Search Result
Results for "
tumor efficacy
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-146185
-
|
|
Molecular Glues
Bcl-2 Family
|
Cancer
|
|
CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
|
-
-
- HY-W272058
-
|
|
Others
|
Cancer
|
|
Isometronidazole is a hypoxic cell sensitizer. Isometronidazole (750 mg/kg) shows an efficacy as a hypoxic cell sensitizer in severely hypoxic FaDu tumors but not in less hypoxic GL tumors.
|
-
-
- HY-141896
-
|
|
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.
|
-
-
- HY-150256
-
|
|
YAP
|
Cancer
|
|
YTP-17 is an orally active YAP-TEAD protein-protein interaction inhibitor with an IC50 of 4 nM. YTP-17 shows anti-tumor efficacy .
|
-
-
- 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-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-146034
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
Cancer
|
|
NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding
oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) .
|
-
-
- HY-157302
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-21 (compound 54) is a c-met inhibitor with an IC50 value of 0.45? nM, and shows anti-tumor efficacy in vivo .
|
-
-
- HY-W272058R
-
|
|
Biochemical Assay Reagents
Reference Standards
|
Cancer
|
|
Isometronidazole (Standard) is the analytical standard of Isometronidazole. This product is intended for research and analytical applications. Isometronidazole is a hypoxic cell sensitizer. Isometronidazole (750 mg/kg) shows an efficacy as a hypoxic cell sensitizer in severely hypoxic FaDu tumors but not in less hypoxic GL tumors.
|
-
-
- HY-16477A
-
|
ME2906 free acid; Mono-L-aspartyl chlorin e6 free acid; NPe6 free acid
|
Photosensitizer
|
Cancer
|
|
Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
|
-
-
- 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-112509
-
|
|
Autophagy
|
Cancer
|
|
STL427944 is a potent and selective FOXM1 inhibitor. STL427944 has the potential for the research of overcoming tumor chemoresistance and improving the efficacy of treatment with conventional cancer drug .
|
-
-
- HY-15855
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Fosbretabulin (tromethamine), also known as combretastatin A4 phosphate (CA4P), is a vascular disrupting agent evaluated for its efficacy against anaplastic thyroid carcinoma (ATC). It targets tumor neovasculature, causing acute and reversible reductions in tumor blood flow and central necrosis .
|
-
-
- HY-164959
-
|
|
Lipocalin Family
|
Cancer
|
|
ZINC00230567 is an inhibitor for Lipocalin-2 (LCN2). ZINC00230567 reduces the colony formation and cell viability of cell SUM149, and exhibits anti-tumor efficacy .
|
-
-
- HY-159642
-
|
|
FGFR
|
Cancer
|
|
Dabogratinib is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM in Ba/F3. Dabogratinib exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
-
-
- HY-13303
-
|
|
MEK
|
Cancer
|
|
RO 4927350 is a potent and selective non-ATP-competitive MEK1/2 inhibitor. RO 4927350 exhibits significant antitumor efficacy in a broad spectrum of tumor models .
|
-
-
- 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-118269
-
|
|
c-Met/HGFR
|
Cancer
|
|
OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
|
-
-
- 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-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-P1919
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase 369-377, human is a HLA-A2.1-restricted epitope derived from tyrosinase, has been used to develop tumor-targeted vaccines with mixed efficacy .
|
-
![[Asp371]-Tyrosinase (369-377), human](//file.medchemexpress.eu/product_pic/hy-p1919.gif)
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
-
- 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-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-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-106154
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 (CPI-0004) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
-
- HY-155003
-
|
|
Fluorescent Dye
|
Cancer
|
|
TPEQM-DMA is a NIR-II photosensitizer. TPEQM-DMA accumulates in cancerous mitochondria, and inhibits cancer cell growth. TPEQM-DMA has potent type-I phototherapeutic efficacy to overcome the intrinsic pitfalls of PDT in combating hypoxic tumors .
|
-
-
- HY-163683
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
EB-PSMA-617 is a modified form of PSMA-617 that has enhanced pharmacokinetic properties by conjugating it to Evans Blue (EB) to extend its circulation half-life to improve prostate tumor uptake and radiotherapy efficacy. In preclinical studies using PC3-PIP-loaded mice, EB-PSMA-617 demonstrated prolonged blood half-life, increased accumulation in PSMA-positive tumors, and successful tumor elimination with lower radioactivity .
|
-
-
- HY-13554
-
|
|
Antibiotic
|
Infection
Cancer
|
|
Annamycin is an antibiotic, that has high affinity for lipid membranes and can bypass the multidrug resistance protein-1 (MDR-1 ) mechanism of cellular drug resistance. Annamycin exhibits antitumor efficacy in multilamellar vesicles against solid tumor .
|
-
-
- HY-130628
-
|
|
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 .
|
-
-
- 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-170554
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
ABBV-706 is a SEZ6 targeting ADC, which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors .
|
-
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
-
- 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-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
-
- HY-148808
-
|
RXC007
|
ROCK
|
Cancer
|
|
Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma .
|
-
-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
|
-
-
- HY-116604
-
|
PD 139530
|
PI3K
Akt
|
Cancer
|
|
RLX (PD 139530) is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness .
|
-
-
- HY-132822A
-
|
SBP-101 hydrochloride
|
Drug Derivative
|
Cancer
|
|
Ivospemin (SBP-101) hydrochloride is an antineoplastic spermine analog. Ivospemin hydrochloride has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin hydrochloride shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin hydrochloride is promising for research of cancers .
|
-
-
- HY-130116A
-
|
|
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 .
|
-
-
- HY-132822
-
|
SBP-101
|
Drug Derivative
|
Cancer
|
|
Ivospemin (SBP-101) is an antineoplastic spermine analog. Ivospemin has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin is promising for research of cancers .
|
-
-
- HY-109084A
-
|
CT-707 tetrahydrochloride
|
FAK
|
Cancer
|
|
Conteltinib tetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride salt form of Conteltinib (HY-109084). Conteltinib tetrahydrochloride is the inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. Conteltinib tetrahydrochloride exhibits a synergistic anti-tumor efficacy with Cabozantinib (HY-13016) .
|
-
-
- HY-111458
-
|
|
Deubiquitinase
|
Cancer
|
|
GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
|
-
-
- HY-161774
-
|
|
CD73
|
Cancer
|
|
ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC) .
|
-
-
- HY-162763
-
|
|
Apoptosis
|
Cancer
|
|
FLQY2 is a camptothecin analog that exhibits outstanding antitumor efficacy against various solid tumors. FLQY2 possesses both in vitro and in vivo anti-pancreatic cancer activity, inhibiting cell proliferation, colony formation, inducing apoptosis, and causing cell cycle arrest at nanomolar concentrations .
|
-
-
- HY-155995
-
|
MK-905
|
Biochemical Assay Reagents
|
Cancer
|
|
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
|
-
-
- HY-116604A
-
|
PD 139530 hydrochloride
|
PI3K
Akt
|
Cancer
|
|
RLX (PD 139530) hydrochloride is the hydrochloride of RLX (HY-116604). RLX is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness .
|
-
-
- HY-P10239A
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
Tyr3-Octreotate acetate is a somatostatin analog. Tyr3-Octreotate acetate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate acetate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
|
-
-
- HY-P10239
-
|
|
Somatostatin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
Tyr3-Octreotate is a somatostatin analog. Tyr3-Octreotate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
|
-
-
- HY-163363
-
|
|
Adrenergic Receptor
|
Cancer
|
|
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
|
-
- HY-115400
-
1V209
4 Publications Verification
TLR7 agonist T7
|
Toll-like Receptor (TLR)
|
Cancer
|
|
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity .
|
-
- HY-155458
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
|
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more .
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
|
-
- HY-159642G
-
|
|
FGFR
|
Cancer
|
|
Dabogratinib (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib (GMP) is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM. Dabogratinib (GMP) exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
-
- HY-174418
-
-
- HY-176508
-
|
|
Casein Kinase
|
Cancer
|
|
KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models .
|
-
- 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-P99320
-
|
OMP 59R5; Anti-Human NOTCH2 Recombinant Antibody
|
Notch
|
Cancer
|
|
Tarextumab (OMP-59R5) is a cross-reactive, fully human IgG2 antibody that selectively inhibits Notch2 and Notch3 signaling. Tarextumab demonstrates broad-spectrum antitumor efficacy in xenograft models of epithelial tumors. Tarextumab can be used for the study of pancreatic cancer .
|
-
- HY-145688
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-33 is a potent HDAC inhibitor with IC50s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
|
-
- HY-178148
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
|
-
- 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-168983
-
|
|
Bcl-2 Family
|
Cancer
|
|
Lonitoclax is a B-cell lymphoma 2 (Bcl-2) inhibitor. Lonitoclax has comparable anti-tumor efficacy to Venetoclax (HY-15531) in both B cell and myeloid malignancy models. Lonitoclax is promising for research of relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas .
|
-
- HY-141606
-
|
BAY 94-9343
|
Microtubule/Tubulin
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
|
-
- HY-175828
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DHPS-IN-2 is an allosteric deoxyhypusine synthase (DHPS) inhibitor with an IC50 of 70 nM and a Kd of 26.4 μM. DHPS-IN-2 significantly suppresses melanoma cell migration and invasiveness in vitro and exhibits potent anti-tumor efficacy in an A375 cell zebrafish xenograft model. DHPS-IN-2 can be used for the study of melanoma .
|
-
- 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-145687
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-32 is a potent HDAC inhibitor with IC50s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity .
|
-
- HY-158039
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors .
|
-
- HY-115581
-
|
Deoxythymidine 3′,5′-diphosphate; pdTp
|
Apoptosis
|
Cancer
|
|
Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of staphylococcal nuclease and tudor domain containing 1 (SND1, the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate exhibits anti-tumor efficacy in vivo .
|
-
- HY-158050
-
|
|
c-Fms
|
Cancer
|
|
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .
|
-
- HY-P99493
-
|
IMGN242; huC242-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (HY-12454). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- 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-170812
-
|
|
Aurora Kinase
|
Cancer
|
|
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
|
-
- HY-W769206
-
|
ME2906 free acid-13C4,15N; Mono-L-aspartyl chlorin e6 free acid-13C4,15N; NPe6 free acid-13C4,15N
|
Isotope-Labeled Compounds
Photosensitizer
|
Cancer
|
|
Talaporfin- 13C4, 15N (ME2906 (free acid)- 13C4, 15N) is the 13C- and 15N-labeled Talaporfin (HY-16477A). Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
|
-
- HY-144132
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner .
|
-
- HY-50672
-
|
|
Kinesin
Apoptosis
Lipoxygenase
|
Cancer
|
|
MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy .
|
-
- 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-P10930A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
wrwycr-NH2 (TFA) is a peptide. wrwycr-NH2 (TFA) is cytotoxic to multiple cancer cells, can induce DNA damage and cell cycle arrest, but does not induce endoplasmic reticulum stress. wrwycr-NH2 (TFA) has anti-tumor activity, and it shows better efficacy when used in combination with DNA-damaging agents .
|
-
- HY-172108
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. TGFβRI-IN-7 inhibits SMAD2/3 phosphorylation and H22 cell viability with IC50 values of 12 and 65 nM, respectively. TGFβRI-IN-7 shows anti-tumor efficacy in a xenograft model of H22 cells, with TGI of 79.6 % .
|
-
- HY-164387
-
|
|
EGFR
PDGFR
VEGFR
|
Cancer
|
|
Sutetinib is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
|
-
- HY-165421
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
|
-
- HY-178921
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
HJ-4 is a Piperine (HY-N0144) derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC) .
|
-
- HY-157014
-
|
|
Tryptophan Hydroxylase
|
Cancer
|
|
TPT-004 is a selective and oraly active tryptophan hydroxylases (TPH) inhibitor with IC50s of 77 nM and 16 nM for TPH1 and TPH2, repsectively. TPT-004 exhibits exceptional selectivity for TPH1 compared with other members of the AAAH family. TPT-004 shows efficacy peripheral serotonin attenuation and colorectal tumor growth in mice[1][2].
|
-
- HY-16290
-
|
ZK 230211; BAY86 5044
|
Progesterone Receptor
|
Endocrinology
|
|
Lonaprisan (ZK 230211; BAY86 5044) is an antagonist for progesterone receptor, with IC50 of 3.6 pM and 2.5 pM for PR-A and PR-B, respectively. Lonaprisan exhibits antiprogestagenic activity in rabbits, interrupts early pregnancy in rats, and exhibits antitumor efficacy against DMBA (HY-W011845)-induced mammary tumor. Lonaprisan reveals antiglucocorticoid and antiandrogenic effect .
|
-
- HY-163028
-
|
|
Tim3
|
Cancer
|
|
ML-T7 is a potent Tim-3 inhibitor. ML-T7 blocks Tim-3 interactions with PtdSer and CEACAM1.
ML-T7 not only enhances the antitumor activity of adoptive transfer therapy with cytotoxic T lymphocytes (CTLs) and CAR T cells but also increases the effector function of T cell. ML-T7 promotes NK cells’ killing activity against tumor cells and DC antigen-presenting capacity. ML-T7 directly exerts antitumor efficacy in preclinical tumor models either alone or in combination with Nivolumab (HY-P9903A). ML-T7 can be used for tumor immunotherapy research .
|
-
- HY-159577
-
|
|
PI3K
mTOR
Akt
|
Cancer
|
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
|
-
- HY-148114
-
|
|
Autophagy
|
Cancer
|
|
MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-119624). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells .
|
-
- HY-151462
-
RP-6685
2 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-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-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-119467
-
|
|
Ser/Thr Protease
|
Cancer
|
|
MDK0734 is a selective inhibitor that inhibits feline hepsin B endopeptidase and exopeptidase activities. MDK0734 demonstrated efficacy in a cell-based in vitro tumor invasion model, significantly attenuating the invasive ability of MCF-10A neoT cells. MDK0734 provides new potential inhibitors for the development of clinically useful compounds targeting the deleterious effects of feline hepsin B in cancer progression .
|
-
- HY-B0067B
-
|
(R)-SM-5887
|
Topoisomerase
|
Cancer
|
|
(R)-Amrubicin ((R)-SM-5887) is an anthracycline that effectively treats lung cancer by intercalating into DNA and inhibiting topoisomerase II activity, which consequently hampers DNA replication as well as RNA and protein synthesis, leading to cell growth inhibition and apoptosis. This compound exhibits superior anti-tumor efficacy compared to traditional anthracycline drugs while lacking the cumulative cardiac toxicity typically associated with this drug class.
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1 (HY-19792)) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-W110138
-
|
|
DNA/RNA Synthesis
Cytochrome P450
ROCK
|
Cancer
|
|
Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
|
-
- HY-149428
-
AD4
1 Publications Verification
|
PROTACs
|
Cancer
|
|
AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
|
-
- HY-164387A
-
|
|
EGFR
VEGFR
PDGFR
|
Cancer
|
|
Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
|
-
- 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-15160A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-15160B
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-169937
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(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) .
|
-
- HY-144720
-
|
|
SWI/SNF Complex
|
Cancer
|
|
BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .
|
-
- HY-115567
-
|
1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
|
Apoptosis
|
Cancer
|
|
5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
|
-
- HY-162730
-
|
|
Molecular Glues
Phosphodiesterase (PDE)
|
Cancer
|
|
OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor .
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-159803
-
|
6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin
|
Endogenous Metabolite
|
Cancer
|
|
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 .
|
-
- HY-P99712
-
|
hz208F2-4
|
IGF-1R
Apoptosis
ADC Antibody
|
Cancer
|
|
Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody, serveing as a targeting vector for antibody-drug conjugates (ADCs). Lonigutamab causes G2-M phase cell cycle arrest and increases apoptosis in IGF-1R-overexpressing tumor cells. Lonigutamab demonstrates potent antitumor efficacy in IGF-1R-overexpressing xenograft models. Lonigutamab can be used for the study of Solid tumors with overexpression of IGF-1R and thyroid eye
diseases sup>[2].
|
-
- HY-174437
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-32 is a potent and orally active FLT3 inhibitor. FLT3-IN-32 shows high selectivity for FLT3 and efficiently inhibits FLT3-activating mutations and induces apoptosis. FLT3-IN-32 shows good tolerability in non-tumor bearing mice. FLT3-IN-32 demonstrates outstanding anti-tumor efficacy in MV4-11 bearing NOD/SCID mice, prolonging the survival noticeably. FLT3-IN-32 can be used for the research of acute myeloid leukemia .
|
-
- HY-116452
-
|
|
VEGFR
|
Cancer
|
|
YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis .
|
-
- HY-156397
-
|
|
AMPK
YAP
|
Cancer
|
|
HTH-02-006 is a NUAK2 inhibitor, with an IC50 value of 126 nM. HTH-02-006 inhibits NUAK2-mediated signaling by reducing phosphorylation of its substrate MYPT1 at S445 and downstream MLC. HTH-02-006 shows growth inhibitory efficacy in YAP-high cancer cells (HuCCT-1, SNU475). HTH-02-006 significantly suppresses YAP-induced hepatomegaly (reduced liver/body weight ratio) in TetO-YAP S127A transgenic mice and demonstrates significant anti-tumor efficacy in mice bearing HMVP2 prostate cancer allografts. HTH-02-006 can be used for the study of liver cancer and prostate cancer .
|
-
- HY-15882
-
|
|
Endogenous Metabolite
|
Cancer
|
|
GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
|
-
- HY-W013272
-
|
HFT
|
Androgen Receptor
Drug Metabolite
Akt
PI3K
Gap Junction Protein
Integrin
|
Cancer
|
|
Hydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC50 of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases .
|
-
- HY-175660
-
|
|
Heme Oxygenase (HO)
|
Cancer
|
|
KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC50 = 123 nM) and human HO-1: IC50 = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1 + perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer .
|
-
- HY-172930
-
|
|
Molecular Glues
IKZF Family
Potassium Channel
|
Inflammation/Immunology
Cancer
|
|
PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
|
-
- HY-175290
-
|
|
Arf Family GTPase
|
Cancer
|
|
Arf1-GEFs-IN-1 is a potent and orally active ADP-ribosylation factor 1- guanine nucleotide exchange factors (Arf1-GEFs) inhibitor with an IC50 value of 40.85 μM against CT26 cells. Arf1-GEFs-IN-1 primarily mediates tumor regression by triggering anti-tumor immune responses, rather than through direct cytotoxicity. Arf1-GEFs-IN-1 effectively promotes CCL5 expression, demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 can be used for the study of colon cancer .
|
-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
- HY-126170
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Valanimycin is an antibiotic, which inhibits Escherichia coli (BE1121) through interaction with DNA. Valanimycin exhibits cytotoxicity to mouse leukemia L1210, P388/S (doxorubicin (HY-15142A)-sensitive), and P388/ADR (doxorubicin-resistant), with IC50 of 0.79, 2.65, and 1.44 μg/mL, respectively. Valanimycin exhibits antitumor efficacy against ehrlich ascites tumors or L1210 in mice .
|
-
- HY-15496
-
|
ER-806201
|
MEK
FLT3
|
Cancer
|
|
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
|
-
- HY-164426
-
|
|
P2X Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
HEI3090 is a P2X7R activator. HEI3090 stimulates dendritic cells expressing P2X7R to produce IL-18, which subsequently promotes Natural Killer cells and CD4 T cells within tumors to produce IFN-γ, leading to a sustained antitumor response. HEI3090 can be used to enhance the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC) .
|
-
- HY-162962
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/TDO-IN-7 (Compound 43b), an isoquinoline derivative, is a potent dual IDO1/TDO inhibitor, with IC50s of 0.31 μM and 0.08 μM, respectively. IDO1/TDO-IN-7 displays acceptable pharmacokinetic profiles and potent antitumor efficacy with low toxicity in B16-F10 tumor model .
|
-
- HY-145561
-
|
BLD-0409; PAT-409
|
Phosphodiesterase (PDE)
LPL Receptor
|
Inflammation/Immunology
Cancer
|
|
Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc .
|
-
- HY-178045
-
|
|
c-Myc
|
Cancer
|
|
MYC-IN-4 is a MYC inhibitor. MYC-IN-4 impairs MYC/MAX protein-protein interaction (IC50 = 3.06 μM). MYC-IN-4 inhibits MYC-aberrant PC-3 prostate cancer cells with an IC50 of 0.440 μM. MYC-IN-4 demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts. MYC-IN-4 can be used for the study of prostate cancer .
|
-
- HY-15160C
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-173065
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
|
-
- HY-W338346
-
|
|
Drug Derivative
Interleukin Related
TNF Receptor
Polo-like Kinase (PLK)
|
Inflammation/Immunology
Cancer
|
|
Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer .
|
-
- HY-175874
-
|
|
Microtubule/Tubulin
PI3K
Akt
Apoptosis
|
Cancer
|
|
Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer .
|
-
- HY-120281
-
|
|
MEK
PI3K
Akt
Apoptosis
Caspase
|
Cancer
|
|
ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
|
-
- HY-204056
-
|
|
Telomerase
|
Cancer
|
|
Telomerase-IN-8 is an orally active telomerase inhibitor, with an IC50 value of 0.98 μM. Telomerase-IN-8 exhibits potent antiproliferative activity against multiple tumor cell lines, including PC3, Bcap-37, MGC-803 and HepG2. Telomerase-IN-8 demonstrates potent antitumor efficacy in S180 sarcoma or HepG2 hepatoma xenograft mice. Telomerase-IN-8 can be used for the study of telomerase-targeted anticancer .
|
-
- HY-P10925
-
|
FOG-001; I-66
|
β-catenin
|
Cancer
|
|
Zolucatetide (FOG-001;I-66) is a potent β-catenin inhibitor with an IC50 of <50 nM. Zolucatetide can inhibits β-catenin and T-cell factor (TCF) transcription factor interaction. Zolucatetide inhibits cell proliferation and induces cell cycle arrest in target cells. Zolucatetide exhibits anti-tumor efficacy in mice bearing COLO320DM colon cancer cell (with APC, TP53 mutations) xenografts. Zolucatetide can be used for the study of colon cancer .
|
-
- HY-176300
-
|
|
Integrin
|
Cancer
|
|
RGD-DA6 is an αvβ3-targeted ligand. RGD-DA6 consists of RGDfK (an integrin αvβ3-targeted RGD peptide), DOTADG, d-Glu, Lys, AMBA, and IPBA. RGD-DA6 can be radiolabeled as an αvβ3-targeted radioligand and used for high-contrast tumor imaging and enhanced anticancer efficacy .
|
-
- HY-108417
-
|
|
STAT
JAK
Bcr-Abl
|
Cancer
|
|
Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
|
-
- HY-147214
-
|
|
YAP
|
Cancer
|
|
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
|
-
- HY-175214
-
|
|
Reactive Oxygen Species (ROS)
Photosensitizer
|
Cancer
|
|
Antitumor photosensitizer-9 is a near-infrared Photosensitizer (PS) with a high singlet oxygen production rate (relative rate = 1.79). Antitumor photosensitizer-9 exhibits strong phototoxicity against various cancer cells and induces ROS generation under light irradiation. Antitumor photosensitizer-9 inhibits tumor growth in vivo and exhibits excellent anticancer photodynamic therapy (PDT) efficacy at low drug and light doses. Antitumor photosensitizer-9 can be used in photodynamic therapy research .
|
-
- HY-101144
-
|
TCD-717
|
Choline Kinase
|
Cancer
|
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
|
-
- HY-138742
-
|
|
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 .
|
-
- HY-143434
-
|
|
FLT3
|
Cancer
|
|
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) .
|
-
- HY-151292
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Antitumor agent-74 (compound 13da) is a quinoxalines derivative, an antitumor agent. Antitumor agent-74 exhibits more potent efficacy on tumor inhibition, mixed with regioisomer Antitumor agent-75(HY-151295, compound 14 da) (mriBIQ 13da/14da). mriBIQ 13da/14da attests cell cycle at S phase, inhibits DNA synthesis, and induces mithochondrial apoptosis .
|
-
- HY-178018
-
|
iOXCT1
|
Mitochondrial Metabolism
|
Cancer
|
|
D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC) .
|
-
- HY-178472
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
|
-
- 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-N7694
-
|
|
TGF-β Receptor
JAK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
|
-
- HY-169921
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers .
|
-
- HY-168491
-
|
|
Phosphodiesterase (PDE)
STING
PD-1/PD-L1
|
Cancer
|
|
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .
|
-
- HY-131667
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy .
|
-
- HY-175555
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-54 is a tubulin inhibitor. Tubulin-IN-54 exhibits anti-proliferative activity against various cancer cells. Tubulin-IN-54 inhibits tubulin polymerization, disrupts microtubule networks, induces G2/M cell cycle arrest, and promotes cancer cell apoptosis. Tubulin-IN-54 demonstrates significant anti-tumor efficacy in mice bearing PC-3/TxR xenografts. Tubulin-IN-54 can be used for the study of taxane-resistant cancers (prostate cancer, melanoma) .
|
-
- HY-179019
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
Caspase
|
Neurological Disease
Cancer
|
|
HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3, 10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research .
|
-
- HY-175981
-
|
|
Drug Derivative
|
Cancer
|
|
Paclitaxel-bromothiophene is a semisynthetic taxane analogue of Paclitaxel (HY-B0015). Paclitaxel-bromothiophene exhibits potent antiproliferative activity against 4-T1 breast cancer cells, with an IC50 value of 15.18 nM. Paclitaxel-bromothiophene shows high binding affinity to C5aR1 (Kd = 19.4 μM). Paclitaxel-bromothiophene demonstrates excellent anti-tumor efficacy in 4-T1 breast cancer-bearing mice. Paclitaxel-bromothiophene can be used for the study of breast cancer .
|
-
- HY-116861
-
|
|
MetAP
|
Cancer
|
|
A-357300 is a reversible and selective MetAP2 inhibitor with IC50s of 0.12 and 57 μM against MetAP2 and MetAP1. A-357300 induces cytostasis by cell cycle arrest at the G1 phase selectively in endothelial cells and in a subset of tumor cells. A-357300 inhibits angiogenesis both in vitro and in vivo and shows potent antitumor efficacy in carcinoma, sarcoma, and neuroblastoma murine models. A-357300 can be used for the studies of neuroblastoma, fibrosarcoma and breast cancer .
|
-
- HY-151443
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-134813
-
MRTX1133
Maximum Cited Publications
32 Publications Verification
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-156096
-
|
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- 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-111033
-
|
|
MEK
ERK
Apoptosis
p38 MAPK
CDK
PARP
|
Cancer
|
|
RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research .
|
-
- HY-W347368
-
|
Methyl punicate
|
Endogenous Metabolite
|
Cancer
|
|
9Z,11E,13Z-Octadecatrienoicacid, methylester (Methyl punicate) is a fatty acid methyl ester, which can be isolated from seeds of Punica granatum L.. 9Z,11E,13Z-Octadecatrienoicacid, methylester exhibits antitumor efficacy, which interferes with tumor cell cycle, drug resistance and angiogenesis. 9Z,11E,13Z-Octadecatrienoicacid, methylester is the derivative of Punicic acid (HY-139066) .
|
-
- HY-175714
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
STING agonist-46 is an orally active STING agonist. STING agonist-46 activates the STING signaling pathway, promoting phosphorylation of TBK1 and IRF3, and secretion of IFN-β and IP-10. STING agonist-46 directly binds to STING and increases its thermal stability. STING agonist-46 demonstrates potent anti-tumor efficacy in B16F10, CT26, and 4T1 mouse models. STING agonist-46 can be used for cancer immunotherapy studies .
|
-
- HY-111790
-
M3258
2 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
|
-
- HY-U00279B
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Nitracrine hydrochloride is a platinum-based antineoplastic drug with selective toxicity to hypoxic cells. Nitracrine hydrochloride exhibits significant cytotoxicity against the Chinese hamster ovary cell line AA8 under hypoxic conditions. Nitracrine hydrochloride exerts its effect by binding to the insertion of DNA and forming covalent adducts. The cytotoxicity of Nitracrine hydrochloride under hypoxic conditions is related to its reductive metabolism to form alkylated substances. At the same time, it may enhance the reactivity to DNA through the insertion of DNA, thereby improving the efficacy. Nitracrine hydrochloride can also inhibit RNA synthesis, contributing to its anti-tumor effect .
|
-
- HY-P10925A
-
|
(Z)-FOG-001; I-67
|
β-catenin
|
Cancer
|
|
(Z)-Zolucatetide ((Z)-FOG-001; I-67), a structural isomer of Zolucatetide (HY-P10925), is a potent β-catenin inhibitor with an IC50 of <50 nM. Zolucatetide can inhibits β-catenin and T-cell factor (TCF) transcription factor interaction. Zolucatetide inhibits cell proliferation and induces cell cycle arrest in target cells. Zolucatetide exhibits anti-tumor efficacy in mice bearing COLO320DM colon cancer cell (with APC, TP53 mutations) xenografts. Zolucatetide can be used for the study of colon cancer .
|
-
- HY-175846
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
TQFL13 is derivative of Thymoquinone (TQ) (HY-D0803) with potent anti-breast cancer activity. TQFL13 exhibits higher cytotoxicity against breast cancer cells (BT549, MDA-MB-231, 4T1). TQFL13 increases apoptosis and blocks the cell cycle at S and G2/G1 phases in breast cancer cells. TQFL13 shows dose-dependent anti-tumor efficacy in mouse breast cancer allograft model. TQFL13 can be used for the study of breast cancer .
|
-
- HY-178777
-
|
|
BCL6
|
Cancer
|
|
BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
|
-
- HY-175544
-
|
|
Drug Derivative
|
Cancer
|
|
anti-TNBC agent-10 is an anti-TNBC agent. anti-TNBC agent-10 shows potent anti-TNBC activity against BT549 cells (IC50 = 0.018 μM) and maintains activity against MDA-MB-231 cells (IC50 = 4.16 μM). anti-TNBC agent-10 9 demonstrates significant anti-tumor efficacy in mice bearing subcutaneous MDA-MB-231 TNBC xenografts. anti-TNBC agent-10 can be used for the study of triple-negative breast cancer (TNBC) .
|
-
- HY-170947
-
|
|
STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
|
-
- HY-177578
-
|
|
Antibody-Drug Conjugates (ADCs)
c-Kit
Apoptosis
Microtubule/Tubulin
ERK
Akt
Caspase
|
Cancer
|
|
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
|
-
- HY-145939
-
|
BRD5846
|
Casein Kinase
|
Cancer
|
|
BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
|
-
- HY-155073
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
|
-
- HY-159966
-
|
|
Topoisomerase
HDAC
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562) .
|
-
- HY-174458
-
|
|
PROTACs
MDM-2/p53
IKZF Family
Casein Kinase
|
Cancer
|
|
MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
|
-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
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 .
|
-
- HY-N1934
-
|
|
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
|
-
- HY-155222
-
|
|
Epigenetic Reader Domain
HDAC
|
Cancer
|
|
TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026) .
|
-
- HY-N3389
-
|
|
SARS-CoV
Sirtuin
CDK
Apoptosis
|
Infection
Metabolic Disease
Cancer
|
|
Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-Cyclin E1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC50 of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection .
|
-
- HY-175589
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma .
|
-
- HY-178219
-
|
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE is a drug-linker conjugate for ADC. 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE contains a linker and bioactive small molecule toxins MMAE (HY-15162). 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE can conjugate with NN2101 (HY-P991293) (anti c-Kit) for synthesizing NN3201. NN3201 rapidly internalizes and inhibits SCF-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) .
|
-
- HY-175542
-
|
|
STAT
Apoptosis
Reactive Oxygen Species (ROS)
PARP
|
Cancer
|
KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer .
|
-
- HY-162098
-
|
|
PROTACs
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
|
-
- HY-P990068
-
|
SRF617
|
NTPDase
|
Inflammation/Immunology
Cancer
|
|
Perenostobart (SRF617) is a human IgG4 antibody with inhibitory activity against CD39 ATPase. Perenostobart inhibits CD39-mediated hydrolysis of extracellular ATP to AMP, with IC50 values of 1.9 nM (HEK293 OE cells), 0.7 nM (MOLP-8 cells), and 1.2 nM (RBC-lysed whole blood). Perenostobart enhances CD4 + T-cell proliferation, promotes dendritic cell maturation, and boosts inflammasome activation in macrophages in the presence of ATP. Perenostobart demonstrates significant single-agent anti-tumor efficacy in MOLP-8 and H520 xenograft models. Perenostobart can be used for the study of cancer .
|
-
- HY-134813A
-
|
|
Ras
|
Cancer
|
|
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-119272
-
EF24
2 Publications Verification
|
ERK
Caspase
NF-κB
Apoptosis
p38 MAPK
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
|
-
- HY-164202
-
|
|
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 .
|
-
- HY-175698
-
|
|
Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
|
Cancer
|
|
Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [ 3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC) .
|
-
- HY-161785
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
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 .
|
-
- HY-175502
-
|
|
Molecular Glues
IKZF Family
Apoptosis
|
Cancer
|
|
MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL) .
|
-
- HY-105369
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
|
-
- HY-161826
-
|
|
Wnt
β-catenin
HSP
CDK
c-Myc
|
Cancer
|
|
Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
|
-
- HY-114340
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
LEM-14 is a potent and selective NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has very weak activitv
against NSD1 and has no activity against NSD3. LEM-14 inhibits fibrotic gene expression in ND but not DIO BMDMs. LEM-14 combined with ionizing radiation (IR) enhances the apoptosis rate and reduces the colony-formation ability of CRC cells. LEM-14 exhibits enhanced anti-tumor efficacy in Balb/c nude mice bearing LoVo cell xenografts when combined with ionizing radiation. LEM-14 has the potential for the research of multiple myeloma and colorectal cancer .
|
-
- HY-175497
-
|
|
ROR
Apoptosis
Bcl-2 Family
PARP
|
Cancer
|
|
ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC) .
|
-
- HY-160151
-
|
|
PROTACs
Phosphatase
JAK
IFNAR
MHC
|
Cancer
|
|
TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: (HY-138964), Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002)) .
|
-
- HY-158156
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
|
-
- HY-101741
-
|
A-289099
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
|
-
- HY-175826
-
|
|
Deubiquitinase
Ferroptosis
Reactive Oxygen Species (ROS)
Glutathione Peroxidase
|
Cancer
|
|
USP30-IN-20 is an orally active USP30 inhibitor (Kd = 1.61 μM, IC50 = 12.8 μM). USP30-IN-20 induces ferroptosis by promoting ubiquitination-mediated degradation of GPX4. USP30-IN-20 inhibits the proliferation, migration, invasion, and stemness of prostate cancer cells. USP30-IN-20 induces G0/G1 cell cycle arrest and ROS levels in prostate cancer cells. USP30-IN-20 exhibits significant anti-tumor efficacy in PC3 cell subcutaneous xenografts in mice. USP30-IN-20 can be used for the study of advanced prostate cancer .
|
-
- HY-161275
-
|
|
EGFR
Akt
ERK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-N1934R
-
|
|
Reference Standards
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
|
-
- HY-W015490R
-
|
|
DNA/RNA Synthesis
NF-κB
Monoamine Oxidase
TNF Receptor
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
|
-
- HY-W015490
-
|
|
DNA/RNA Synthesis
NF-κB
Monoamine Oxidase
TNF Receptor
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
|
-
- HY-174437B
-
|
|
FLT3
Apoptosis
STAT
p38 MAPK
Akt
|
Cancer
|
|
FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC50s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
|
-
- HY-W015490S
-
|
|
Isotope-Labeled Compounds
DNA/RNA Synthesis
NF-κB
Monoamine Oxidase
TNF Receptor
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone. 1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
|
-
- HY-159922
-
|
|
Androgen Receptor
|
Cancer
|
|
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 .
|
-
- HY-167854
-
|
|
Aurora Kinase
Apoptosis
IGF-1R
|
Cancer
|
|
KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
|
-
- HY-170926
-
|
|
RET
Apoptosis
|
Cancer
|
CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
|
-
- HY-154974
-
|
|
Liposome
|
Cancer
|
|
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 .
|
-
- HY-178032
-
|
|
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 .
|
-
- HY-178858
-
|
|
PROTACs
FLT3
Checkpoint Kinase (Chk)
STAT
ERK
c-Myc
Akt
|
Cancer
|
|
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .
|
-
- HY-175610
-
|
|
PROTACs
FLT3
JAK
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
|
-
-
-
HY-L179
-
|
|
40 compounds
|
|
Radiotherapy is a common treatment for various cancers, and more than 50% of cancer patients require radiotherapy during the disease treatment. With advances in radiation technology and a better understanding of tumor biology, the efficacy of radiation therapy has gradually improved, and more and more patients have benefited from it. However, even with the use of advanced radiotherapy techniques, there are still many malignant tumor cells with low sensitivity to radiation, leading to the radiation effect is not ideal. To solve this problem, radiosensitizers have received more and more attention. Radiosensitizer is a kind of drug that can enhance the radiosensitivity of tumor cells and improve the effect of radiotherapy. Radiation sensitizers act in a variety of ways, such as killing hypoxic cells, enhancing DNA damage, inhibiting DNA damage repair, and blocking cell cycle progression, making tumor cells more susceptible to radiation damage and death than surrounding normal cells.
MCE designs a unique collection of 40 compounds with definite reported radiosensitization. It can be used for drug combination research in anti-cancer treatment.
|
| Cat. No. |
Product Name |
Type |
-
- HY-159642G
-
|
|
Fluorescent Dye
|
|
Dabogratinib (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib (GMP) is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM. Dabogratinib (GMP) exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
| Cat. No. |
Product Name |
Type |
-
- HY-159642G
-
|
|
Biochemical Assay Reagents
|
|
Dabogratinib (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib (GMP) is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM. Dabogratinib (GMP) exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-113003
-
|
γ-Glutamylglutamine; γ-Glu-Gln
|
Peptides
|
Others
Cancer
|
|
H-γ-Glu-Gln-OH is a hydrophilic peptide and can be conjugated to drugs. The carrier composed of H-γ-Glu-Gln-OH has the characteristics of high water solubility and drug-loading capacity, good biocompatibility, low toxicity, improved tumor targeting ability, and anti-tumor efficacy .
|
-
- HY-P1919
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase 369-377, human is a HLA-A2.1-restricted epitope derived from tyrosinase, has been used to develop tumor-targeted vaccines with mixed efficacy .
|
-
- HY-P10239A
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
Tyr3-Octreotate acetate is a somatostatin analog. Tyr3-Octreotate acetate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate acetate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
|
-
- HY-P10239
-
|
|
Somatostatin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
Tyr3-Octreotate is a somatostatin analog. Tyr3-Octreotate exhibits high uptake into tumor, that is capable to be labeled with radioactive metal and thus exhibits antitumor efficacy. Tyr3-Octreotate can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
|
-
- HY-P10925
-
|
FOG-001; I-66
|
β-catenin
|
Cancer
|
|
Zolucatetide (FOG-001;I-66) is a potent β-catenin inhibitor with an IC50 of <50 nM. Zolucatetide can inhibits β-catenin and T-cell factor (TCF) transcription factor interaction. Zolucatetide inhibits cell proliferation and induces cell cycle arrest in target cells. Zolucatetide exhibits anti-tumor efficacy in mice bearing COLO320DM colon cancer cell (with APC, TP53 mutations) xenografts. Zolucatetide can be used for the study of colon cancer .
|
-
- HY-P10925A
-
|
(Z)-FOG-001; I-67
|
β-catenin
|
Cancer
|
|
(Z)-Zolucatetide ((Z)-FOG-001; I-67), a structural isomer of Zolucatetide (HY-P10925), is a potent β-catenin inhibitor with an IC50 of <50 nM. Zolucatetide can inhibits β-catenin and T-cell factor (TCF) transcription factor interaction. Zolucatetide inhibits cell proliferation and induces cell cycle arrest in target cells. Zolucatetide exhibits anti-tumor efficacy in mice bearing COLO320DM colon cancer cell (with APC, TP53 mutations) xenografts. Zolucatetide can be used for the study of colon cancer .
|
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
- HY-P10930A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
wrwycr-NH2 (TFA) is a peptide. wrwycr-NH2 (TFA) is cytotoxic to multiple cancer cells, can induce DNA damage and cell cycle arrest, but does not induce endoplasmic reticulum stress. wrwycr-NH2 (TFA) has anti-tumor activity, and it shows better efficacy when used in combination with DNA-damaging agents .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99320
-
|
OMP 59R5; Anti-Human NOTCH2 Recombinant Antibody
|
Notch
|
Cancer
|
|
Tarextumab (OMP-59R5) is a cross-reactive, fully human IgG2 antibody that selectively inhibits Notch2 and Notch3 signaling. Tarextumab demonstrates broad-spectrum antitumor efficacy in xenograft models of epithelial tumors. Tarextumab can be used for the study of pancreatic cancer .
|
-
- HY-141606
-
|
BAY 94-9343
|
Microtubule/Tubulin
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
|
-
- HY-P99493
-
|
IMGN242; huC242-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (HY-12454). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1 (HY-19792)) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-P99712
-
|
hz208F2-4
|
IGF-1R
Apoptosis
ADC Antibody
|
Cancer
|
|
Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody, serveing as a targeting vector for antibody-drug conjugates (ADCs). Lonigutamab causes G2-M phase cell cycle arrest and increases apoptosis in IGF-1R-overexpressing tumor cells. Lonigutamab demonstrates potent antitumor efficacy in IGF-1R-overexpressing xenograft models. Lonigutamab can be used for the study of Solid tumors with overexpression of IGF-1R and thyroid eye
diseases sup>[2].
|
-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
- HY-P990068
-
|
SRF617
|
NTPDase
|
Inflammation/Immunology
Cancer
|
|
Perenostobart (SRF617) is a human IgG4 antibody with inhibitory activity against CD39 ATPase. Perenostobart inhibits CD39-mediated hydrolysis of extracellular ATP to AMP, with IC50 values of 1.9 nM (HEK293 OE cells), 0.7 nM (MOLP-8 cells), and 1.2 nM (RBC-lysed whole blood). Perenostobart enhances CD4 + T-cell proliferation, promotes dendritic cell maturation, and boosts inflammasome activation in macrophages in the presence of ATP. Perenostobart demonstrates significant single-agent anti-tumor efficacy in MOLP-8 and H520 xenograft models. Perenostobart can be used for the study of cancer .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-113003
-
-
-
- HY-N7694
-
-
-
- HY-N1934
-
-
-
- HY-N3389
-
-
-
- HY-N12044
-
-
-
- HY-126170
-
|
|
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Antibiotic
Bacterial
|
|
Valanimycin is an antibiotic, which inhibits Escherichia coli (BE1121) through interaction with DNA. Valanimycin exhibits cytotoxicity to mouse leukemia L1210, P388/S (doxorubicin (HY-15142A)-sensitive), and P388/ADR (doxorubicin-resistant), with IC50 of 0.79, 2.65, and 1.44 μg/mL, respectively. Valanimycin exhibits antitumor efficacy against ehrlich ascites tumors or L1210 in mice .
|
-
-
- HY-N1934R
-
|
|
Alkaloids
other families
Source classification
Plants
Isoquinoline Alkaloids
|
Reference Standards
Potassium Channel
HSP
|
|
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-157029S
-
|
|
|
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-157031S
-
|
|
|
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-W769206
-
|
|
|
Talaporfin- 13C4, 15N (ME2906 (free acid)- 13C4, 15N) is the 13C- and 15N-labeled Talaporfin (HY-16477A). Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
|
-
-
- HY-W015490S
-
|
|
|
1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone. 1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157029S
-
|
|
|
Alkynes
|
|
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-157031S
-
|
|
|
Alkynes
|
|
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-134813
-
|
|
|
Alkynes
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-115567
-
|
1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
|
|
Nucleoside Analogs
|
|
5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model .
|
-
- HY-154974
-
|
|
|
Cationic Lipids
|
|
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 .
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
![[Asp371]-Tyrosinase (369-377), human](http://file.medchemexpress.eu/product_pic/hy-p1919.gif)
