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Results for "

robust efficacy

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

2

Peptides

1

Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-130115A
    IACS-8803 disodium
    1 Publications Verification

    		 STING Cancer
    IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy .
    IACS-8803 disodium
  • HY-141896
    RET-IN-7

    		RET Cancer
    RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
    RET-IN-7
  • HY-130115B
    IACS-8803 diammonium
    1 Publications Verification

    		 STING Cancer
    IACS-8803 diammonium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 diammonium has a robust systemic antitumor efficacy .
    IACS-8803 diammonium
  • HY-179004
    ONO-9517601

    VU6022856

    		 Potassium Channel Neurological Disease
    ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders .
    ONO-9517601
  • HY-179005
    ONO-7927846

    VU6024391

    		 Potassium Channel Neurological Disease
    ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders .
    ONO-7927846
  • HY-130115
    IACS-8803

    		STING Cancer
    IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy .
    IACS-8803
  • HY-130116
    IACS-8779

    		STING Cancer
    IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy .
    IACS-8779
  • HY-130116A
    IACS-8779 disodium

    		STING Cancer
    IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma .
    IACS-8779 disodium
  • HY-130628
    PAK4-IN-1

    		PAK Cancer
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions .
    PAK4-IN-1
  • HY-174990
    HW201877

    		15-PGDH Metabolic Disease Inflammation/Immunology
    HW201877 is a potent and orally active 15-prostaglandin dehydrogenase (15-PGDH) inhibitor with an IC50 of 3.6 nM. HW201877 demonstrates robust cellular efficacy in elevating PGE2 levels in A549 cells and exhibits remarkable efficacy in animal models of tissue injury and fibrosis. HW201877 can be used for the study of inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF) and Crohn’s disease (CD) .
    HW201877
  • HY-151561
    WM382

    		Parasite Infection
    WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile .
    WM382
  • HY-155543
    Anticancer agent 135

    		Androgen Receptor Cancer
    Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
    Anticancer agent 135
  • HY-136527
    BMS-986251

    		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) .
    BMS-986251
  • HY-174382
    ROR1-IN-3

    		Akt mTOR NF-κB ROR Apoptosis Cancer
    ROR1-IN-3 (Compound 24d) is a potent and highly selective ROR1 kinase inhibitor (IC50 = 17.6 nM). ROR1-IN-3 demonstrates robust antitumor activity and inhibitory effect against ROR1 both in vitro and in vivo. ROR1-IN-3 has robust antiproliferative efficacy in vitro and in vivo. ROR1-IN-3 induces apoptosis in cancer cell lines. ROR1-IN-3 inhibits ROR1 downstream AKT/mTOR and NF-κB signaling pathway. ROR1-IN-3 can be studied in antitumor research .
    ROR1-IN-3
  • HY-174819
    VNRX-9945

    		HBV Infection
    VNRX-9945 is a potent, broadly and orally active HBV CAM (capsid assembly modulator) with an EC50 of 2.6 nM. VNRX-9945 exhibits excellent and broad antiviral activity against multiple HBV genotypes in vitro, along with favorable pharmacokinetic profiles across multiple species. VNRX-9945 demonstrates robust antiviral efficacy in the adeno-associated virus mice models of HBV (AAV-HBV) infection .
    VNRX-9945
  • HY-P4146
    Survodutide

    BI 456906

    		 GLP Receptor GCGR Metabolic Disease
    Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
    Survodutide
  • HY-138742
    HPK1-IN-7

    		MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
    HPK1-IN-7
  • HY-P4146A
    Survodutide TFA

    BI 456906 TFA

    		 GLP Receptor GCGR Metabolic Disease
    Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake .
    Survodutide TFA
  • HY-163083
    JN122

    		MDM-2/p53 Apoptosis Cancer
    JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
    JN122
  • HY-P991613
    BGB-A445

    		Orexin Receptor (OX Receptor) NF-κB Cancer
    BGB-A445 is a humanized non-ligand-blocking agonistic OX40 monoclonal antibody with high affinity to OX40. BGB-A445 activates downstream NF-κB pathway to induce immune cell activation, proliferation, and survival. BGB-A445 dose-dependently and significantly depletes regulatory T cells via antibody-dependent cellular cytotoxicity (ADCC). BGB-A445 demonstrates robust and dose-dependent antitumor efficacy in the MC38 mice models. BGB-A445 can be used for the research of cancer, such as colon adenocarcinoma .
    BGB-A445
  • HY-175469
    VNT-101

    		Influenza Virus Infection
    VNT-101 is an orally active influenza A (IAV) inhibitor. VNT-101 disrupts NP-NP PPI to block NP oligomerization and destabilize the viral ribonucleoprotein (RNP) complex, with potent antiviral activity across multiple influenza A subtypes. VNT-101 exhibits EC50 values of 4-5 nM in cellular cytopathic effect (CPE) assay, 4-8 nM in neuraminidase (NA) assay, and 21-45 nM in RNP assay. VNT-101 demonstrates robust in vivo antiviral efficacy in mice infected with lethal H1N1 virus. VNT-101 can be used for the study of influenza A infection .
    VNT-101
  • HY-W002942
    Ferroptosis-IN-21

    1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline

    		 Ferroptosis Reactive Oxygen Species (ROS) Inflammation/Immunology
    Ferroptosis-IN-21 is a ferroptosis inhibitor that protects against renal I/R injury by suppressing ferroptosis and directly scavenging peroxyl radicals. Ferroptosis-IN-21 displays broad-spectrum anti-ferroptotic efficacy across multiple inducers in renal tubular epithelial cells, with nanomolar potency and robust suppression of lipid Reactive Oxygen Species (ROS). Ferroptosis-IN-21 significantly ameliorates renal I/R injury in mice, reducing histological damage, functional impairment, and inflammatory cytokine expression, while decreasing lipid peroxidation biomarkers such as 4-hydroxynonenal. Ferroptosis-IN-12 can be used for research in the field of ferroptosis-targeted drug development .
    Ferroptosis-IN-21
  • HY-164202
    ORM-5029

    		Antibody-Drug Conjugates (ADCs) Cancer
    ORM-5029 is a first-in-class human epidermal growth factor receptor 2 (HER2)-targeted antibody-drug conjugate (ADC) comprised of SMol006, a highly potent GSPT1 degrader, conjugated to Pertuzumab (HY-P9912). ORM-5029 exhibits robust efficacy across 14 HER2-positive breast cancer cell lines, with IC50 values ranging from 0.3 to 14.4 nM.ORM-5029 demonstrates anti-tumor activity in the BT474 xenograft model. ORM-5029 can be used for study of breast cancer .
    ORM-5029
  • HY-176428
    PROTAC MNK1 degrader-1

    		PROTACs MNK Apoptosis Eukaryotic Initiation Factor (eIF) Cancer
    PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
    PROTAC MNK1 degrader-1
  • HY-178032
    PARP1-IN-44

    		PARP Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis STING Cancer
    PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .
    PARP1-IN-44

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