promotes improvements in spatial learning and memory caused by small vessel disease in mouse models .
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- HY-117356A
-
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P2Y Receptor
NF-κB
ERK
Apoptosis
|
Inflammation/Immunology
|
|
MRS2693 ammonium is the ammonium dalt form of MRS2693 (HY-117356). MRS2693 ammonium is a selective agonist for P2Y6 with an EC50 of 0.015 μM. MRS2693 ammonium protects C2C12 skeletal muscle cells from TNFα-induced apoptosis. MRS2693 ammonium reduces the activation of NF-kB, activates the ERK1/2 pathway, and has a cytoprotective effect on mouse ischemia-reperfusion injury model [2].
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-
- HY-156025
-
|
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Hydroxycarboxylic Acid Receptor (HCAR)
|
Inflammation/Immunology
|
|
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
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-
- HY-155848
-
|
|
Phosphatase
|
Cancer
|
|
LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
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-
- HY-N13083
-
|
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PCSK9
|
Cardiovascular Disease
|
|
PCSK9-IN-28 (Compound C11) is a PCSK9 inhibitor that can be isolated from Euphorbia esula. By binding to HNF1α, PCSK9-IN-28 inhibits PCSK9 transcription by binding to HNF1α and affecting its nuclear distribution, thereby enhancing LDLR and promoting LDL uptake. PCSK9-IN-28 exhibits significant lipid-lowering activity in the high-fat diet (HFD) mouse model and can be used in the study of hyperlipidemia .
|
-
- HY-168770
-
|
|
RIP kinase
TNF Receptor
Apoptosis
|
Cardiovascular Disease
|
|
Cl-Necrostatin-1 is a RIPK1 inhibitor. Cl-Necrostatin-1 can also inhibit TNF-α-induced necroptosis in Jurkat cells deficient in Fas-associated death domain protein (FADD; EC50 = 180 nM), a modification that prevents caspase activation in response to death-domain receptor signaling. Cl-Necrostatin-1 can also reduce infarct size in a mouse model of middle cerebral artery occlusion (MCAO). Cl-Necrostatin-1 is used for research in cardiovascular and cerebrovascular diseases .
|
-
- HY-169403
-
|
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STAT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
|
-
- HY-111817A
-
|
|
Parasite
|
Infection
|
|
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.
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-
- HY-123045
-
|
|
CDK
|
Cancer
|
|
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
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-
- HY-170402
-
|
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Sirtuin
Apoptosis
|
Cancer
|
|
SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
|
-
- HY-168773
-
|
|
EAAT
|
Neurological Disease
|
|
(R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. (R)-AS-1 (at doses of 60 and 90 mg/kg) increases spontaneous locomotor activity in mice. Additionally, it demonstrates anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electrical stimuli (32 or 44 mA), with ED50s of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. (R)-AS-1 can be used in neurological disease research .
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-
- HY-142042
-
|
|
MEK
TGF-beta/Smad
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor for bone morphogenetic protein 2 (BMP2) with an IC50 of 2.2 μM. 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is inhibitor for mitogen-activated protein kinase 1 (MEK1). 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles exhibits anti-inflammatory and neuroprotective activity in EAE mouse model .
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-
- HY-162688
-
|
|
Telomerase
G-quadruplex
Apoptosis
Ferroptosis
|
Others
|
|
Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model .
|
-
- HY-168589
-
|
|
Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species
|
Cancer
|
|
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
|
-
- HY-163027
-
|
|
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research .
|
-
- HY-169478
-
|
|
Liposome
|
Cancer
|
|
Lipid N2-3L is an ionizable cationic lipid (pKa = 8.99) that can be used to generate supramolecular lipid nanoparticles (SMLNPs) for mRNA delivery. Lipid nanoparticles formed by encapsulating a luciferase reporter gene with Lipid N2-3L were detected to accumulate in the lymph nodes of mice, indicating that they can effectively enter the mouse immune system. Lipid nanoparticles formed by encapsulating ovalbumin mRNA and the TLR7/8 agonist Resiquimod (HY-13740) with Lipid N2-3L were able to reduce tumor volume and increase survival in the MC-38-OVA mouse colon cancer model. Lipid N2-3L can be used in the research of drug delivery for cancer-related therapies .
|
-
- HY-107588
-
TC-I 15
1 Publications Verification
|
Integrin
|
Cardiovascular Disease
|
|
TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
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-
- HY-173048
-
|
|
ClpP
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-158783
-
|
|
Ceramidase
Bcl-2 Family
LPL Receptor
Apoptosis
|
Neurological Disease
|
|
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-173184
-
|
|
HDAC
|
Inflammation/Immunology
|
|
HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. HDAC6-IN-53 exerts the activity of inhibiting the phenotype of idiopathic pulmonary fibrosis (IPF) by suppressing the collagen expression induced by TGF-β1, and it has demonstrated a good therapeutic effect in a mouse model of pulmonary fibrosis induced by bleomycin (HY-108345). HDAC6-IN-53 can be used in the research of idiopathic pulmonary fibrosis and other related pulmonary fibrosis diseases.
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-N11768
-
|
|
NF-κB
Interleukin Related
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .
|
-
- HY-162644
-
|
|
PD-1/PD-L1
PARP
|
Cancer
|
|
Antitumor agent-170 (Compound C6) exhibits inhibitory activities against PD-1/PD-L1 interaction and PARP7, with IC50 of 0.342 μM and 7.05 nM. Antitumor agent-170 exhibits a high affinity to human PD-L1, with a Ki of 9.31 nM. Antitumor agent-170 restores the T cell function and increases IFN-γ secretion. Antitumor agent-170 exhibits antitumor efficacy against melanoma in mouse models and good pharmacokinetic characteristics .
|
-
- HY-19487
-
|
|
Bacterial
|
Infection
|
|
Ribocil is a selective inhibitor targeting the bacterial FMN riboswitch, regulating the bacterial riboflavin riboswitch. Ribocil competitively binds to the FMN binding site, mimicking the natural ligand FMN to induce conformational changes in the riboswitch, inhibiting ribB gene expression, reducing riboflavin synthesis, and thus inhibiting bacterial growth. Ribocil strongly inhibits GFP expression (EC50=0.3 μM). Ribocil exhibits in vivo antibacterial activity in a mouse model and can be used to study antibacterial drugs related to drug-resistant bacterial infections and bacterial riboflavin metabolic pathways[1][2].
|
-
- HY-16468
-
|
MSI-1256
|
Bacterial
HBV
FAK
Dengue Virus
|
Infection
Neurological Disease
Cancer
|
|
Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson ,s disease mouse models .
|
-
- HY-18652A
-
|
Ro 5126766 potassium; CH5126766 potassium
|
Raf
MEK
|
Cancer
|
|
Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-172092
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
BG11 induces the accumulation of Fe 2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models .
|
-
- HY-170448
-
|
|
PROTACs
Androgen Receptor
|
Endocrinology
|
|
PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM. PROTAC AR Degrader-9 promotes the expressions of paracrine factors, such as TGF-β1 and β-catenin, exhibits hair regenerating efficacy in mouse models . (Pink: ligand for target protein AR ligand-38 (HY-170450); Black: linker; Blue: ligand for E3 ligase Cereblon (HY-170449))
|
-
- HY-120920
-
|
|
Dopamine Receptor
|
Inflammation/Immunology
|
|
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .
|
-
- HY-100847
-
|
|
PARP
|
Cancer
|
|
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models .
|
-
- HY-161644
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-27 (Compound 41) is an orally active inhibitor for phosphorylation of STAT3 (KD is 4.4 μM) and STAT3 transcription (IC50 is 22.57 nM). STAT3-IN-27 inhibits proliferation of various cancer cells with IC50 of 10-500 nM. STAT3-IN-27 arrests the cell cycle at G2/M phase, induces mitochondrial dysfunction and apoptosis in HCT116, inhibits cell migration of HCT116. STAT3-IN-27 exhibits antitumor efficacy in mouse model .
|
-
- HY-19522C
-
|
MBX-8025 Lysine dihydrate; RWJ-800025 Lysine dihydrate
|
PPAR
|
Metabolic Disease
|
|
Seladelpar (MBX-8025) Lysine dihydrate is the Lysine dihydrate salt form of Seladelpar (HY-19522). Seladelpar Lysine dihydrate is an orally active agonist for potent PPAR-δ, with EC50 of 2 nM. Seladelpar Lysine dihydrate shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar Lysine dihydrate can be used for the study of primary biliary cholangitis. Seladelpar Lysine dihydrate normalizes hyperglycemia, hyperinsulinemia, glucose, serum lipids and cholesterol levels, ameliorates the nonalcoholic steatohepatitis in mouse model .
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-
- HY-172135
-
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p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
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PDE4-IN-26 (Compound A5) is an orally active and highly selective PDE4 inhibitor. PDE4-IN-26 has anti-inflammatory activity and can inhibit the phosphorylation of p38 MAPK. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 can improve pulmonary inflammation, injury and fibrosis, promote sputum secretion and relieve cough in mice. PDE4-IN-26 can be used for the research of lung injury-related diseases .
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-
- HY-145580
-
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UCB0599; (R)-NPT200-11
|
α-synuclein
|
Neurological Disease
|
|
Minzasolmin (UCB0599; (R)-NPT200-11) is an orally active, blood-brain-permeable α-synuclein (α-Syn) inhibitor that selectively binds to α-Syn misfolded intermediates (such as oligomers) and inhibits aggregation and fibril formation by regulating their conformational stability. Minzasolmin can reduce the generation of pathological oligomers and block neurotoxic signaling, thereby reducing the abnormal accumulation of α-Syn in the brain. Minzasolmin significantly improved motor deficits, reduced neuroinflammatory markers, and α-Syn-related pathological deposition in transgenic mouse models .
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- HY-172088
-
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Microtubule/Tubulin
MMP
NF-κB
Apoptosis
|
Cancer
|
|
Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC50 of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models .
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-
- HY-162873
-
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MEK
Raf
|
Cancer
|
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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- HY-170799
-
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|
DNA/RNA Synthesis
SARS-CoV
Arenavirus
|
Infection
|
|
HNC-1664 is the orally active inhibitor for RNA-dependent RNA polymerase (RdRP). HNC-1664 exhibits broad-spectrum antiviral activity against coronavirus (SARS-CoV-2 wildtype and its mutants XBB.1.18, HK.3.1, BF.7.14, BA.1HCoV-229E, HCoV-OC43) and arenavirus. HNC-1664 exhibits anti-infectious activity in SARS-CoV-2 Delta infected mouse models .
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- HY-170855A
-
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PROTACs
RET
|
Cancer
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|
YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858) .
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-
- HY-172264
-
|
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Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
XT17 is an anthrone compound with broad-spectrum antibacterial activity. It exerts its antibacterial effect by disrupting the cell wall and inhibiting DNA synthesis. XT17 exhibits weak hemolytic activity, low cytotoxicity against mammalian cell lines, and a low frequency of drug resistance. Meanwhile, XT17 shows in vivo efficacy in a mouse corneal infection model induced by Staphylococcus aureus or Pseudomonas aeruginosa. Further docking studies have confirmed that XT17 can form a stable complex with bacterial gyrase. XT17 can be used in the research of the anti - infection field .
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-
- HY-163436
-
|
|
FXR
Cytochrome P450
RAR/RXR
PPAR
ROR
|
Metabolic Disease
|
|
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders .
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-
- HY-154968
-
|
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RSV
|
Infection
|
|
RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection .
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-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
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-
- HY-168439
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
HLB-0532259 is a PROTAC degrader for Aurora-A and N-Myc. HLB-0532259 degrades Aurora-Ain a non-MYCN amplified MCF-7 with a DC50 of 20.2 nM, degrades N-Myc in MYCN amplified cells SK-N-BE and Kelly with DC50 of 179 nM and 229 nM. HLB-0532259 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-168440); Black: linker (HY-W007957); Blue: ligand for E3 ligase Cereblon (HY-41547))
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-
- HY-157169
-
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AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
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-
- HY-173522
-
|
|
Kinesin
|
Cancer
|
|
KIF2C-IN-1 (Compound 7S9) is a selective and potent small-molecule KIF2C inhibitor. KIF2C-IN-1 stabilizes the KIF2C-tubulin interaction, blocking the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel (HY-B0015) in paclitaxel-resistant triple-negative breast cancer (TNBC) cells and significantly reduces tumor growth combined with Paclitaxel in mouse models .
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-
- HY-126876
-
|
|
Apoptosis
AMPK
Reactive Oxygen Species
|
Cancer
|
|
GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
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-
- HY-115574
-
|
|
RSV
|
Infection
|
|
RSV L-protein-IN-1 (compound D) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.021 μM). RSV L-protein-IN-1 inhibits Polymerase (IC50=0.089 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-1 shows moderate cytotoxicity (CC50=8.4 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection .
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-
- HY-P10947
-
|
|
Epigenetic Reader Domain
YAP
|
Cancer
|
|
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
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-
- HY-Y0546R
-
|
|
Endogenous Metabolite
Photosensitizer
|
Cancer
|
|
Benzophenone (Standard) is the analytical standard of Benzophenone. This product is intended for research and analytical applications. Benzophenone standard is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone standard can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone standard can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone standard exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone standard exhibits estrogenic activity .
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-
- HY-33299
-
|
BTCA
|
Biochemical Assay Reagents
|
Cancer
|
|
Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
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-
- HY-139792
-
|
SHR117887
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Besigliptin tosylate (SHR117887) is a DPP-4 inhibitor with activity to improve metabolic control and β-cell function. Besigliptin tosylate can effectively reduce serum DPP-4 activity and improve oral glucose tolerance. Besigliptin tosylate significantly reduces fasting blood glucose levels and improves lipid profiles in a diabetic mouse model. The effect of besigliptin tosylate is comparable to that of the known compound vildagliptin (HY-14291) at the same concentration. Besigliptin tosylate increases insulin staining of pancreatic islet cells in chronic administration, indicating improved β-cell function .
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-
- HY-161778
-
|
|
HDAC
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization .
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- HY-N10439
-
|
|
Glycosidase
|
Inflammation/Immunology
|
|
3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitory activity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibits MPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear .
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-
- HY-P10415
-
|
hSA(408–423) peptide
|
CXCR
|
Infection
Inflammation/Immunology
Cancer
|
|
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
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-
- HY-112142A
-
|
DVR-23
|
HBV
|
Inflammation/Immunology
|
|
(Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .
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-
- HY-170228
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
Kit-IN-9 (Compound D9) is an inhibitor of c-Kit. c-Kit-IN-9 inhibits the inflammatory responses in J774A.1, RAW264.7, MPMs cells and lung tissues by blocking the activation of the NF-κB pathway induced by LPS (HY-D1056). Meanwhile, c-Kit-IN-9 exhibits good anti-inflammatory activities in acute lung injury and sepsis mouse models. c-Kit-IN-9 can be used in the research of acute lung injury and related inflammatory diseases .
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-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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-
- HY-168438
-
|
|
EGFR
Akt
ERK
|
Cardiovascular Disease
|
|
ERBB agonist-1 (Compound EF-1) is an agonist for ERBB4, that activates the ERBB4 signaling pathway by inducing dimerization of the ERBB4 receptor with an EC50 of 10.5 μM. ERBB agonist-1 induces phosphorylation of Akt and ERK1/2, reduces the collagen expression in cardiac fibroblasts, inhibits H2O2-induced cardiomyocyte death and Ang II (HY-13948)-induced cardiomyocyte hypertrophy. ERBB agonist-1 prevents fibrosis and exhibits cardioprotective efficacy in mouse models .
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-
- HY-168102
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
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-
- HY-173235
-
|
|
Galectin
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Galectin-3-IN-6 (Compound 12) is an orally active inhibitor of galectin-3 (Gal-3), with an IC50 value of 12 nM and a Kd value of 13 nM for Gal-3. In a mouse model of acute liver injury and fibrosis induced by CCl4, Galectin-3-IN-6 can significantly reduce the levels of fibrosis markers collagen-1 and α-smooth muscle actin (αSMA) by 64% and 71%, respectively, showing significant anti-fibrotic activity. Galectin-3-IN-6 can be used in the research of fibrotic diseases, cancer, and cardiovascular diseases .
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-
- HY-149913
-
|
|
Orphan Receptor
|
Cancer
|
|
NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model .
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-
- HY-160887
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
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-
- HY-176451
-
|
|
CDK
|
Cancer
|
|
CDK9 degrader-1 is a selective CDK9 degrader (DC50: 0.4073 µM). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway and forms autophagosomes by recruiting LC3, which then fuses with lysosomes to degrade CDK9 and its partner protein Cyclin T1 (DC50: 1.215 µM). CDK9 degrader-1 induces caspase 3-mediated apoptosis. CDK9 degrader-1 has antitumor activity in a mouse HCT116 xenograft model .
|
-
- HY-P99667
-
|
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
|
-
- HY-168716
-
|
|
SOS1
Ras
|
Cancer
|
|
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC50 of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC50 of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC50 of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .
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-
- HY-129510R
-
|
|
EGFR
Mitosis
|
Cancer
|
|
4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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-
- HY-W276819
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-9 (Compound M2) is an inhibitor for polo-like kinase 1 (PLK1), that inhibits PLK proteins modified with peptides 1010pT, cdc25c and PBIP, with IC50s of 1.6, 0.8 and 1.4 μM, respectively. PLK1-IN-9 inhibits proliferations of cancer cells HeLa, HL60, SNU387/499, HepG2, exhibits cytotoxicity and induces apoptosis. PLK1-IN-9 inhibits tumor growth in HepG2 xenograft mouse model .
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-
- HY-155731
-
|
|
Influenza Virus
|
Infection
|
|
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM .
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-
- HY-170574
-
|
|
Molecular Glues
Ser/Thr Kinase
Apoptosis
|
Cancer
|
|
CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .
|
-
- HY-W753806
-
|
UK 33274 hydrochloride
|
Akt
|
Cardiovascular Disease
|
|
Doxazosin hydrochloride (UK 33274 hydrochloride) is a compound used to inhibit hypertension and prostate hyperplasia, with activity that inhibits postsynaptic α1-adrenoceptors on vascular smooth muscle. Doxazosin hydrochloride can cause vasodilation, thereby reducing peripheral vascular resistance. Doxazosin hydrochloride was found to inhibit the proliferation and migration of hepatic stellate cells in a mouse liver fibrosis model. Doxazosin hydrochloride regulates fibrosis, autophagy, and apoptosis of hepatic stellate cells by activating the PI3K/Akt/mTOR signaling pathway. Doxazosin hydrochloride also blocks autophagic flux and induces apoptosis of hepatic stellate cells .
|
-
- HY-170451
-
|
|
PROTACs
MDM-2/p53
Apoptosis
|
Cancer
|
|
KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. KT-253 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))
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-
- HY-170405
-
|
|
PROTACs
mTOR
|
Cancer
|
|
YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
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-
- HY-161781
-
|
|
HSP
EGFR
Akt
Survivin
|
Cancer
|
|
HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-B0722R
-
|
|
Endogenous Metabolite
Reactive Oxygen Species
|
Metabolic Disease
Cancer
|
|
Histamine (dihydrochloride) (Standard) is the analytical standard of Histamine (dihydrochloride). This product is intended for research and analytical applications. Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
|
-
- HY-155523
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
|
Cancer
|
|
Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
|
-
- HY-155732
-
|
|
Parasite
|
Infection
|
|
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
|
-
- HY-P5396
-
|
|
Amino Acid Decarboxylase
|
Others
|
|
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
|
-
- HY-125726
-
|
(3'-sulfo)Galβ-Cer(d18:1/24:1); N-Nervonoyl Sulfatide; C24:1 Sulfatide
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
Sulfo galactosylceramide (N-Nervonoyl Sulfatide; C24:1 Sulfatide) is a glycolipid and the major sulfolipid species in mature myelin. Sulfo galactosylceramide interacts with C-type lectins and immunoglobulin-like receptors, with the highest affinity for LMIR5. Sulfo galactosylceramide induces MCP-1 production by basophils but not mast cells, and increases NFAT activation via LMIR5. Sulfo galactosylceramide alleviates symptoms and improves survival in a mouse model of chronic relapsing-remitting experimental autoimmune encephalomyelitis (EAE), and reduces inflammatory lesions and the number of infiltrating mononuclear cells in the lumbar spinal cord of EAE mice.
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-
- HY-115987
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
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- HY-169864
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LPL Receptor
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Inflammation/Immunology
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KRO-105714 is the antagonist for sphingosine phosphocholine receptor (SPC Receptor) and sphingosine-1-phosphate receptor 1 (S1P1 Receptor) (IC50=79.2 nM). KRO-105714 inhibits SPC-induced proliferation of NIH3T3 (IC50=5.6 nM), inhibits SPC-induced cell migration (IC50=0.59 μM) and tube formation in HUVECs. KRO-105714 inhibits SPC-induced generation of IL-4 and IL-5, exhibits anti-inflammtory efficacy in mouse atopic dermatitis models .
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- HY-148409
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Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
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Cancer
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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- HY-163909
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable .
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- HY-113058
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Endogenous Metabolite
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Metabolic Disease
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3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
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- HY-134090
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Antibiotic TS 885; NSC 248958
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Bacterial
VSV
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Infection
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9-Methylstreptimidone is a microbial metabolite originally isolated from Streptomyces sp. S-885 that has antifungal and antiviral activities. It is active against several fungi, including S. sake, S. fragilis, R. rubra, T. rubra, and C. albidus (MICs=4-20 μg/mL) and has antiviral activity against poliovirus, vesicular stomatitis virus (VSV), and Newcastle disease virus (NDV) in vitro (MIC=0.02 μg/mL for all). 9-Methylstreptimidone increases survival in mouse models of infection with influenza A2 (H2N2) or C. albicans when administered prior to infection.
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- HY-145549
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N-eicosanoyl-D-erythro-Sphingosylphosphorylcholine; SM(d18:1/20:0)
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Endogenous Metabolite
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Endocrinology
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C20 Sphingomyelin (d18:1/20:0) (N-eicosanoyl-D-erythro-Sphingosylphosphorylcholine; SM(d18:1/20:0)) is a naturally occurring sphingolipid. C20 Sphingomyelin (d18:1/20:0) levels are upregulated in the hippocampus of streptozotocin (HY-13753)-induced diabetic rats and in human plasma, positively correlating with insulin resistance in obese humans. C20 Sphingomyelin (d18:1/20:0) is also upregulated in the liver of a mouse model of Niemann-Pick C1 disease, a neurodegenerative cholesterol sphingolipid lysosomal storage disorder.
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- HY-172399
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Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
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Cancer
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|
FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC50 of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC50 for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .
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- HY-169831
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|
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α-synuclein
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Neurological Disease
|
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HUP-55 is a prolyl endopeptidase inhibitor (IC50 = 5 nM). HUP-55 reduces the dimerization of α-synuclein in Neuro2a cells and induces autophagy (Autophagy) in HEK293 cells. It also decreases the increase in reactive oxygen species (ROS) production induced by hydrogen peroxide in SH-SY5Y cells at a concentration of 10 μM. In a mouse Parkinson’s disease model, HUP-55 (10 mg/kg) improves motor function (reduces the use frequency of the impaired paw) and decreases the levels of harmful oligomers of α-synuclein in the striatum caused by overexpression of α-synuclein .
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- HY-163767
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β-catenin
|
Inflammation/Immunology
Cancer
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Antitumor agent-171 (Compound 35) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 1.61 μM. Antitumor agent-171 exhibits high affinity to β-catenin with Kd of 0.63 μM. Antitumor agent-171 inhibits the gene expression of axin2 with IC50 of 0.84 μM. Antitumor agent-171 inhibits cell viability of HCT116 with IC50 of 4.39 μM. Antitumor agent-171 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
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-
- HY-172113
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PROTACs
YAP
c-Myc
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Cancer
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H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM, and exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki of 2.0, 3.6 and 1.6 nM. H122 downregulates the expression of Myc. H122 inhibits the cell growth of MSTO-211H and NCI-H226 with IC50 of 21.3 nM and 0.6 nM, and exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-151525); Black: linker (HY-W573128); Blue: ligand for E3 ligase Cereblon (HY-W087383))
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- HY-P10870
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Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
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Cancer
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Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
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- HY-137936
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Antibiotic
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Infection
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Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs=25, 50, and 25 μg/mL, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells.2 In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P388 murine leukemia.
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- HY-123960
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Raphin1
3 Publications Verification
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Phosphatase
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Neurological Disease
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Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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- HY-170403
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Histone Demethylase
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Cancer
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LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .
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- HY-161641
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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- HY-168081
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-52 (Compound III-5) is an orally active PD-1/PD-L1 inhibitor that blocks the interaction between PD-1 and PD-L1, with an IC50 of 109.9 nM. PD-1/PD-L1-IN-52 exhibits antitumor activity in a C57BL/6 mouse xenograft model implanted with human PD-1-expressing MC38 colon cancer cells, with a TGI of 49.6% .
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- HY-172209
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p38 MAPK
Apoptosis
Reactive Oxygen Species
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Cancer
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PPIA-IN-1 (Compound 20b) is the inhibitor for peptidylprolyl isomerase A (PPIA) with a KD of 0.52 μM. PPIA-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for HCT116 is 0.69 μM), arrests the cell cycle at G0/G1 phase, and exhibits anti-metastatic effect in cell HCT116. PPIA-IN-1 increases ROS, causes DNA damage, ER stress and mitochondrial dysfunction, inducing apoptosis in HCT116 through MAPK pathway. PPIA-IN-1 exhibits antitumor activity in mouse CT26 xenograft models .
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- HY-N0507
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TNF Receptor
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-162643
-
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PD-1/PD-L1
PARP
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Cancer
|
|
Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics .
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- HY-149127
-
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ASC-JM17; ALZ-003
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Keap1-Nrf2
Androgen Receptor
HSP
Mitophagy
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Metabolic Disease
|
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Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
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- HY-P99116
-
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RG7716
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VEGFR
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
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- HY-113817
-
|
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Phosphatase
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Inflammation/Immunology
|
|
SHIP1 activator 1 is an SH3 domain-containing inositol 5-phosphatase regulator with SHIP1 activating activity. SHIP1 activator 1 retains its SHIA-1 activating ability by removing unnecessary functional groups. SHIP1 activator 1 is able to activate SHIP1 in vitro, inhibit Akt phosphorylation in MOLT-4 cells, and show dose-dependent activity in a mouse model of inflammation. SHIP1 activator 1 is an important chemical tool for evaluating the potential of SHIP1 activators as inhibitors of hematopoietic diseases involving abnormal PI3K cell signaling .
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- HY-P10744
-
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-123960A
-
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Phosphatase
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Neurological Disease
|
|
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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- HY-169830
-
|
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Drug Derivative
Apoptosis
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Cancer
|
|
2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model .
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- HY-113509B
-
|
15-epi-LXA4
|
STAT
|
Neurological Disease
Inflammation/Immunology
|
|
15(R)-Lipoxin A4 (15-epi-LXA4) is a STAT-6 activator and a lipid-derived lipoxin-type specialized pro-resolving mediator (SPM) that plays a role in promoting inflammation resolution and regulating immune cell function. 15(R)-Lipoxin A4 can improve the phagocytic function of microglia and exhibits anti-inflammatory activity. In Alzheimer's disease (AD) mouse models, 15(R)-Lipoxin A4 improves AD-like pathology. 15(R)-Lipoxin A4 holds potential for use in inflammation and neurodegenerative disease research .
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-
- HY-173047
-
|
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Ras
ERK
|
Cancer
|
|
KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS G12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .
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- HY-164503
-
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NEP010
|
EGFR
|
Cancer
|
|
Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR wt, EGFR L858R/T790M, EGFR L858R and EGFR T790M, respectively .
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-
- HY-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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- HY-P10786
-
|
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Transmembrane Glycoprotein
|
Cancer
|
|
LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
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- HY-164411
-
|
|
c-Met/HGFR
|
Cancer
|
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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- HY-121663
-
|
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Dengue Virus
|
Infection
|
|
ST-148 is a novel small molecule compound that has potent inhibitory effects against all four dengue virus serotypes. In the nonlethal AG129 mouse dengue virus infection model, ST-148 significantly reduced viremia and viral load in vital organs and tended to reduce plasma cytokine levels. Compound resistance was associated with the dengue virus capsid (C) gene, and the direct interaction of ST-148 with the C protein was presumed to be achieved through the protein's built-in fluorescence change in the presence of the compound. Therefore, ST-148 appears to interact with the dengue virus C protein and inhibit one or more unique steps of the viral replication cycle.
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- HY-159179
-
|
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Integrin
|
Inflammation/Immunology
|
|
α4 integrin receptor antagonist 3 (Compound 11) is an orally active α4integrin receptor antagonist. α4 integrin receptor antagonist 3 can inhibit the adhesion of K562 cells mediated by the interaction between α4β1/VCAM-1 and α4β7/MAdCAM-1, with IC50 values of 130 nM and 2 nM, respectively. α4 integrin receptor antagonist 3 has the potential to be used in the study of dextran sulfate sodium (DSS) colitis mouse model .
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- HY-161769
-
|
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PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
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-
- HY-173060
-
|
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ERK
Apoptosis
Autophagy
|
Cancer
|
|
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
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-
- HY-147081
-
|
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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-
- HY-P991461
-
|
XmAb968
|
CD38
|
Cancer
|
|
AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .
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-
- HY-150613
-
|
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Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
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-
- HY-161988
-
|
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Bacterial
|
Infection
Inflammation/Immunology
|
|
Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300 .
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-
- HY-125327
-
|
|
SGLT
|
Metabolic Disease
|
|
YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.
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- HY-143881
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-173059
-
|
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CDK
|
Cancer
|
|
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
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-
- HY-161615
-
|
|
Apoptosis
PROTACs
|
Cancer
|
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PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
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- HY-173039
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Microtubule/Tubulin
Keap1-Nrf2
Reactive Oxygen Species
Apoptosis
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Cancer
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α-Tubulin polymerization-IN-1 (Compound 8l) is an inhibitor for α-Tubulin polymerization. α-Tubulin polymerization-IN-1 modulates the NRF2/KEAP-1 signaling pathway, induces ROS generation in PC-3 cell, thereby inducing apoptosis in PC-3. α-Tubulin polymerization-IN-1 inhibits the proliferation of PC-3 cell with a GI50 of 0.17 µM, arrests the cell cycle at G2/M phase. α-Tubulin polymerization-IN-1 exhibits antitumor efficacy in mouse model .
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- HY-163691
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Carbonic Anhydrase
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Cancer
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Antitumor agent-163 (Compound 3) is a photosensitizer used in Molecular-Targeted Photodynamic Therapy (MT-PDT) targeting carbonic anhydrase IX (CAIX). Antitumor agent-163 inactivates CAIX protein via singlet oxygen under 540 nm wavelength light, without affecting internal standard proteins such as α-tubulin, β-actin, and proliferating cell nuclear antigen (PCNA). Antitumor agent-163 induces cell membrane damage, inhibits cell viability (IC50 is 0.2 and 0.05 μM for A549 and U87MG). Antitumor agent-163 exhibits antitumor efficacy in mouse model .
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- HY-168725
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PROTACs
Kinesin
Apoptosis
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Cancer
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PROTAC KSP-IN-1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP-IN-1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP-IN-1 exhibits antitumor efficacy in mouse model . (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
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- HY-156438
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NOD-like Receptor (NLR)
Interleukin Related
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Neurological Disease
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NT-0796 is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. NT-0796 inhibits IL-1β release in human PBMC cells with an IC50 value of 0.32 nM. NT-0796 is an isopropyl ester that undergoes intracellular conversion to NDT-19795, the carboxylic acid active species. NT-0796 reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. NT-0796 is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis .
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- HY-124832
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Caspase
Amyloid-β
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Neurological Disease
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δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
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- HY-163982
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NF-κB
FOXO
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Inflammation/Immunology
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FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
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- HY-P10393
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ERα (295-311)
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Apoptosis
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Cancer
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ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-162972
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PROTACs
PD-1/PD-L1
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Cancer
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PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model .
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- HY-W017540
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ATP Synthase
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
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Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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- HY-168936
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
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- HY-144088
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HPK1-IN-22
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MAP4K
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Inflammation/Immunology
Cancer
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ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
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- HY-161785
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Apoptosis
EGFR
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Cancer
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EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
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- HY-150609
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SHP2
Phosphatase
CDK
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Cancer
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SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
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- HY-N0507R
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TNF Receptor
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-121081
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CDK
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Cancer
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BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
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- HY-153830
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C16 Lactosylceramide (d18:1/16:0)
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Endogenous Metabolite
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Neurological Disease
Metabolic Disease
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LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
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- HY-168714
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Microtubule/Tubulin
Apoptosis
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Cancer
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Microtubule inhibitor 12 (Compound 2k) is an inhibitor for microtubule polymerization with an IC50 of 22.23 μM. Microtubule inhibitor 12 arrests the cell cycle of B16-F10 at G2/M phase, induces apoptosis in B16-F10, and inhibits cell migration. Microtubule inhibitor 12 inhibits the proliferation of cancer cells B16-f10, A549, HepG2 and MCF-7, with IC50s of 0.098, 0.135, 0.109, and 0.259 μM, respectively. Microtubule inhibitor 12 exhibits antitumor efficacy in mouse model .
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- HY-160777
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Galeterone 3β-imidazole
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Molecular Glues
Androgen Receptor
MNK
Apoptosis
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Cancer
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VNPP433-3β (Galeterone 3β-imidazole) is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2.VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
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- HY-172217
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DNA Methyltransferase
Apoptosis
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Cancer
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DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
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- HY-172258
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5-HT Receptor
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Cancer
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5-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. 5-HT2B antagonist-2 can downregulate the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, and significantly reduce the deposition of fibrosis, thereby reducing the fibrotic area and inhibiting the fibrotic process in CCl4-induced liver fibrosis mouse models. 5-HT2B antagonist-2 can be used in the study of immune inflammatory-related diseases, particularly in the research of pulmonary fibrosis diseases .
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- HY-151411
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RUNX
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Cancer
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RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model .
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- HY-168715
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SHP2
Apoptosis
MAPKAPK2 (MK2)
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Cancer
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SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
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- HY-16622A
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LPL Receptor
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Others
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GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
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- HY-168574
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PROTACs
Sirtuin
Apoptosis
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Cancer
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SZU-B6 is a PROTAC degrader for SIRT6 with DC50 of 45 nM and 154 nM in cell SK-HEP-1 and Huh-7. SZU-B6 inhibits the proliferation of cell SK-HEP-1 with an IC50 of 1.51 μM, inhibits the colony formation of SK-HEP-1 and Huh-7, induces apoptosis and arrests the cell cycle at G2/M phase in SK-HEP-1. SZU-B6 exhibits antitumor efficacy in mouse model. (Pink: ligand for target protein (HY-16605); Black: linker (HY-W012935); BLue: ligand for E3 ligase (HY-W453548)
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- HY-169006
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Apoptosis
PKC
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Cancer
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Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
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- HY-157228
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PROTACs
Ras
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Cancer
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ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
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- HY-168135
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PROTACs
c-Met/HGFR
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Cancer
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PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models . (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
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- HY-118243
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Amyloid-β
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Others
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KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
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- HY-169001
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5-HT Receptor
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Neurological Disease
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5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .
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- HY-156110
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Insulin Receptor
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Cancer
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IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
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- HY-167939
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Adrenergic Receptor
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Inflammation/Immunology
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(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
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- HY-126969
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PPAR
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Metabolic Disease
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C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
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- HY-158726
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Fluorescent Dye
Apoptosis
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Cancer
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Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model .
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- HY-170968
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EGFR
Apoptosis
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Cancer
|
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EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
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- HY-156296
-
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CDK
Apoptosis
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Cancer
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CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .
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- HY-172200
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PD-1/PD-L1
HDAC
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Cancer
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PD-L1/HDAC6-IN-1 (Compound HP29) is the inhibitor for PD-L1 and HDAC6 that inhibits the PD-L1/PD-1 interaction and HDAC6 with an IC50 of 26.8 nM and 69 nM. PD-L1/HDAC6-IN-1 enhances the killing ability of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. PD-L1/HDAC6-IN-1 exhibits good pharmacokinetics characteristics in rats with a drug exposure of 871.62 ng·h/mL, and exhibits antitumor activity in mouse B16-F10 xenograft models .
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- HY-173147
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CDK
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Cancer
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CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer .
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- HY-120974
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GLUT
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Metabolic Disease
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α-Lipoic Acid Derivative 1 (Compound AN-7) is an α-lipoic acid derivative that enhances glucose transport in skeletal muscle by releasing active α-lipoic acid (LA), significantly improving glucose metabolism. In L6 skeletal muscle cells, α-Lipoic Acid Derivative 1 significantly increases glucose transport rates, approximately 12 times more potent than the parent compound α-lipoic acid (HY-N0492). In a mild diabetic mouse model, 10 mg/kg of α-Lipoic Acid Derivative 1 administered for two weeks significantly reduced blood glucose levels by 39%. α-Lipoic Acid Derivative 1 shows significant potential in research related to glucose metabolism in diabetes .
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- HY-159912
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YAP
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Cancer
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pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
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- HY-N0538
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Xylite
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Autophagy
Endogenous Metabolite
Bacterial
Atg7
Atg8/LC3
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Metabolic Disease
Cancer
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Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-N0469R
-
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Endogenous Metabolite
Virus Protease
HSV
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Infection
Metabolic Disease
Inflammation/Immunology
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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- HY-170522
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HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
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ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases .
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- HY-168954
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c-Fms
Apoptosis
Akt
ERK
STAT
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Inflammation/Immunology
Cancer
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CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22% .
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- HY-168204
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Bacterial
Fungal
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Infection
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3-Acetyl-28-N–(3–guanidinobutoxy)-oleanolic acid (compound J1) is a potent antimicrobial agent. 3-Acetyl-28-N–(3–guanidinobutoxy)-oleanolic acid shows anti-gram-positive bacteria and fungi activity. 3-Acetyl-28-N–(3–guanidinobutoxy)-oleanolic acid can be used as antibiotic adjuvants. 3-Acetyl-28-N–(3–guanidinobutoxy)-oleanolic disrupts the bacterial cell membrane, inserts into the DNA, and binds to DNA gyrase. 3-Acetyl-28-N–(3–guanidinobutoxy)-oleanolic reduces microbial count in a mouse MRSA skin infection model and accelerates wound healing .
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- HY-161577
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Bcl-2 Family
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Cancer
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BFC1103 is a small-molecule compound whose primary mechanism of action involves interaction with a specific domain of Bcl-2, particularly its loop domain. This interaction induces a conformational change in Bcl-2, exposing its BH3 (Bcl-2 homology 3) domain, thereby switching Bcl-2's function from anti-apoptotic to pro-apoptotic. The cell death induced by BFC1103 is dependent on the presence of Bax or Bak, both of which are key proteins involved in the intrinsic apoptotic pathway mediated by mitochondria. BFC1103 has successfully inhibited lung metastasis of triple-negative breast cancer in mouse models. It can be utilized in studying the roles of Bcl-2 family proteins in cancer development and how they impact the survival and proliferation of cancer cells .
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- HY-116062A
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Histone Methyltransferase
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Neurological Disease
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JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
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- HY-158029
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PI3K
Apoptosis
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Cancer
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PI3Kα-IN-21 (compound 8) is a PI3Kα inhibitor, and its selectivity for PI3Kα is 10.41/16.99/37.53 times higher than PI3Kβ/γ/δ respectively (IC50: 96.89/568.24/397.48 nM ). PI3Kα-IN-21 inhibits cancer cell activity, proliferation, and migration, and induces mitochondrial apoptosis through the PI3K/Akt/mTOR pathway. PI3Kα-IN-21 exhibits in vivo antitumor potency in a mouse model of non-small cell lung cancer .
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- HY-W738639
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18-OH-DOC; 11-Deoxy-18-hydroxycorticosterone
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Melanocortin Receptor
Angiotensin Receptor
Drug Metabolite
Mineralocorticoid Receptor
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Cardiovascular Disease
Metabolic Disease
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18-Hydroxy-11-deoxy corticosterone (18-OH-DOC) is a mineralocorticoid whose synthesis is regulated by adrenocorticotropic hormone (ACTH) and angiotensin II.
18-Hydroxy-11-deoxy corticosterone is an intermediate in the metabolism of progesterone and plays an important role in regulating blood pressure and water-salt balance. Continuous infusion of
18-Hydroxy-11-deoxy corticosterone can increase systolic blood pressure in rats, and plasma levels of
18-Hydroxy-11-deoxy corticosterone are significantly elevated in the db/db mouse model of type 2 diabetes, suggesting its potential involvement in metabolic dysregulation and diabetes-related regulation.
18-Hydroxy-11-deoxy corticosterone holds promise for research in areas such as hypertension, diabetes, and other related fields .
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- HY-169938
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HDAC
Histone Demethylase
Apoptosis
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Cancer
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LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
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- HY-173033
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Constitutive Androstane Receptor
Cytochrome P450
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Metabolic Disease
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MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .
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- HY-129602
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SD-36
5 Publications Verification
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PROTACs
STAT
Apoptosis
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Cancer
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SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-156096
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HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
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Cancer
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HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
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- HY-168971
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CP-25
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IFNAR
STAT
TNF Receptor
Interleukin Related
CXCR
JAK
G Protein-coupled Receptor Kinase (GRK)
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Inflammation/Immunology
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Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model .
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- HY-170978
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PROTACs
CDK
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Cancer
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PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
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- HY-P99395
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JNJ 56022473; CSL 362
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Interleukin Related
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Cancer
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Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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- HY-163913
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SARS-CoV
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Infection
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SARS-CoV-IN-5 (compound 49) is a highly selective, nonpeptidic and noncovalent 3CL pro inhibitor with IC50s of 38 nM, 21.1 nM and 86 nM for 3CL pro of SARS-CoV-1, SARS-CoV-2, Bat coronavirus WIV1, respectively. SARS-CoV-IN-5 inhibits the replication of the SARS-CoV-2 delta variant with an EC50 of 0.272 μM. SARS-CoV-IN-5 significantly reduces the lung viral copies in a K18-hACE2 transgenic mouse model. SARS-CoV-IN-5 has good target-specific and potential broad-spectrum anticoronavirus activities against SARS-CoV-1, WIV1, MERS, HCoV-OC43, HCoV-229E, and HKU9 .
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- HY-170524
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SARS-CoV
DNA Methyltransferase
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Infection
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TDI-015051 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 ≤0.15 nM. TDI-015051 inhibits SARS-CoV-2 NSP14 in Huh-7.5 cell (EC50=11.4 nM) and in ACE2-TMPRSS2 expressing A549 cell (EC50=64.7 nM). TDI-015051 also inhibits other coronaviruses like α-hCoV-NL63, α-hCoV-229E and β-hCoV-MERS with IC50s of 1.7, 2.6 and 3.6 nM, respectively. TDI-015051 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and viral replication, and exhibits anti-infectious activity in mouse models .
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- HY-169363
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PD-1/PD-L1
Autophagy
AUTACs
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Cancer
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PD-L1 degrader-2 (Compound B3) is an orally active AUTAC degrader, that degrades PD-L1 through autophagy-lysosome pathway with a DC50 of 0.5 μM. PD-L1 degrader-2 exhibits inhibitory activity against PD-1/PD-L1 interaction with an IC50 of 22.8 nM. PD-L1 degrader-2 upregulates the expressions of Atg9b, Lamp1 and Mitf, and activates the autophagy lysosome system. PD-L1 degrader- exhibits antitumor efficacy in CT26 mouse model . (Pink: autophagy-lysosome activator (HY-159894); Black: linker (HY-W015088); Blue: PD-L1 ligand (HY-169365))
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- HY-159122
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Carbonic Anhydrase
Reactive Oxygen Species
Apoptosis
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Cancer
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CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
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- HY-159922
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Androgen Receptor
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Cancer
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AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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- HY-163709
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PROTACs
FAK
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Cancer
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PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
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- HY-170928
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EGFR
Anaplastic lymphoma kinase (ALK)
Cytochrome P450
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Cancer
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DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
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- HY-169262
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Phospholipase
Apoptosis
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Cancer
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PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
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- HY-170852
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PROTACs
RET
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Cancer
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QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) .
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- HY-174086
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Glutathione Peroxidase
Ferroptosis
ROS Kinase
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Cancer
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PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)) .
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- HY-163985
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PROTACs
FGFR
Apoptosis
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Cancer
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PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
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- HY-154974
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Liposome
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Cancer
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LNP Lipid-8 (11-A-M) is an ionizable single-tail multi-head lipid that can be used as a lipid nanoparticle (LNP) to deliver siRNA to T cells without targeting ligands. LNP Lipid-8 is more selective for T cells than other cell types such as hepatocytes. LNP Lipid-8 selectively delivers siRNA/sgRNA to T cells (especially CD8 + T cells) through endogenous lipid transport pathways, and can enter cells and release RNA through endocytosis to achieve gene silencing. LNP Lipid-8 loaded with GFP siRNA (siGFP) significantly led to GFP gene silencing in mouse models. LNP Lipid-8 showed good efficacy and safety in both cells and animals, without obvious liver targeting and toxicity. LNP Lipid-8 can be used for RNA delivery research in the fields of tumor immunotherapy and T cell-mediated autoimmune diseases .
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- HY-W587743
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AMK hydrochloride
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Prostaglandin Receptor
PGE synthase
COX
Reactive Oxygen Species
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Neurological Disease
Metabolic Disease
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N1-Acetyl-5-methoxykynuramine (AMK) hydrochloride is an active metabolite of the neurohormone melatonin (HY-B0075). N1-Acetyl-5-methoxykynuramine hydrochloride (200 µM) effectively scavenges singlet oxygen (ROS).1 It also inhibits the production of prostaglandin E2 (PGE2) and prostaglandin D2 (PGD2) induced by epinephrine and arachidonic acid in a concentration- and time-dependent manner, and suppresses the increase in COX-2 levels induced by LPS (HY-D1056) in RAW 264.7 macrophages at a concentration of 500 µM. In a mouse model of Parkinson's disease induced by MPTP (HY-15608), N1-Acetyl-5-methoxykynuramine hydrochloride (20 mg/kg) reduces the increase in lipid peroxidation in the cytosol and mitochondria of the substantia nigra and striatum. N1-Acetyl-5-methoxykynuramine hydrochloride can be used in research on metabolic and neurological diseases
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- HY-136765
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PI3K
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Cancer
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PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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- HY-159803
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6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin
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Endogenous Metabolite
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Cancer
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IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
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- HY-170329
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PROTACs
Androgen Receptor
Apoptosis
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Cancer
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PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model . (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))
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- HY-173077
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PD-1/PD-L1
Bacterial
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Infection
Inflammation/Immunology
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PD-L1/LpxC-IN-1 (Conpound 12b) is the inhibitor for PD-L1 and LpxC with IC50 of 5.2 μM and 0.081 μM. PD-L1/LpxC-IN-1 inhibits the biosynthesis of bacterial lipopolysaccharide, causes the lysis and death of bacterial cells. PD-L1/LpxC-IN-1 inhibits Gram-negative bacteria, MIC for K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028 and P. aeruginosa ATCC 9027 is 0.25-0.5 μg/mL. PD-L1/LpxC-IN-1 downregulates the expression of inflammatory factors IL-2 and IFN-γ, upregulates the expression of CD4+ and CD8+ cells, thereby activating the immune system and inhibiting excessive inflammatory responses. PD-L1/LpxC-IN-1 exhibits antibacterial activity in K. pneumoniae ATCC 13883 infected mouse models .
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- HY-W050154
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Parasite
Tyrosinase
NF-κB
CDK
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Infection
Inflammation/Immunology
Cancer
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Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity .
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- HY-W050154R
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Parasite
Tyrosinase
NF-κB
CDK
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Infection
Inflammation/Immunology
Cancer
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Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .
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- HY-173148
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SARS-CoV
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Infection
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TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-156466
-
|
|
STAT
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC50=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC50=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE) .
|
-
- HY-162812
-
|
|
Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
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-
- HY-B2167R
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
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-
-
-
HY-L217
-
|
|
334 compounds
|
|
Metabolic abnormalities lead to dysfunction of metabolic pathways and the accumulation or lack of metabolites, which are recognized hallmarks of the disease. The metabolite signature is closely related to the disease phenotype and is very useful for predicting the diagnosis and prognosis of the disease as well as monitoring treatment. Metabolites can be used as disease markers for diagnostic therapy. As the classic model of disease experiment in vivo, mice metabolites also play a role in disease diagnosis and mechanism research.
MCE provides 334 mouse metabolites that can be used in disease research.
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| Cat. No. |
Product Name |
Type |
-
- HY-D2376
-
|
|
Dyes
|
|
BH-Vis is a two-photon fluorescent probe that inhibits cell plasma membrane (CPM). BH-Vis has great potential to accurately identify pyroptosis at the cellular level during AAA development in the mouse abdominal aortic aneurysm AAA model .
|
-
- HY-D2620
-
|
|
Fluorescent Dyes/Probes
|
|
CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC50 of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models .
|
-
- HY-158726
-
|
|
Fluorescent Dyes/Probes
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model .
|
| Cat. No. |
Product Name |
Type |
-
- HY-114360A
-
|
|
Biochemical Assay Reagents
|
|
Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
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-
- HY-N0830B
-
|
|
Cell Assay Reagents
|
|
Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
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-
- HY-145405
-
|
|
Drug Delivery
|
|
C12-200 is a type of ionizable cationic lipid and helper lipid commonly used for mRNA delivery. In the hemophilia B mouse model, mRNA encoding human erythropoietin (EPO) and coagulation factor IX (FIX) can be successfully delivered and expressed using C12-200. C12-200 is utilized in research related to hemophilia B .
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-
- HY-113058
-
|
|
Biochemical Assay Reagents
|
|
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
|
-
- HY-131420
-
|
Aseanostatin P1; Isotetradecanoic acid
|
Drug Delivery
|
|
12-Methyltridecanoic acid is a methylated fatty acid that has been found in milk. 12-Methyltridecanoic acid (200 μM) reduces angiogenesis and corneal opacity in alkaline or Pseudomonas aeruginosa-induced ocular mouse models.
|
-
- HY-W127408
-
|
|
Drug Delivery
|
|
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P4253A
-
|
|
VEGFR
|
Cardiovascular Disease
|
|
Arginyl-Glutamine TFA is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy .
|
-
- HY-156430
-
|
|
MMP
|
Cancer
|
|
MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
|
-
- HY-156002
-
|
Paluratide
|
Ras
ERK
|
Cancer
|
|
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
|
-
- HY-145237
-
BM213
1 Publications Verification
|
Complement System
|
Cancer
|
|
BM213, a potent and selective agonist for C5aR1, shows antitumor activity in a mouse model of mammary carcinoma.
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-
- HY-P2464
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Myosin H Chain Fragment, mouse is a fragment of the α-Myosin heavy chain peptide. Myosin H Chain Fragment can be used to induce experimental autoimmune myocarditis (EAM) mouse model .
|
-
- HY-P3163
-
|
|
PPAR
Collagen
SOD
|
Inflammation/Immunology
|
|
Hexapeptide-9 is a signaling peptide. Hexapeptide-9 can promote collagen production. Hexapeptide-9 has anti-aging activity, and can be used in cosmetic research .
|
-
- HY-P3350
-
|
|
Bacterial
|
Infection
|
|
LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
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-
- HY-P5183
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Hm1a is a disulfide-rich spider-venom peptide, and a NaV1.1 activator. Hm1a restores the function of inhibitory interneurons in Dravet syndrome (DS) mouse model .
|
-
- HY-P4253
-
|
|
VEGFR
|
Cardiovascular Disease
|
|
Arginyl-Glutamine is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy .
|
-
- HY-P2464A
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Myosin H Chain Fragment, mouse acetate salt is a fragment of the α-Myosin heavy chain peptide. Myosin H Chain Fragment can be used to induce experimental autoimmune myocarditis (EAM) mouse model .
|
-
- HY-P1727
-
|
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P1727A
-
|
|
YAP
|
Cancer
|
|
Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P2287
-
|
|
CRFR
|
Neurological Disease
|
|
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an EC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive agent in the mouse model .
|
-
- HY-P1787
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (4-10) is an epitope for the polyclonal anti-Aβ(1-42) antibody, reduces amyloid deposition in a transgenic Alzheimer disease mouse model .
|
-
- HY-P10850
-
|
|
TNF Receptor
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model .
|
-
- HY-P4866
-
|
|
Peptides
|
Metabolic Disease
|
|
Q-Peptide is the angiopoietin-1 derived peptide (QHREDGS).Q-Peptide increases keratinocyte migration to improve wound healing, in diabetic mouse model. Q-Peptide accelerates wound closure .
|
-
- HY-P3341
-
-
- HY-W096171
-
|
3-Hydroxy-D-tyrosine
|
Carboxypeptidase
|
Neurological Disease
|
|
D-Dopa is a non-competitive, allosteric inhibitor for glutamate carboxypeptidase II (GCPII) with an IC50 of 200 nM. D-Dopa exhibits good pharmacokinetic characteristics, and low blood-brain barrier permeability in mouse model .
|
-
- HY-P5907
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-P5462A
-
|
|
Peptides
|
Inflammation/Immunology
|
|
PLP (180-199) TFA is the TFA salt form of PLP (180-199) (HY-P5462). PLP (180-199) TFA induces the activation and differentiation of T cells, and induces the experimental autoimmune encephalomyelitis (EAE) in mouse model .
|
-
- HY-P1728
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P10432
-
|
|
Formyl Peptide Receptor (FPR)
|
Others
Inflammation/Immunology
|
|
SHAAGtide is a FPRL1 activator. SHAAGtide has anti-inflammatory activity, mediates its biological activity via FPR2 and is used to reduce the expression of inflammatory cytokines in mouse models. SHAAGtide can be used in the study of diseases such as lung inflammation and fibrosis .
|
-
- HY-P10914
-
|
|
MDM-2/p53
Autophagy
|
Inflammation/Immunology
Cancer
|
|
D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
|
-
- HY-P10435
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
KEMPFPKYPVEP is a 12-amino acids neuropeptide, which upregulates levels of dopamine (DA) and norepinephrine (NE) in the prefrontal cortex, exhibits spatial and object recognition memory promoting ability in Scopolamine (HY-N0296)-induced amnesia mouse model .
|
-
- HY-P1728A
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P1120
-
|
|
Formyl Peptide Receptor (FPR)
PERK
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
WKYMVm is a selective formylpeptide receptor 2 (FPR2) agonist. WKYMVm has a powerful anti-inflammatory effect that can reduce lung injury and spinal cord injury. WKYMVm ameliorates obesity by regulating lipid metabolism and leptin signaling. WKYMVm is involved in the regulation of immune cells by activating FPRs. WKYMVm can promote the chemotactic migration of immune cells and inhibit the apoptosis of phagocytes. In addition, WKYMVm may play a favorable or unfavorable role in tumors, depending on the type of tumor .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613); EP-100
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P10414A
-
|
KP1 (human) hydrochloride
|
TGF-beta/Smad
p38 MAPK
|
Inflammation/Immunology
|
|
Klotho-derived peptide 1 (KP1 human) hydrochloride blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
|
-
- HY-P10414
-
|
KP1 (human)
|
TGF-beta/Smad
p38 MAPK
|
Inflammation/Immunology
|
|
Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
|
-
- HY-P10019
-
|
|
GCGR
|
Neurological Disease
|
|
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
|
-
- HY-P2032
-
|
|
Endogenous Metabolite
|
Infection
Cancer
|
|
Cyclochlorotine is a mycotoxin that can be extracted from the yellow rice infectant Penicillium islandicum Sopp. Cyclochlorotine promotes glycogenolysis, inhibits glycogen synthesis, affects fat synthesis and protein synthesis in liver cells. Cyclochlorotine exhibits chronic toxicity in liver that induces liver fibrosis and cirrhosis in mouse models. Cyclochlorotine exhibits carcinogenicity .
|
-
- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
|
-
- HY-P1709
-
|
|
Bacterial
|
Infection
|
|
Protactin is a pentapeptide lactone produced by Streptomyces cucumeris strain L703-4 (ATCC 53784) with significant antioxidant properties. Protactin can be converted to actinomycin Zp by ferrocyanide oxidation. Actinomycin Zp exhibits potent antibacterial activity in vitro and has significant antitumor effects against P-388 leukemia in a mouse model .
|
-
- HY-P3291
-
|
ZP7570
|
GCGR
|
Metabolic Disease
|
|
Dapiglutide (ZP7570) is a long-acting glucagon-like peptide-1 receptor 1R (GLP-1R)/Glucagon-like peptide-2 receptor (GLP-2R) dual agonist. Dapiglutide alleviates intestinal dysfunction in a mouse short bowel model and has anti-obesity effects .
|
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
|
-
- HY-P10360
-
|
|
α-synuclein
|
Neurological Disease
|
|
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .
|
-
- HY-P10559
-
|
|
Bacterial
|
Infection
|
|
(RXR)4XB is a cell-penetrating peptide, that binds the phosphorodiamidate morpholino oligomers (PMOs), forms peptide-conjugated PMOs (PPMOs), and improves the delivery of PMO into bacterial cells. (RXR)4XB-PMO conjugate prevents the formation of biofilms, inhibits Pseudomonas aeruginosa with MIC50 of 0.5 to 16 μM, and reduces the bacterial burden in mouse acute pneumonia models .
|
-
- HY-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-P10492
-
|
|
Peptides
|
Others
Metabolic Disease
|
|
Tregitope 289 is a peptide derived from the Fc region of immunoglobulin G (IgG) and is a highly conserved T cell epitope that stimulates the expansion of natural regulatory T cells. Co-delivery of Tregitope 289 with type 1 diabetes (T1D) antigens delays the development of hyperglycemia and reduces the incidence of diabetes in the NOD mouse model. Tregitope 289 can be used to study T1D and other autoimmune diseases .
|
-
- HY-P10826
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1 inhibitory peptide C8 is inhibits PD-1/PD-L1 interaction, promotes the activation of CD8+ and CD4+ T cells, and increases the IFN-γ secretion. PD-1/PD-L1 inhibitory peptide C8 exhibits antitumor efficacy in mouse model .
|
-
- HY-P10913
-
|
|
Bacterial
|
Infection
|
|
HYNIC-UBI29-41 is composed of a bifunctional chelator HYNIC and an antimicrobial peptide UBI 29-41. HYNIC-UBI29-41 retains the antibacterial properties of UBI 29-41, and exhibits good affinity to Gram-positive and Gram-negative bacteria. HYNIC-UBI29-41 can be used as an imaging agent for bacterial infection detection in mouse models, when labeled with the radioactive element technetium (99mTc) .
|
-
- HY-P10439
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
CVRARTR is a programmed cell death ligand-1 (PD-L1) antagonist with a KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and T cell proliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model. CVRARTR can be used in melanoma research .
|
-
- HY-P1416
-
Foxy-5
Maximum Cited Publications
6 Publications Verification
|
Wnt
|
Cancer
|
|
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-P10872
-
|
|
SARS-CoV
|
Infection
|
|
P315V3 is an pan inhibitor for coronavirus, that inhibits SARS-CoV-2 prototypePT, Delta, BA.1 and BA.4 strain with IC50s of 10.9, 8.9, 8.6, and 2.7 nM. P315V3 exhibits cytotoxicity in Vero cell with CC50 of 4.3 μM. P315V3 exhibits anti-infectious efficacy in mouse models .
|
-
- HY-P1416A
-
Foxy-5 TFA
Maximum Cited Publications
6 Publications Verification
|
Wnt
|
Cancer
|
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-P10947
-
|
|
Epigenetic Reader Domain
YAP
|
Cancer
|
|
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
|
- HY-P10415
-
|
hSA(408–423) peptide
|
CXCR
|
Infection
Inflammation/Immunology
Cancer
|
|
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
|
- HY-P5396
-
|
|
Amino Acid Decarboxylase
|
Others
|
|
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
|
- HY-P10870
-
|
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
|
- HY-P10744
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
- HY-P10786
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
|
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-K6008
-
1 Publications Verification
|
|
MCE Basement Membrane Matrix HC (High Concentration) is primarily composed of natural basement membrane matrix extracted from mouse tumors, with higher content of various cytokines than the standard type.This product is mainly used for angiogenesis experiments, construction of animal models and 3D tumor models.
|
-
- HY-K6005
-
|
|
|
MCE Basement Membrane Matrix HC (High Concentration, Phenol Red) is primarily composed of natural basement membrane matrix extracted from mouse tumors, with higher content of various cytokines than the standard type.This product is mainly used for angiogenesis experiments, construction of animal models and 3D tumor models.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99590A
-
|
RAP-011
|
TGF-beta/Smad
|
Cardiovascular Disease
|
|
Sotatercept (mIgG2a) has direct cardioprotective actions, which reduces right ventricular (RV) remodeling and improves function in a pulmonary artery banding (PAB) mouse model .
|
-
- HY-P99351
-
|
Anti-MMP9 Reference Antibody (andecaliximab)
|
MMP
|
Cancer
|
|
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-P99604
-
|
AZD-1061; COV2-2130
|
SARS-CoV
|
Infection
|
|
Cilgavimab (AZD-1061; COV2-2130) is a human SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-P991456
-
|
|
Mesothelin
|
Cancer
|
|
LMB-100 is a human immunotoxin targeting MSLN/Mesothelin. LMB-100 induces systemic inflammation and CD8 T cell recruitment. LMB-100 enhances the antitumor effects of anti-PD-1 antibodies in a human peripheral blood mononuclear cell transplanted mesothelioma mouse model and a syngeneic lung adenocarcinoma mouse model expressing human mesothelin. LMB-100 can be used in mesothelioma research. Recommended isotype control: Fab fused with a fragment of Pseudomonas exotoxin A .
|
-
- HY-P991380
-
|
|
Transferrin Receptor
|
Neurological Disease
|
|
TXB4 is a brain-permeable human monoclonal antibody (mAb) targeting CD71. TXB4 prevents 6-OHDA-induced death of TH-positive neurons in the SNc in a 6-OHDA mouse model of Parkinson's disease (PD). TXB4 can be used in neurodegenerative diseases, acute brain and spinal cord injury, and depression research .
|
-
- HY-P991307
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
BND-35 is a human monoclonal antibody (mAb) targeting LILRB4/ILT3/CD85k. BND-35 blocks the interaction of ILT3 with APOE and fibronectin, enhances the pro-inflammatory activity of various myeloid cells, and reverses ILT3-mediated immunosuppression of T cells by various suppressive myeloid cells. BND-35 has anti-tumor activity in the hILT3 transgenic mouse tumor model .
|
-
- HY-P99578
-
|
HL036337; HBM9036
|
TNF Receptor
|
Inflammation/Immunology
|
|
Tanfanercept (HL036337) is an TNF-α receptor fusion protein that targets TNF-α. Tanfanercept is effective in ameliorating corneal erosions in a dry eye (DE) mouse model .
|
-
- HY-P991230
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
MK-4830 is a fully humanized monoclonal antibody of the immunoglobulin G4 subclass that specifically binds to ILT4 and blocks its interaction with HLA-G and other ligands. MK-4830 inhibits tumor growth in humanized mouse cancer models .
|
-
- HY-P991310
-
|
LT3015; LT-3000
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Lpathomab (LT3015; LT-3000) is a human IgG1 monoclonal antibody (mAb) targeting LPA. Lpathomab reduces the release of IL-8 and IL-6 cytokines in SKOV3 cells and blocks LPA-triggered tumor cell migration. Lpathomab reduces neovascularization in Matrigel plug and CNV models. Lpathomab inhibits brain injury in the CCI mouse model. Lpathomab can be used in the study of brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P991464
-
|
|
TNF Receptor
|
Cancer
|
|
IBI37G5 is a human monoclonal antibody (mAb) targeting TNFRSF18/GITR/CD357. IBI37G5 has anti-tumor activity in MC38 and B16F10 mouse tumor models. IBI37G5 can be used in the study of cancer immunity .
|
-
- HY-P991455
-
|
|
TNF Receptor
|
Cancer
|
|
PTX-35 is a human IgG monoclonal antibody (mAb) targeting TNFRSF25. PTX-35 reduces the suppressive activity of regulatory T cells and enhances CD4+ T cell effector responses in a mouse melanoma model. PTX-35 can be used in Islet cell transplant rejection and Solid tumours research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P991481
-
|
|
CCR
|
Cancer
|
|
S-531011 is a human IgG1 monoclonal antibody (mAb) targeting CCR8. S-531011 reduces tumor-infiltrating CCR8+ Tregs and has anti-tumor activity in CT26.WT and EMT6 tumor-bearing mouse tumor models. S-531011 can be used in the study of cancer immunity. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-P99056
-
|
PF 05082566
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Utomilumab (PF 05082566) is a fully human IgG2 agonist monoclonal antibody that selectively binds to 4-1BB/CD137. Utomilumab can be used in the research of tumors such as follicular and other CD20 + non-Hodgkin lymphomas .
|
-
- HY-P991233
-
|
|
EGFR
|
Cancer
|
|
BAT1006 is a monoclonal antibody targeting HER2 extracellular domain II with enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) for the study of HER2-positive locally advanced/metastatic solid tumors. BAT1006 has an approximately 5-fold enhanced ADCC effect compared to pertuzumab (HY-P9912) and exhibits potent anti-tumor activity in the HER2-positive Calu-3 xenograft mouse model .
|
-
- HY-P990025
-
|
ARGX-117
|
Complement System
|
Inflammation/Immunology
|
|
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .
|
-
- HY-P991328
-
|
|
Notch
|
Cancer
|
|
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
|
-
- HY-P99667
-
|
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
|
-
- HY-P99116
-
|
RG7716
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
|
-
- HY-P991461
-
|
XmAb968
|
CD38
|
Cancer
|
|
AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-123033C
-
-
- HY-N0656
-
-
- HY-N0421R
-
|
|
Structural Classification
Animals
Source classification
Steroids
|
Apoptosis
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-N12044
-
-
- HY-107811
-
-
- HY-163001
-
|
|
Microorganisms
Source classification
|
Autophagy
p62
Atg8/LC3
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-N11499
-
-
- HY-113365
-
-
- HY-N14354
-
|
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Antibiotic
Bacterial
|
|
Ferrocin B is an iron-containing cyclic decapeptide antibiotic found in the bacterium Pseudomonas fluorescens YK-310, exhibiting strong antibacterial activity primarily against Gram-negative bacteria, with particularly potent inhibitory effects on Pseudomonas aeruginosa. In a mouse infection model, Ferrocin B shows a half effective dose (ED50) of 0.593 mg/kg against P. aeruginosa. Ferrocin B holds potential for research in the field of anti-infective therapies .
|
-
- HY-N0747
-
-
- HY-B1864AR
-
-
- HY-123033AR
-
|
|
Alkaloids
Structural Classification
Animals
Source classification
Pyridine Alkaloids
|
Sirtuin
Endogenous Metabolite
|
|
Nicotinamide riboside (chloride) (Standard) is the analytical standard of Nicotinamide riboside (chloride). This product is intended for research and analytical applications. Nicotinamide riboside Chloride, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
|
-
- HY-Y0546
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
|
Endogenous Metabolite
Photosensitizer
|
|
Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-N14035
-
|
|
Structural Classification
Natural Products
Guttiferae
Source classification
Garcinia cambogia Desr.
Plants
|
ATP Citrate Lyase
|
|
Garcinia cambogia extract contains several active compounds, including hydroxycitric acid (HCA) (an ECC inhibitor), xanthones, benzophenones, hydroxycitric acid (an ATP-citrate lyase inhibitor). Garcinia cambogia extract lowers the body weight gain, visceral fat accumulation, blood and hepatic lipid concentrations, and plasma insulin and leptin levels in a high-fat diet (HFD)-induced obesity mouse model. Garcinia cambogia extract is promising for research of fatty liver, dyslipidemia, hyperinsulinemia and hyperleptinemia rendered by HFD .
|
-
- HY-134914
-
-
- HY-N0841
-
-
- HY-N3980R
-
|
|
Structural Classification
Natural Products
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
|
Autophagy
RAD51
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Infection
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
Disease Research Fields
|
Autophagy
RAD51
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N1486R
-
-
- HY-B0722
-
-
- HY-107811R
-
-
- HY-N0352
-
-
- HY-N13083
-
-
- HY-N11768
-
-
- HY-16468
-
-
- HY-Y0546R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Photosensitizer
|
|
Benzophenone (Standard) is the analytical standard of Benzophenone. This product is intended for research and analytical applications. Benzophenone standard is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone standard can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone standard can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone standard exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone standard exhibits estrogenic activity .
|
-
- HY-N10439
-
-
- HY-B0722R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Reactive Oxygen Species
|
|
Histamine (dihydrochloride) (Standard) is the analytical standard of Histamine (dihydrochloride). This product is intended for research and analytical applications. Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
|
-
- HY-113058
-
|
|
Microorganisms
Source classification
|
Endogenous Metabolite
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3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
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- HY-N0507
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Structural Classification
Simple Phenylpropanols
Rhodiola rosea Linn.
Crassulaceae
Source classification
Phenylpropanoids
Plants
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TNF Receptor
Interleukin Related
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Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-113509B
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15-epi-LXA4
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Structural Classification
Natural Products
Source classification
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STAT
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15(R)-Lipoxin A4 (15-epi-LXA4) is a STAT-6 activator and a lipid-derived lipoxin-type specialized pro-resolving mediator (SPM) that plays a role in promoting inflammation resolution and regulating immune cell function. 15(R)-Lipoxin A4 can improve the phagocytic function of microglia and exhibits anti-inflammatory activity. In Alzheimer's disease (AD) mouse models, 15(R)-Lipoxin A4 improves AD-like pathology. 15(R)-Lipoxin A4 holds potential for use in inflammation and neurodegenerative disease research .
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- HY-N0507R
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Structural Classification
Simple Phenylpropanols
Rhodiola rosea Linn.
Crassulaceae
Source classification
Phenylpropanoids
Plants
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TNF Receptor
Interleukin Related
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Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-153830
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C16 Lactosylceramide (d18:1/16:0)
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Structural Classification
Microorganisms
Source classification
Saccharides
Monosaccharides
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Endogenous Metabolite
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LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
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- HY-N0538
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- HY-N0469R
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Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
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Endogenous Metabolite
Virus Protease
HSV
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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- HY-W050154
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- HY-W050154R
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Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
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Parasite
Tyrosinase
NF-κB
CDK
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Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .
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- HY-N6871
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Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
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Bacterial
IKK
Ferroptosis
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Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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- HY-B2167R
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Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endogenous metabolite
Cardiovascular System Disorder
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Endogenous Metabolite
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Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1899S
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Taurodeoxycholic acid-d5 is the deuterium labeled Taurodeoxycholic acid (HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
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- HY-B0149S3
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Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
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- HY-126242S
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Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model .
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- HY-157029S
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-114360AS1
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Taurohyodeoxycholic acid-d4 (sodium) is a deuterated labeled Taurohyodeoxycholic acid (sodium) . Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
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- HY-13762S
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Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
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- HY-B0702S
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Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
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- HY-W757743
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Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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- HY-128423AS
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Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9) is the deuterium labeled Tylvalosin (HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
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- HY-A0143S
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Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
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- HY-117985S
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Evogliptin-d9 (DA-1229-d9) is deuterium labeled Evogliptin. Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
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| Cat. No. |
Product Name |
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Classification |
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- HY-157029S
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Alkynes
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Alkynes
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-168328
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Alkynes
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FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
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- HY-129602
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SD-36
5 Publications Verification
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PROTAC Synthesis
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SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-129510
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Alkynes
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4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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| Cat. No. |
Product Name |
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Classification |
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- HY-153482
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siRNAs
siRNA drugs
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ATU027 is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
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- HY-153482A
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siRNAs
siRNA drugs
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ATU027 sodium is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 sodium has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
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- HY-148230
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Decoy ODNs
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TFEB Decoy ODN sodium is a synthetic oligonucleotide with a hairpin ring structure, which were designed to inhibit Transcription factor EB (TFEB). TFEB decoy ODN inhibited fibrosis and autophagy in a UUO mouse model. The TFEB decoy ODNs also showed anti-inflammatory effects.
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- HY-145405
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Cationic Lipids
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C12-200 is a type of ionizable cationic lipid and helper lipid commonly used for mRNA delivery. In the hemophilia B mouse model, mRNA encoding human erythropoietin (EPO) and coagulation factor IX (FIX) can be successfully delivered and expressed using C12-200. C12-200 is utilized in research related to hemophilia B .
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- HY-147410
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ION-363
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Antisense Oligonucleotides
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Ulefnersen (ION363) is an Antisense Oligonucleotide (ASO) directed against the 6th intron of the fused-in sarcoma (FUS) transcript to silence FUS in a non-allele-specific manner. Ulefnersen can reduce postnatal levels of FUS protein in the brain and spinal cord in disease-relevant mouse model of ALS-FUS , delaying motor neuron degeneration. Ulefnersen can be used in the research of Amyotrophic Lateral Sclerosis (ALS) .
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- HY-159700
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Cationic Lipids
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AA3-DLin is an ionizable cationic lipid with a pKa value of 5.8. AA3-DLin is used to delivery mRNA combined with lipid nanoparticles (LNPs). AA3-DLin LNP COVID-19 vaccines encapsulating SARS CoV-2 spike mRNAs successfully induces strong immunogenicity in a BALB/c mouse model .
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- HY-147410A
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ION-363 sodium
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Antisense Oligonucleotides
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Ulefnersen sodium (ION363) is an Antisense Oligonucleotide (ASO) directed against the 6th intron of the fused-in sarcoma (FUS) transcript to silence FUS in a non-allele-specific manner. Ulefnersen sodium can reduce postnatal levels of FUS protein in the brain and spinal cord in disease-relevant mouse model of ALS-FUS , delaying motor neuron degeneration. Ulefnersen sodium can be used in the research of Amyotrophic Lateral Sclerosis (ALS) .
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- HY-147081
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AGRO-100
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Aptamers
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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- HY-160061
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Aptamers
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P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
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- HY-158830
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Antisense Oligonucleotides
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MDM4-targeting ASO sodium is a 25mer antisense oligonucleotide targeting?MDM4. MDM4-targeting ASO sodium induced exon 6 skipping, leading to nonsense-mediated decay of the mRNA transcript that excludes exon-6. In multiple human melanoma cell lines and in melanoma patient-derived xenograft (PDX) mouse models, MDM4-targeting ASO-mediated skipping of exon 6 decreased MDM4 abundance, inhibited melanoma growth, and enhanced sensitivity to MAPK-targeting therapeutics.
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- HY-N0538
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Xylite
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Fillers
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Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-154974
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Cationic Lipids
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LNP Lipid-8 (11-A-M) is an ionizable single-tail multi-head lipid that can be used as a lipid nanoparticle (LNP) to deliver siRNA to T cells without targeting ligands. LNP Lipid-8 is more selective for T cells than other cell types such as hepatocytes. LNP Lipid-8 selectively delivers siRNA/sgRNA to T cells (especially CD8 + T cells) through endogenous lipid transport pathways, and can enter cells and release RNA through endocytosis to achieve gene silencing. LNP Lipid-8 loaded with GFP siRNA (siGFP) significantly led to GFP gene silencing in mouse models. LNP Lipid-8 showed good efficacy and safety in both cells and animals, without obvious liver targeting and toxicity. LNP Lipid-8 can be used for RNA delivery research in the fields of tumor immunotherapy and T cell-mediated autoimmune diseases .
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