Search Result
Results for "
Inhibitor
" in MedChemExpress (MCE) Product Catalog:
9938
Inhibitors & Agonists
21
Biochemical Assay Reagents
81
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-16695
-
|
Inhibitor of Mcl-1
|
Bcl-2 Family
|
Cancer
|
|
MIM-1 is an inhibitor of myeloid cell factor 1 (Mcl-1).
|
-
-
- HY-156781
-
|
|
Sirtuin
|
Metabolic Disease
|
|
Sirtuin-1 inhibitor 1 (Compound 8) is an inhibitor of Sirtuin-1 that plays important roles in obesity-induced diabetes and aging-related diseases .
|
-
-
- HY-131005
-
-
-
- HY-162294
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 13 (compound A6) is a c-MYC transcription inhibitor. c-Myc inhibitor 13 selectively stabilizes c-MYC G4 and inhibits G4-associated c-MYC transcription .
|
-
-
- HY-162091
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo .
|
-
-
- HY-169106
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase inhibitor 4 (compound 45) is a potent Topoisomerase1/2 inhibitor. Topoisomerase inhibitor 4 causes cell cycle arrest in the G2/M phase by inducing Apoptosis. Topoisomerase inhibitor 4 has antitumor activity .
|
-
-
- HY-14412
-
|
|
p38 MAPK
|
Cancer
|
|
p38α inhibitor 4 (compound 10) is a selective and allosteric p38α inhibitor with an IC50 value of 1.2 μM. p38α inhibitor 4 exhibits no activity against p38β, p38γ, and p38δ .
|
-
-
- HY-160445
-
|
|
Others
|
Cancer
|
|
KRAS G12D inhibitor 19 (Compound 7) is a KRAS G12D inhibitor. KRAS G12D inhibitor 19 can be used for the research of cancer .
|
-
-
- HY-162971
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-33 (compound 115a) is an inhibitor of pyridopyrimidine kras (IC50 ≤ 100nM) .
|
-
-
- HY-146709
-
-
-
- HY-134929
-
|
|
Hexokinase
|
Infection
Cancer
|
|
Hexokinase 2 inhibitor 1 (Compound 2a) is a hexokinase 2 (HK2) inhibitor with anti-tumor activity and can be used in cancer research .
|
-
-
- HY-161686
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 24 (Compound 11) is a human carbonic anhydrase (carbonic anhydrase) inhibitor. Ki values of Carbonic anhydrase inhibitor 24 for hCAs IX and XII were 10.7 and 7.5 nM, respectively .
|
-
-
- HY-P10066
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 31 (compound 18) is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM .
|
-
-
- HY-145826
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112 .
|
-
-
- HY-160859
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 8 (Example 224) is a WRN helicase inhibitor with IC50 value of 48 nM. WRN inhibitor 8 can be used in cancer research .
|
-
-
- HY-160549
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 14 (Compound 13A) is a c-Myc protein inhibitor. The IC50 value of HL60 inhibitor is <100 nM. c-Myc inhibitor 14 shows antitumor activity .
|
-
-
- HY-154851
-
|
|
GSK-3
CDK
Tau Protein
|
Neurological Disease
|
|
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
|
-
-
- HY-157308
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 10 (compound a8) inhibits the activity of α-Syn aggregation with low IC50 value (1.08 μM). α-Synuclein inhibitor 10 exhibits good binding affinity to α-Syn residues. α-Synuclein inhibitor 10 can be used in the research of Parkinson's disease (PD) .
|
-
-
- HY-164315
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 67 (example 35) is a KRAS G12C inhibitor that selectively inhibits the growth of many KRAS G12C mutant tumor cell lines .
|
-
-
- HY-159611
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 68 (compound I-063) is a KRAS G12C inhibitor with an IC50 of 7 nM. KRAS G12C inhibitor 68 has anti-tumor activity .
|
-
-
- HY-161695
-
|
|
Others
|
Cancer
|
|
Angiogenesis inhibitor 6 (Compound 8) is a non-tyrosine kinase inhibitor with effective antiangiogenic properties. Angiogenesis inhibitor 6 has antitumor activity .
|
-
-
- HY-126388
-
-
-
- HY-163519
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 13 is an inhibitor of α-synuclein (α-Syn). α-Synuclein inhibitor 13 inhibits the aggregation of α-Syn proteins and is able to break down formed fibers. It is mainly used in Parkinson's disease research .
|
-
-
- HY-113571
-
|
|
Tie
|
Cardiovascular Disease
|
|
Tie2 kinase inhibitor 2 (compound 7) is a selective Tie2 kinase inhibitor with an IC50 value of 1 μM. Tie2 kinase inhibitor 2 inhibits endothelial cell tube formation, and can be used for Tie2-mediated angiogenic disorders research .
|
-
-
- HY-163720
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS G12C inhibitor 63 (K45) is a KRAS G12C inhibitor. KRAS G12C inhibitor 63 can induce Apoptosis. KRAS G12C inhibitor 63 has antitumor activity .
|
-
-
- HY-162452
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
|
|
Prolyl endopeptidase inhibitor 2 (Compound 8) was a proline endopeptidase (PEP) inhibitor with IC50 value 31.11 μM. Prolyl endopeptidase inhibitor 2 can be used in the study of neurodegenerative diseases .
|
-
-
- HY-160499
-
-
-
- HY-162804
-
|
|
Bacterial
ATP Synthase
|
Infection
|
|
ATP synthase inhibitor 3 (compound PT6) is an orally active inhibitor of mycobacterial F-ATP synthase (IC50=0.788 μM). ATP synthase inhibitor 3 inhibits the growth of Mycobacterium tuberculosis H37Rv strain (ATCC-27294) in vitro and depletes intracellular ATP levels at an IC50 value of 30μM .
|
-
-
- HY-156819
-
|
KRAS G12D Inhibitor 18
|
Ras
|
Cancer
|
|
RMC-9805 (KRAS G12D inhibitor 18) is a KRAS G12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling to induce apoptosis in KRAS G12D mutant cancer cells .
|
-
-
- HY-157166
-
|
|
EGFR
|
Cancer
|
|
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .
|
-
-
- HY-149636
-
|
|
EGFR
CDK
VEGFR
|
Cancer
|
|
Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
|
-
-
- HY-112569
-
-
-
- HY-142934
-
|
|
ROR
|
Inflammation/Immunology
Cancer
|
|
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC50 of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt .
|
-
-
- HY-142853
-
|
|
Carbonic Anhydrase
|
Endocrinology
|
|
Carbonic anhydrase inhibitor 3 (compound 11g) is a carbonic anhydrase II inhibitor. Carbonic anhydrase inhibitor 3 reduces the intraocular pressure in glaucomatous rabbits .
|
-
-
- HY-142849
-
|
|
Carbonic Anhydrase
|
Endocrinology
|
|
Carbonic anhydrase inhibitor 1 (compound 7c) is a carbonic anhydrase II inhibitor. Carbonic anhydrase inhibitor 3 reduces the intraocular pressure in glaucomatous rabbits .
|
-
-
- HY-157330
-
|
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
P-gp inhibitor 16 (compound 14) is a p-glycoprotein inhibitor. P-gp inhibitor 16 significantly increases Doxorubicin-induced apoptosis and shows anticancer effects .
|
-
-
- HY-45131
-
|
|
Others
|
Metabolic Disease
|
|
Cholesterol absorption inhibitor 1 (compound 21) is a cholesterol absorption inhibitor that reduces liver cholesteryl ester .
|
-
-
- HY-149725
-
|
|
MMP
|
Neurological Disease
|
proMMP-9 selective inhibitor-1 (compound 33) is a highly potent and selective inhibitor of proMMP-9 activation .
|
-
-
- HY-163322
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-A inhibitor 2 (compound HT4) is a monoamine oxidase A (MAO-A) inhibitor with an IC50 of 14.3 µM. MAO-A inhibitor 2 shows a less effect on MAO-B (IC50 of 106 µM) and shows almost ineffective on xanthine oxidase (XO). MAO-A inhibitor 2 can be used for the neurodegenerative disorders and oxidative stress research .
|
-
-
- HY-142460
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1) .
|
-
-
- HY-142458
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737) .
|
-
-
- HY-142457
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737) .
|
-
-
- HY-148899
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 10 (compound 43) is a relatively strong MCL-1 inhibitor (IC50=0.67 μM). Mcl-1 inhibitor 10 interacts with specific binding sites of MCL-1 protein to block the pro-survival signal of MCL-1 and push cancer cells into apoptosis. Mcl-1 inhibitor 10 can be used in the study of MCL-1 dependent cancers .
|
-
-
- HY-162854
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
Diacylglycerol acyltransferase inhibitor-2 (Example 8) is an inhibitor of Diacylglycerol Acyl Transferase 2 (DGAT2) with an IC50 value of 3.7 nM .
|
-
-
- HY-162447
-
|
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase .
|
-
-
- HY-115880
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 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-162799
-
|
|
Others
|
Cancer
|
|
ChoKα inhibitor-6 (compound Fa22) is a less specific ChoKα1 inhibitor with antitumor activity .
|
-
-
- HY-162800
-
|
|
Others
|
Cancer
|
|
ChoKα inhibitor-7 (compound PL48) is a less specific ChoKα1 inhibitor with antitumor activity .
|
-
-
- HY-119374
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity .
|
-
-
- HY-118933
-
|
SJA6017
|
Proteasome
|
Others
|
|
Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract .
|
-
- HY-118712
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor WYE-23 is a mTOR inhibitor, and IC50 is 0.45 nM. It is selective to PI3Kα and IC50 is 661 nM. mTOR inhibitor WYE-23 has antitumor activity .
|
-
- HY-112546
-
|
|
MMP
|
Cancer
|
|
MMP-2 Inhibitor I (OA-Hy) is a potent MMP-2 inhibitor with a Ki of 1.7 μM .
|
-
- HY-152156
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
|
-
- HY-115880A
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146) . KRAS G12D inhibitor 3 (TFA) 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-163362
-
|
|
Reverse Transcriptase
PKC
HIV
|
Infection
|
|
HIV-1 inhibitor-65 (compound 3c) is an inhibitor of HIV-1 (EC50: 2.9 nM) and an activator of protein kinase C (PKC). HIV-1 inhibitor-65 inhibits syncytium formation (EC50: 7.0 nM) and inhibits HIV-1 entry and HIV-1 reverse transcriptase .
|
-
- HY-168079
-
|
|
GSK-3
Tau Protein
|
Neurological Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3β inhibitor (IC50=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitory activities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease .
|
-
- HY-146739
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research .
|
-
- HY-P5989
-
|
Mu-Val-HPh-FMK
|
Antibiotic
|
Infection
|
|
Calpain inhibitor V (Mu-Val-HPh-FMK) is a cell-permeable and irreversible inhibitor of calpain that has anti-chlamydial activity .
|
-
- HY-154986
-
|
|
MARK
AMPK
|
Cancer
|
|
MARK4 inhibitor 2 is an inhibitor of microtubule affinity-regulating kinase 4 (MARK4) with an Km of 6.3×10 7 and an IC50 of 0.82 μM. MARK4 inhibitor 2 inhibits the growth of human cells and can be used for cancer research .
|
-
- HY-163145
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
|
-
- HY-163118
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 17 (compound 4c) is an inhibitor of thiazolopyrimidine topoisomerase (Topoisomerase) Top II (IC50: 0.23 μM). Topoisomerase II inhibitor 17 can significantly cause cell cycle disruption and apoptosis .
|
-
- HY-147705
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects .
|
-
- HY-149524
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 8 (compound 10) is a competitive inhibitor (IC50: 5.38 μM) of sirtuin SIRT5 with anticancer potential .
|
-
- HY-149525
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 9 (compound 14) is a competitive inhibitor (IC50: 4.07 μM) of sirtuin SIRT5 with anticancer potential .
|
-
- HY-160708
-
|
|
Tie
|
Cancer
|
|
Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .
|
-
- HY-149856
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research .
|
-
- HY-149350
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT .
|
-
- HY-149694
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora Kinase Inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth .
|
-
- HY-115999
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines .
|
-
- HY-142467
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-11, a fused pyridine ring derivative, is a HIV-1 inhibitor. WO2021104413A1 ( compound 1-1b) .
|
-
- HY-112412
-
|
PDGF Receptor Tyrosine Kinase Inhibitor III
|
PDGFR
|
Neurological Disease
|
|
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis .
|
-
- HY-119423
-
|
|
MMP
|
Cancer
|
|
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively .
|
-
- HY-155090
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity .
|
-
- HY-155029
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-16 is a soluble epoxide hydrolase (sEH) inhibitors with an IC50 of 2 nM. sEH inhibitor-16 reduces the inflammatory damage in Cerulein (HY-A0190)-induced acute pancreatitis (AP) in mice and can be used for inflammation/immunology research .
|
-
- HY-155138
-
|
|
Glutaminase
|
Metabolic Disease
Cancer
|
|
GLS1 Inhibitor-7 (compound 4d) is a GLS1 inhibitor (IC50=46.7 μM), with potential anti-cancer, anti-aging and anti-obesity properties .
|
-
- HY-103271
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro .
|
-
- HY-154852
-
|
|
GSK-3
CDK
|
Neurological Disease
|
|
GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies .
|
-
- HY-143280
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-149018
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) with IC50 of 218 nM but lost its inhibitory activity of LPAR1 .
|
-
- HY-161354
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .
|
-
- HY-143235
-
|
|
Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
|
-
- HY-P10072A
-
|
Hsp25 kinase Inhibitor acetate; Mk2 pseudosubstrate acetate
|
JNK
HSP
MAPKAPK2 (MK2)
p38 MAPK
ERK
|
Others
|
|
MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-138222
-
|
WHI-P131 hydrochloride; Jak3 Inhibitor I hydrochloride
|
JAK
|
Cancer
|
|
JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3 inhibitor (Ki=2.3 μM). JANEX-1 hydrochloride shows potent JAK3 inhibitory activity (IC50=78 μM), does not inhibit JAK1 and JAK2 .
|
-
- HY-P10072
-
|
Hsp25 kinase Inhibitor; Mk2 pseudosubstrate
|
ERK
JNK
p38 MAPK
HSP
MAPKAPK2 (MK2)
|
Others
|
|
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-143721
-
|
|
Monoamine Oxidase
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
SSAO inhibitor-2 (Compound 1) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 10-100 μM for human SSAO and MAO-A, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc .
|
-
- HY-143723
-
|
|
Monoamine Oxidase
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc .
|
-
- HY-70005
-
|
Carboxypeptidase Inhibitor
|
Carboxypeptidase
|
Metabolic Disease
|
|
CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a Ki of 0.32 μM .
|
-
- HY-136121
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM .
|
-
- HY-136123
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM .
|
-
- HY-136122
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM .
|
-
- HY-151996
-
|
|
Microtubule/Tubulin
|
Cardiovascular Disease
|
|
Tubulin inhibitor 31 is a potent tubulin inhibitor with an IC50 value of 4 µM. Tubulin inhibitor 31 shows anti-proliferative activity. Tubulin inhibitor 31 inhibits the HUVEC migration .
|
-
- HY-147891
-
|
|
Apoptosis
|
Cancer
|
|
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos .
|
-
- HY-147890
-
|
|
Apoptosis
|
Cancer
|
|
Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos .
|
-
- HY-156554
-
|
|
Raf
|
Cancer
|
|
Raf inhibitor 3 (Example 30) is a Raf inhibitor. Raf inhibitor 3 inhibits B-Raf and C-Raf with IC50 values less than 15 nM. Raf inhibitor 3 can be used for research of cancers .
|
-
- HY-146711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity .
|
-
- HY-145821
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells .
|
-
- HY-145822
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells .
|
-
- HY-128403
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM .
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-115956
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases .
|
-
- HY-168187
-
|
|
Src
|
Cancer
|
|
Src Inhibitor 3 (Compound 7d) is a Src inhibitor with an IC50 of 285 nM. Src Inhibitor 3 inhibits HepG2 cells proliferative with an IC50 of 1.55 μM .
|
-
- HY-118371
-
|
|
Arginase
|
Cancer
|
|
Arginase inhibitor 2 is an Arginase inhibitor (Page 130 in reference patent). Arginase inhibitor 2 synergizes with adoptively transferred antigen- specific T cells to inhibit tumor growth .
|
-
- HY-153159
-
|
|
Others
|
Cancer
|
|
Angiogenesis inhibitor 4 is a potent angiogenesis inhibitor. Angiogenesis inhibitor 4 can be used in research of cancer .
|
-
- HY-144818
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia .
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
|
-
- HY-115957
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 19 (compound 9b) is a potent inhibitor of tubulin. Tubulin inhibitor 19 is an indole chalcone compound. Tubulin inhibitor 19 has the potential for the research of cancer diseases .
|
-
- HY-151983
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant .
|
-
- HY-114199
-
-
- HY-49066
-
-
- HY-153692
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 1 (example 7) is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity. WRN inhibitor 1 has the potential to study cancer .
|
-
- HY-160854
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 43 (Compound 29) has significant antitumor activity. Tubulin inhibitor 43 inhibits the proliferation and growth of cancer cells by inhibiting the activity of β-microtubulin, and finally induces apoptosis .
|
-
- HY-161386
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 7 (Compound h6) is a WRN inhibitor. WRN inhibitor 7 effectively inhibits WRN's helicase and ATPase activity (IC50: 9.8 μM and 15.8 μM respectively). WRN inhibitor 7 can be used for research of microsatellite instable (MSI) cancers .
|
-
- HY-163797
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
|
-
- HY-168560
-
|
|
MMP
|
Cancer
|
|
MMP Inhibitor 4 (compound 4 B) is a potent MMP inhibitor. MMP Inhibitor 4 shows antiproliferative activity. MMP Inhibitor 4 induces cell cycle arrest at subG1 phase. MMP Inhibitor 4 decreases the mRNA expression of MMP2, MMP9 and VEGFA .
|
-
- HY-163195
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 40 (compound 45) is a tubulin inhibitor with IC50 of 1.2 μM. Tubulin inhibitor 40 shows selective cytotoxicity towards cancer cells. Tubulin inhibitor 40 processes antitumor activity .
|
-
- HY-162625
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 47 (compound C11) is a potent tubulin inhibitor. Tubulin inhibitor 47 induces apoptosis and cell cycle arrest at the M phase. Tubulin inhibitor 47 shows anti-tumor activity .
|
-
- HY-115958
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 20 (compound 1) is a potent inhibitor of tubulin. Tubulin inhibitor 20 has the potential for the research of cancer diseases .
|
-
- HY-162101
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase inhibitor 3 (compound 9) is a potent Topoisomerase inhibitor. Topoisomerase inhibitor 3 shows antiproliferative and anti-tumor activity .
|
-
- HY-128617
-
|
|
Legumain
|
Cancer
|
|
Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research .
|
-
- HY-144766
-
|
|
Apoptosis
|
Cancer
|
|
ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation .
|
-
- HY-147888
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site .
|
-
- HY-161075
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 8 (MP-HJ-1b) is a potent inhibitor of microtubule. Microtubule inhibitor 8 triggers cell death through ferroptosis. Microtubule inhibitor 8 has anti-tumor effect .
|
-
- HY-145820
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features .
|
-
- HY-151879
-
-
- HY-112607
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis .
|
-
- HY-143251
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 13 (E27) is a potent tubulin inhibitor with an IC50 value of 16.1 μM for the tubulin polymerization inhibition. Tubulin inhibitor 13 inhibits migration and invasion of cancer cells, induces apoptosis and has anticancer activity .
|
-
- HY-143420
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model .
|
-
- HY-147727
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization .
|
-
- HY-147726
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
|
-
- HY-146205
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis .
|
-
- HY-132196
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities .
|
-
- HY-142644
-
-
- HY-143730
-
|
|
Btk
|
Cancer
|
|
BTK inhibitor 20 is a potent BTK inhibitor with an IC50 of 8 nM .
|
-
- HY-168592
-
-
- HY-157954
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
WRN inhibitor 6 (compound 3ci) is a potent WRN inhibitor. WRN inhibitor 6 induces apoptosis. WRN inhibitor 6 increases the expression of p-p53, P-Chk2, γH2AX expression .
|
-
- HY-10217
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2.
Thrombin Inhibitor 2 has antithrombotic activity .
|
-
- HY-131705
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research .
|
-
- HY-152150
-
|
|
Others
|
Metabolic Disease
|
|
Thrombin inhibitor 7 is a potent FXIIa inhibitor with IC50 values of 28 nM, >132 µM for FXIIa and FXIa, respectively. Thrombin inhibitor 7 shows low cytotoxicity .
|
-
- HY-146672
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
|
-
- HY-148838
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research .
|
-
- HY-149364
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 34 (compound b5) is a potent anticancer agent. Tubulin inhibitor 34 can inhibit tubulin polymerization and induce G2/M arrest and apoptosis. Tubulin inhibitor 34 exhibits significant antivascular and antitumor activity .
|
-
- HY-146889
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 μM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-146890
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 μM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-144817
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 27 (DYT-1) is a tubulin polymerisation inhibitor with an IC50 of 25.6 µM. Tubulin inhibitor 27 shows anti-angiogenesis and antitumor activities .
|
-
- HY-161061
-
|
|
Arginase
|
Cancer
|
|
Arginase inhibitor 7 (compound A17) is an arginase (ARG1) inhibitor, with an IC50 of 0.16 μM. Arginase inhibitor 7 has high oral bioavailability .
|
-
- HY-163637
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
Sodium Channel inhibitor 5 (compound 7d) is a potent inhibitor of sodium channel, with the IC50 of 2.7 μM. Sodium Channel inhibitor 5 plays an important role in antiarrhythmic research .
|
-
- HY-149375
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 37 (Compound 12) is a Tubulin inhibitor that can effectively inhibit Tubulin aggregation (IC50=1.3 µM). Tubulin inhibitor 37 exhibits antiproliferative activity against human tumor cell lines and has potential for studying cancer .
|
-
- HY-161747
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 46 (Compound 21) is a potent tubulin assembly inhibitor. Tubulin inhibitor 46 has antiproliferative activities, with GI50 values of 0.0095-33 μM for cancer and non-cancerous cells. Tubulin inhibitor 46 can be used for the reserch of cancer .
|
-
- HY-153745
-
|
|
Trk Receptor
|
Cancer
|
|
Protein kinase inhibitor 5 is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 inhibits cell viability .
|
-
- HY-153692A
-
|
|
Biochemical Assay Reagents
|
Others
|
|
(R)-WRN inhibitor 1 is the R-isomer of WRN inhibitor 1 (example 7). WRN inhibitor 1 is a WRN inhibitor with anticancer activity .
|
-
- HY-15357
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM) .
|
-
- HY-15358
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM) .
|
-
- HY-144748
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 17 (Compound 3b) is a tubulin polymerization inhibitor with an IC50 of 12.38 µM. Tubulin inhibitor 17 has anticancer activities and induces cell apoptosis .
|
-
- HY-139881
-
|
|
Btk
|
Cancer
|
|
BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
|
-
- HY-142296
-
-
- HY-161734
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 11 (compound 33) is a microtubule inhibitor with a mechanism of action similar to colchicine (HY-N0282). Microtubule inhibitor 11 can be used in cancer-related research .
|
-
- HY-146778
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis .
|
-
- HY-W013478
-
|
|
Phosphatase
|
Cancer
|
|
PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect .
|
-
- HY-146122
-
-
- HY-146124
-
-
- HY-161721
-
|
|
Cathepsin
|
Cancer
|
|
Cathepsin Inhibitor 4 (Compound 45) is a selective inhibitor for Cathepsin S with Ki of 0.04 nM .
|
-
- HY-161153
-
|
|
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 9 (Compound O-7) is a 2-Aryl-1H-benzo [d] imidazole derivative with in vitro anticancer activity. Microtubule inhibitor 9 can induce cell cycle arrest at the G2/M phase and early apoptosis. Microtubule inhibitor 9 inhibits cancer cell migration by inhibiting wound healing and colony formation .
|
-
- HY-162879
-
|
|
FAK
Src
Akt
Autophagy
|
Cancer
|
FAK inhibitor 7 is a type of FAK inhibitor with an IC50 value of 3.58 nM. FAK inhibitor 7 can inhibit the downstream signaling cascades of FAK (like Src and AKT), causing ovarian cancer cells to stall in the G0/G1 phase and induce cytotoxic autophagy. FAK inhibitor 7 can also suppress tumor metastasis and growth in ovarian cancer mice .
|
-
- HY-143250
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity .
|
-
- HY-156579
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 3 (example 110), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 3 can be used for the research of cancer .
|
-
- HY-156580
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 4 (example 107), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 4 can be used for the research of cancer .
|
-
- HY-156581
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 5 (example 157), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 5 can be used for the research 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-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
|
-
- HY-13278A
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.
|
-
- HY-P4028
-
|
|
Virus Protease
|
Infection
|
|
Herpes virus inhibitor 1 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 1 inhibits viral replication .
|
-
- HY-P4030
-
|
|
HIV Protease
|
Infection
|
|
Herpes virus inhibitor 2 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 2 inhibits viral replication .
|
-
- HY-148839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research .
|
-
- HY-149374
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 36 (Compound 10) is a novel and potent tubulin inhibitor and inhibits the polymerization of microtubular protein then induces apoptosis with an IC50 value of 1.5±0.1 μM. Tubulin inhibitor 36 (Compound 10) has significant anti-mitotic effect and exhibits activities against glioblastoma cells. Tubulin inhibitor 36 (Compound 10) has anti-tumor effects and can be used for glioblastoma multiforme (GBM) research .
|
-
- HY-124638
-
|
|
MNK
|
Cancer
|
|
MNK inhibitor 9 is a potent and selective inhibitor of MNK1/2 with IC50 values of 0.003 µM and 0.003 µM for MNK1 and MNK2 respectively. MNK inhibitor 9 has good cell permeability. MNK inhibitor 9 can be used in tumor related research .
|
-
- HY-125997
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment .
|
-
- HY-147887
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells .
|
-
- HY-148037
-
|
|
Proteasome
|
Cardiovascular Disease
|
|
Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism .
|
-
- HY-13276
-
-
- HY-119938
-
|
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 1 is a potent and non-cytotoxic trypanosoma brucei growth inhibitor with an EC50 of 5 nM .
|
-
- HY-112913
-
-
- HY-146123
-
-
- HY-162109
-
-
- HY-168583
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 11 (Example 17) is an orally active inhibitor of WRN helicase, with the IC50 of 63 nM .
|
-
- HY-156130
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth .
|
-
- HY-154987
-
|
|
MARK
|
Cancer
|
|
MAPK4 inhibitor 3 (compound 23b) is an inhibitor of MAPK4 with an IC50 value of 1.01 μM. MAPK4 inhibitor 3 inhibits cancer cells growth. MAPK4 inhibitor 3 can be used for research on cancer and tauopathies .
|
-
- HY-143419
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 14 (compound 4), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 0.41 nM. ATX inhibitor 14 has the potential for fibrosis relevant diseases research .
|
-
- HY-160169
-
-
- HY-162593
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 45 (compound 5) is an inhibitor of tubulin protein active sites. Tubulin inhibitor 45 against MCF7 and HePG2 cancer cells with IC50 values of 11 μM and 13 μM .
|
-
- HY-156013
-
-
- HY-157315
-
|
|
Bacterial
|
Infection
|
|
21272541 is a potent inhibitor of FabI protein. 21272541 significantly inhibits the infections caused by Gram-negative organisms .
|
-
- HY-162341
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I with anticancer activity. Topoisomerase I inhibitor 15 inhibits A549 cells with an IC50 of 7.34 μM .
|
-
- HY-124793
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 .
|
-
- HY-124793A
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2 .
|
-
- HY-10439
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX .
|
-
- HY-147725
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization .
|
-
- HY-143237
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research .
|
-
- HY-144647
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SP inhibitor 1 (compound 34) is a selective SARS-CoV-2 spike protein (SP) inhibitor with an IC50 of 3.26 μM, >25 μM, >25 μM for SP, M pro and PL pro protein, respectively. SP inhibitor 1 is a vitro SARS-CoV-2 replication inhibitor at non-toxic concentrations (0.3250<5.98 μM). SP inhibitor 1 shows cellular antiviral activity .
|
-
- HY-156969
-
|
|
Topoisomerase
Btk
|
Cancer
|
|
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK .
|
-
- HY-146387
-
|
|
Sirtuin
|
Neurological Disease
Cancer
|
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases .
|
-
- HY-149989
-
|
|
Ack1
Akt
|
Cancer
|
|
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity .
|
-
- HY-153970
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research .
|
-
- HY-15775
-
|
|
Arginase
|
Cancer
|
|
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
|
-
- HY-111506
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively .
|
-
- HY-U00377
-
-
- HY-13278
-
-
- HY-18928
-
|
|
FAK
|
Cancer
|
|
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range .
|
-
- HY-143581
-
-
- HY-153661
-
-
- HY-143583
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
Cancer
|
|
ATX inhibitor 10 is a potent inhibitor of ATX. ATX inhibitor 10 is s nitrogen-containing heterocyclic compound. ATX plays a role in causing pathological conditions including fibrosis, arthritis, neurodegeneration, neuropathic pain, and cancer. ATX inhibitor 10 has the potential for the research of ATX related diseases (extracted from patent WO2021115375A1, compound 35) .
|
-
- HY-146662
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
|
-
- HY-152214
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor .
|
-
- HY-P2166
-
|
|
MMP
|
Cancer
|
|
MMP3 inhibitor 3 is an inhibitor of MMP3. MMP3 inhibitor 3 can used to study breast cancer .
|
-
- HY-109574
-
|
|
Raf
|
Cancer
|
|
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research .
|
-
- HY-133019
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently .
|
-
- HY-47026
-
|
|
Others
|
Others
|
|
Protein kinase inhibitor 6 is a protein kinase inhibitor.
|
-
- HY-163431
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1 .
|
-
- HY-13280
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC50 of 160 nM.
|
-
- HY-130255
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM .
|
-
- HY-132884
-
|
|
Others
|
Cancer
|
|
TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
|
-
- HY-163093
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 24 is a potent ATX inhibitor with IC50 of 7.51±0.72 nM that has anti-tumor effect .
|
-
- HY-153750
-
|
|
Wnt
|
Cancer
|
|
Wnt pathway inhibitor 3 is a potent wnt inhibitor with an IC50 value of 45 nM. Wnt pathway inhibitor 3 shows antiproliferative activity .
|
-
- HY-160215
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGF-βRI inhibitor 1 (compoimd i) is a TGF-βRI inhibitor. TGF-βRI inhibitor 1 can be used for cancer research .
|
-
- HY-W028145
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGF-βRI inhibitor 2 (compound 13) is a TGF-βRI inhibitor. TGF-βRI inhibitor 2 can be used in cancer research .
|
-
- HY-144797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction .
|
-
- 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-144774
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
|
-
- HY-153401
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis .
|
-
- HY-153594
-
-
- HY-144366
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .
|
-
- HY-147761
-
|
|
Antibiotic
Flavivirus
Dengue virus
|
Infection
|
|
GAK inhibitor 2 (Compound 14g) is a potent cyclin G-associated kinase (GAK) inhibitor with an IC50 of 0.024 μM. GAK inhibitor 2 shows antiviral activity with an EC50 of 1.049 μM against dengue virus (DENV) .
|
-
- HY-153706
-
-
- HY-111489B
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-126134
-
-
- HY-U00370
-
-
- HY-111489A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP inhibitor 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-111489
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-160170
-
|
|
Necroptosis
|
Cancer
|
|
Necrosis inhibitor 3 (compound B3) is a poteng inhibitor of necrosis, with the IC50 value of 0.29 nM in HT29 cells .
|
