Search Result
Results for "
Nanomolar
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-12607
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Parasite
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Infection
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ML251, a potent nanomolar T. brucei and T. cruzi phosphofructokinase (PFK) inhibitor, inhibits T. brucei PFK (IC50=0.37 μM) and T. cruzi PFK (IC50=0.13 μM). ML251 can be used for the research of parasite .
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- HY-141520
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ART558
Maximum Cited Publications
19 Publications Verification
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DNA/RNA Synthesis
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Cancer
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ART558 is a nanomolar potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer .
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- HY-138649
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Others
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Neurological Disease
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PB2 is a tris(2-carboxyethyl)phosphine (TCEP) analogue increasing retinal ganglion (RGCs) cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB2 is substantially more permeable than TCEP. PB2, as a reducing agent, is highly neuroprotective for RGCs .
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- HY-132298
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Adenylate Cyclase
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Others
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TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound .
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- HY-138648
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Others
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Neurological Disease
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PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
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- HY-108579
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Potassium Channel
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Cardiovascular Disease
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UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness .
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- HY-130613
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Bacterial
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Infection
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MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA) .
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- HY-145823
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EGFR
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Cancer
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EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .
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- HY-145824
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EGFR
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Cancer
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EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .
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- HY-146229
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VEGFR
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Cancer
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VEGFR-2-IN-25 (compound 5d) is a highly potent VEGFR-2 inhibitor with an IC50 value of 12.1 nM. VEGFR-2-IN-25 can be used for researching anticancer .
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- HY-139625
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Microtubule/Tubulin
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Cancer
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Dolastatinol is a synthetic analog of dolastatin 10 and low nanomolar inhibitor of tubulin polymerization.
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- HY-137392
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1-Naphthalenesulfonyl-Ile-Trp-CHO
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Cathepsin
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Others
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Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations .
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- HY-142253
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HIV
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Infection
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HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
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- HY-135727
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EGFR
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Cancer
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PF-6422899 is an inhibitor for EGFR, that it selectively binds to EGFR and SOAT1 in nanomolar levels .
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- HY-114361
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- HY-132868
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Others
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Others
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SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with nanomolar potency.
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- HY-18287
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Smo
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Cancer
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MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
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- HY-139832
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PI3K
mTOR
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Cancer
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MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.
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- HY-133735
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RABV
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Infection
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GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains .
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- HY-132906
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Parasite
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Infection
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Antimalarial agent 3 shows nanomolar antiplasmodial activity (IC50 = 0.035 μM) and has a very high selectivity index with respect to mammalian cells.
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- HY-18622
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Src
FGFR
PDGFR
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Cancer
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PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.
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- HY-N3755
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Estrogen Receptor/ERR
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Cancer
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Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .
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- HY-141495
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- HY-114388
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QM385
2 Publications Verification
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Others
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Inflammation/Immunology
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QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability .
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- HY-132170
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Dihydroorotate Dehydrogenase
Parasite
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Infection
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DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs .
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- HY-141841
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SARS-CoV
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Infection
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SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.
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- HY-139631
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HIV
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Infection
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HIV-1 inhibitor-9 is found to be potent inhibitor against the wild-type (WT) HIV-1 strain or multiple NNRTI-resistant strains at low nanomolar levels.
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- HY-143465
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Cholinesterase (ChE)
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Neurological Disease
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BChE-IN-5 is a potent and selective BChE inhibitor of hBChE over hAChE with an IC50 of 2.8 nM for BChE. BChE-IN-5 has the potential for the research of alzheimer’s disease .
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- HY-112862
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Aminoacyl-tRNA Synthetase
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Infection
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Arg-AMS (compound 24) is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes .
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- HY-146214
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CDK
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Cancer
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As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
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- HY-146441
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STAT
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Cardiovascular Disease
Inflammation/Immunology
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Prohibitin ligand 1 (Compound 22i), a cardioprotectant prohibitin ligand, induces a phosphorylation of the pro-survival factor STAT3. Prohibitin ligand 1 exhibits in vitro cardioprotectant activities at nanomolar concentrations .
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- HY-12866
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LOXO-101; ARRY-470
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Trk Receptor
Apoptosis
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Cancer
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Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
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- HY-120530
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mGluR
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Neurological Disease
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JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71) .
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- HY-101213
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OSW-1
2 Publications Verification
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Others
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Cancer
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OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
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- HY-133735A
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RABV
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Infection
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GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein .
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- HY-132171
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Dihydroorotate Dehydrogenase
Parasite
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Infection
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DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound .
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- HY-145304
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- HY-156401
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Epigenetic Reader Domain
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Cancer
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BRD9 Degrader-1 is a BRD9 degrader. BRD9 Degrader-1 exhibits micromolar binding affinity to BRD9 and nanomolar affinity for the ternary complex with BRD9 and VCB .
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- HY-156402
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Topoisomerase
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Cancer
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AuM1Gly is a topoisomerase I inhibitor. AuM1Gly affects the growth of MDA-MB-231 breast cancer cells, with IC50?values in the low nanomolar range .
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- HY-164005
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- HY-50001
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Influenza Virus
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Infection
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Nucleozin, a potent inhibitor of influenza A virus infection, induces the formation of nucleoprotein (NP) aggregates and antagonizes its nuclear accumulation, leading to cessation of viral replication. Nucleozin impedes influenza A virus replication in vitro with a nanomolar EC50 .
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- HY-118438
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Aryl Hydrocarbon Receptor
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Inflammation/Immunology
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10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations .
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- HY-156175
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-156176
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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TLR7 agonist 15 (compound 16b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 15 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-156177
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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TLR7 agonist 16 (compound 16d) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-102074
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Others
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Infection
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ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency. .
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- HY-122025
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Androgen Receptor
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Metabolic Disease
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AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .
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- HY-101124
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KAR5585
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Tryptophan Hydroxylase
5-HT Receptor
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Cardiovascular Disease
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Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH) .
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- HY-118423
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IQP-0410
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HIV
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Inflammation/Immunology
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SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase . SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism .
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- HY-163727
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Parasite
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Infection
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MMV1557817 is an orally active and potent antimalarial compound. MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum and Plasmodium vivax aminopeptidases M1 and M17, leading to inhibition of end-stage hemoglobin digestion in asexual parasites .
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- HY-119361
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(Rac)-Deoxysappanone B 7,4' dimethyl ether
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Microtubule/Tubulin
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Cancer
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(Rac)-Deox B 7,4, a homoisoflavanoid compound, inhibits microtubule polymerization via binding near the colchicine site and promote reversible G2 arrest. (Rac)-Deox B 7,4 possesses nanomolar anti-leukemic activity .
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- HY-135845
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CH0793011
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Topoisomerase
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Cancer
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TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38 . TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro .
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- HY-115555
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Phosphodiesterase (PDE)
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Cancer
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K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM .
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- HY-155149
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Methionine Adenosyltransferase (MAT)
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Cancer
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MAT2A Allosteric inhibitor 2 is a potent and selective MAT2A allosteric inhibitor with an IC50 of 5 nM. MAT2A Allosteric inhibitor 2 shows nanomolar activity (IC50=5 μM) in the the proliferation assay (MTAP -/- cell line) .
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- HY-147728
-
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-147724
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-12866A
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LOXO-101 sulfate; ARRY-470 sulfate
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Trk Receptor
Apoptosis
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Cancer
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Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
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- HY-18932
-
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ERK
Apoptosis
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Cancer
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DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
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- HY-126973
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HCV Protease
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Infection
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BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity .
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- HY-153534
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MicroRNA
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Cancer
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microRNA-21-IN-3 (compound 45) can specifically bind to the precursor of oncogenic and pro-inflammatory microRNA-21 with medium nanomolar affinity, reduce cancer cell proliferation and miR-21 levels, and can be used in antitumor research .
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- HY-154854
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Histone Methyltransferase
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Cancer
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BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research .
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- HY-126275
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ROCK
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Cancer
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HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity .
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- HY-P0039
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Bombesin Receptor
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Cancer
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BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. BIM-26226 inhibits BN- or GRP-stimulated amylase release with IC50s in the nanomolar range. BIM-26226 can be used for the research of cancer .
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- HY-161096
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ROR
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Cancer
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Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
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- HY-163442A
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Pim
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Cancer
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PIM3-IN-1 hydrochloride (Compound 19a) is an inhibitor of (PIM2/3), with the highest inhibition level being against PIM3, having an IC50 value in the nanomolar range. PIM3-IN-1 hydrochloride can be used in cancer research .
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- HY-120757
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Others
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Others
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LP-130 is a statin-based inhibitor that is a universal inhibitor with nanomolar inhibitory activity against all tested retroviral proteases. Crystal structure studies of its binding to different retroviral proteases have shown that it can adapt to different active site regions to achieve inhibition.
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- HY-101634
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HCV
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Infection
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ABT-072 is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
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- HY-101634A
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HCV
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Infection
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ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM) .
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- HY-14776
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CX-3543
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DNA/RNA Synthesis
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Cancer
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Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template .
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- HY-135147
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ONC206
2 Publications Verification
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Dopamine Receptor
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Neurological Disease
Cancer
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ONC206 is an analogue of TRAIL inducer ONC201 . ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity .
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- HY-116042
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Adenosine Receptor
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Cardiovascular Disease
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FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium .
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- HY-19509
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Reverse Transcriptase
HIV
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Infection
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IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM .
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- HY-149805
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Apoptosis
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Cancer
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Anticancer agent 110 is an anticancer agent with in vitro anticancer activity and excellent anti-leukemia potency. Anticancer agent 110 is highly cytotoxic to K-562 lineage chronic myelogenous leukemia cells at nanomolar concentrations. Anticancer agent 110 causes DNA damage and leads to apoptosis .
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- HY-12866R
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Trk Receptor
Apoptosis
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Cancer
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Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
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- HY-P2274
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Parasite
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Infection
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Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
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- HY-132171A
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Dihydroorotate Dehydrogenase
Parasite
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Infection
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DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC50=95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs .
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- HY-162763
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Apoptosis
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Cancer
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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 .
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- HY-16978
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- HY-50055
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Others
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Cancer
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EtDO-P4 is a nanomolar inhibitor of glycosphingolipid (GSL) synthesis. EtDO-P4 suppresses activation of the EGFR-induced ERK pathway and various receptor tyrosine kinases (RTKs). EtDO-P4 can be used for various types of cancer, including Burkitt’s lymphoma .
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- HY-139293
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Others
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Cardiovascular Disease
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PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research .
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- HY-155840
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HDAC
Apoptosis
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Cancer
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KH16 is a potent and low nanomolar HDAC inhibitor. KH16 is against class I HDACs HDAC1, HDAC2, and HDAC3, with IC50 ?values ranging from 6 to 34 nM. KH16 induces cell apoptosis and is against tumor cells with various gene expression patterns .
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- HY-156060
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Toll-like Receptor (TLR)
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Inflammation/Immunology
|
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NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
|
-
- HY-127106
-
|
|
Potassium Channel
|
Neurological Disease
|
|
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration .
|
-
- HY-149928
-
|
|
HIV
|
Infection
|
|
NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor featuring significantly anti-resistance efficacy. NNRTIs-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRTIs-IN-1 displays favorable pharmacokinetic properties .
|
-
- HY-19928
-
|
EW-7197; TEW-7197
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect .
|
-
- HY-19928A
-
|
EW-7197 Hydrochloride; TEW-7197 Hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect .
|
-
- HY-124069
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .
|
-
- HY-149292
-
|
|
Casein Kinase
|
Cancer
|
|
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
|
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-P5914
-
|
WaTx
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-156442
-
|
|
Lactate Dehydrogenase
|
Infection
|
|
MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication .
|
-
- HY-129334
-
|
|
Telomerase
|
Cancer
|
|
Macrocalin B is a diterpenoid, which can be isolated from Isodon xerophilus. Macrocalin B inhibits the proliferation of cancer cells K562, HL-60, A549, MKN, CA and HCT with IC50 of 2.81-171 μM. Macrocalin B inhibits the telomerase in K562 with an IC50 in nanomolar level .
|
-
- HY-147663
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Compounds 6b and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6k was effective on HCA XII. Compounds 6b, 14g and 6k can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
|
-
- HY-163537
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
|
-
- HY-130492
-
ARCC-4
1 Publications Verification
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .
|
-
- HY-10293
-
|
INCB007839; INCB7839
|
MMP
|
Cancer
|
|
Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al .
|
-
- HY-145733
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage .
|
-
- HY-153333
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .
|
-
- HY-157416
-
|
|
Others
|
Metabolic Disease
|
|
COP1-ATGL modulator 1 (86) is an orally active modulator for COP1-ATGL axis. COP1-ATGL modulator 1 (86) could increase ATGL protein expression, reduce ATGL ubiquitination and COP1 autoubiquitination, and diminish lipid accumulation in hepatocytes in the nanomolar range .
|
-
- HY-161768
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC50 of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model .
|
-
- HY-131904
-
POMHEX
2 Publications Verification
|
Enolase
Apoptosis
|
Metabolic Disease
Cancer
|
|
POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) proagent of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor .
|
-
- HY-14891
-
|
GSK2248761; FDV
|
HIV
Reverse Transcriptase
|
Infection
|
|
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates .
|
-
- HY-156406
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PITCOIN4 is a highly selective Class II Alpha PI3K-C2α inhibitor. PITCOIN4 shows nanomolar inhibition of PI3K-C2α and >100-fold selectivity in a general kinase panel .
|
-
- HY-106100
-
|
EMD 49980
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor. Antipsychotic and antidepressant activities .
|
-
- HY-144368
-
|
|
Others
|
Inflammation/Immunology
|
|
CO delivery molecule 1 (compound 4) localizes to the endoplasmic reticulum, mitochondria, and lysosomes. Subcellular localization of CO delivery molecule 1 results in CO-induced toxicity effects. Anti-inflammatory effects of CO delivery molecule 1, as measured by TNF-α suppression, occur at the nanomolar level in the absence of CO release, and are enhanced with visible-light-induced CO release .
|
-
- HY-P99294
-
|
AMG 479; Human Anti-IGF1R Recombinant Antibody
|
IGF-1R
|
Cancer
|
|
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
|
-
- HY-161699
-
|
|
PSMA
|
Cancer
|
|
SDTWS01 is a novel 68Ga-labeled prostate-specific membrane antigen (PSMA) targeting tracer. The inhibition constant (Ki) of SDTWS01 for PSMA is in the nanomolar range (less than 10 nM), demonstrating high affinity for PSMA. SDTWS01 exhibits significant tumor uptake and superior PET imaging effects. SDTWS01 can be utilized for diagnostic research of prostate cancer .
|
-
- HY-12284
-
|
|
Others
|
Inflammation/Immunology
|
|
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
|
-
- HY-100233
-
|
|
JNK
|
Inflammation/Immunology
Cancer
|
|
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
|
-
- HY-130622
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-116218
-
|
JPI-289 free base
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
|
Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50=18.5 nM) and cellular PAR formation (IC50=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke .
|
-
- HY-119733
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
|
-
- HY-103110
-
ST1936
1 Publications Verification
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-103110A
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-108350
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
|
-
- HY-139874
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3 + T lymphocytes into the Pan02 tumor tissues .
|
-
- HY-158439
-
|
|
JAK
STAT
|
Cancer
|
|
anti-TNBC agent-7 (Compound 13c) possesses anticancer activity, serving as a molecular probe to recognize and regulate the signal transduction of the USP21/JAK2/STAT3 axis, exhibiting nanomolar-level cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC) .
|
-
- HY-137464A
-
OATD-01
1 Publications Verification
|
Others
|
Inflammation/Immunology
|
|
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
|
-
- HY-139590
-
|
BOS-172738; DS-5010
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
|
-
- HY-12928
-
|
|
Virus Protease
|
Infection
|
|
ML336 is quinazolinone-based inhibitor against venezuelan equine encephalitis virus (VEEV), with IC50s of 32, 20, and 42 nM for VEEV TC-83 CPE , VEEV V3526 CPE, VEEV Wild Type CPE, respectively. ML336 potently inhibits a VEEV-induced cytopathic effect in three strains of the virus (TC-83, V3526, and wild type Trinidad donkey) in the low nanomolar range .
|
-
- HY-162568
-
|
|
DNA Stain
|
Cancer
|
|
7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin (HY-112328), that can be isolated from Fascaplysinopsis sp.. 7-tert-Butylfascaplysin induces replication stress, leads to toxic DNA double-strand breaks and apoptosis-like cell death, and thus exhibits cytotoxicity in cancer cells in nanomolar levels. 7-tert-Butylfascaplysin exhibits DNA intercalating activity with EC50 of 3.2 μM .
|
-
- HY-135276
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
|
-
- HY-N2348
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin D is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin D can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin D displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin D inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N2346
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N2347
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin C is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin C can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin C displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin C inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7049
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin F is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin F can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin F displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin F inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7050
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin G is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin G can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin G displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin G inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7051
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin H is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin H can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin H displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin H inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7052
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin I is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin I can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin I displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin I inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N7053
-
|
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-135581
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-135582
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-136927
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
|
-
- HY-139590A
-
|
BOS-172738 hemiadipate; DS-5010 hemiadipate
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
|
-
- HY-139602
-
|
|
Flavivirus
Dengue virus
Virus Protease
|
Infection
|
|
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
|
-
- HY-P5914A
-
|
WaTx TFA
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-135495
-
|
|
Others
|
Inflammation/Immunology
|
|
AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
|
-
- HY-135276A
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
|
-
- HY-106100A
-
|
EMD 38362
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities .
|
-
- HY-149283
-
|
|
JAK
HDAC
Apoptosis
|
Cancer
|
|
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
|
-
- HY-117540
-
|
|
Others
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
- 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-154978
-
|
|
Others
|
Cancer
|
|
Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
|
-
- HY-153810
-
|
JNJ-1802
|
Virus Protease
Flavivirus
Dengue virus
|
Infection
|
|
Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates .
|
-
- HY-126247
-
|
|
Ras
|
Cancer
|
|
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-108672
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively . NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA) .
|
-
- HY-122587
-
|
|
DNA/RNA Synthesis
RSV
|
Infection
|
|
AVG-233 is a potent, orally active RNA dependent RNA polymerase (RdRp) inhibitor. AVG-233 prevents initiation of the viral polymerase complex at the promoter. AVG-233 binding site is present in the L1-1749 fragment. AVG-233 has nanomolar activity against both RSV strains and clinical RSV isolates (EC50=0.14-0.31 μM). AVG-233 can be used for research of respiratory syncytial virus (RSV) .
|
-
- HY-113658
-
|
|
Others
|
Others
|
|
ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitory activity and is a multi-target CA inhibitor .
|
-
- HY-12513
-
|
LY3023414
|
PI3K
DNA-PK
mTOR
Autophagy
|
Cancer
|
|
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
|
-
- HY-18971
-
TG4-155
1 Publications Verification
|
Prostaglandin Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM . TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1 . TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor .
|
-
- HY-107428
-
|
|
MMP
|
Cardiovascular Disease
|
|
PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
|
-
- HY-P2265
-
|
|
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-149269
-
|
|
COX
Carbonic Anhydrase
LOX-1
|
Inflammation/Immunology
|
|
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
|
-
- HY-119799
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma .
|
-
- HY-15350
-
|
LY 300046 hydrochloride
|
Reverse Transcriptase
|
Others
|
|
Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .
|
-
- HY-16787
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
|
-
- HY-135581S1
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
|
-
- HY-135582S1
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
|
-
- HY-100552
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM .
|
-
- HY-153519
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
|
-
- HY-135582S
-
|
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Endocrinology
|
|
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
|
-
- HY-P10548
-
|
|
Bacterial
|
Infection
|
|
Cyclic L27-11 is a cyclic peptide-like antibiotic with strong antibacterial activity against specific bacteria such as Pseudomonas sp. Cyclic L27-11 shows nanomolar antibacterial activity against Pseudomonas sp., especially Pseudomonas aeruginosa. Cyclic L27-11 interferes with the function of bacterial outer membrane protein LptD, preventing the normal transport of lipopolysaccharide (LPS), leading to the accumulation of membrane-like substances in bacterial cells, which in turn affects the survival of bacteria. Cyclic L27-11 can be used in the development of antibacterial agents .
|
-
- HY-125640
-
|
BC556
|
Cyclophilin
HCV
HBV
HIV
|
Infection
|
|
NVP018 (BC556) is an orally active inhibitor for cyclophilin A with IC50 of 0.3 and 0.1 nM for cyclophilin A and NS5A- cyclophilin A complex. NVP018 inhibits Bilirubin (HY-N0323) transporter OATP1B1 and OATP1B3 with IC50 of 4.31 and 1.75 μM. NVP018 inhibits the replication of HBV (in HepG2), HCV (in Huh-7) and HIV-1 (in HeLa), with IC50 in nanomolar levels. NVP018 exhibits anti-fibrotic effect by inhibiting the mRNA expression of COL1A1 and LOX .
|
-
- HY-155007
-
|
|
Bacterial
|
Infection
|
|
DNA gyrase B-IN-2 (Compound E) is a 2-aminobenzothiazole-based DNA gyrase B inhibitor with promising activity against ESKAPE bacterial pathogens. DNA gyrase B-IN-2 showed low nanomolar inhibition of DNA gyrase (IC50 < 10 nM) and broad-spectrum antibacterial activity against pathogens belonging to the ESKAPE group, with the minimum inhibitory concentration < 0.03 μg/mL for most Gram-positive strains and 4–16 μg/mL against Gram-negative E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae.DNA gyrase B-IN-2 can be used for the research of infection .
|
-
- HY-131708A
-
|
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
|
-
- HY-12443
-
|
|
Casein Kinase
|
Neurological Disease
|
|
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
|
-
- HY-115314
-
|
LG 30435
|
Others
|
Inflammation/Immunology
|
|
Mequitamium iodide (LG 30435) is an antihistamine drug with antiallergic and bronchodilatory activity. Mequitamium iodide can effectively antagonize airway contraction and inflammatory responses induced by histamine and antigens. Mequitamium iodide has nanomolar affinity for the H1 and smooth muscle receptors of histamine and mequitin. Mequitamium iodide, when administered in aerosol form, significantly inhibits histamine- and antigen-induced increases in airway pressure in allergic mice. Mequitamium iodide reduces antigen-induced eosinophil accumulation in the airways. Mequitamium iodide also exhibits inhibitory effects on PAF-induced platelet aggregation and bronchoconstriction, and can be used in the study of allergic diseases such as rhinitis and asthma .
|
-
- HY-W030338
-
|
|
Others
|
Inflammation/Immunology
|
|
aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitory activity, providing the possibility for further development of small molecule aPKC inhibitors .
|
-
- HY-104042
-
|
AG-881
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .
|
-
- HY-129937A
-
GNE-987
1 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
|
-
- HY-131708
-
|
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
|
-
- HY-112626
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
|
-
- HY-126247B
-
|
|
Others
|
Cancer
|
|
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-123882
-
|
|
Others
|
Others
|
|
IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
|
-
- HY-P2265A
-
|
|
Ras
|
Cancer
|
|
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-12583
-
A-366
3 Publications Verification
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
|
-
- HY-122575
-
|
|
P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
|
-
- HY-134813
-
|
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective 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-15334
-
|
|
VEGFR
|
Cancer
|
|
CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
|
-
- HY-13590
-
|
|
Others
|
Cancer
|
|
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
|
-
- HY-118046
-
|
|
G Protein-coupled Receptor Kinase (GRK)
|
Cardiovascular Disease
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GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that may serve as a probe for studying heart failure and Parkinson's disease. Screening of known protein kinase inhibitors by differential scanning fluorescence method revealed that the melting points of GRK2 and GRK5 increased. Enzymatic assays of the 14 most stable hits revealed that three exhibited nanomolar inhibitory potency against a single GRK, with some showing significant selectivity. Most of the identified compounds can be divided into two categories: indazole/dihydropyrimidine compounds selectively inhibit GRK2, and pyrrolopyrimidine compounds effectively inhibit GRK1 and GRK5 but with modest selectivity. The two most inhibitory representative compounds, GSK180736A and GSK2163632A, are co-crystals with GRK2 and GRK1, respectively, and their atomic structures were determined to 2.6 and 1.85 ? distances, respectively. GSK180736A, as an inhibitor of Rho-related coiled-coil protein kinase, binds to GRK2 in a manner similar to paroxetine, while GSK2163632A, as an inhibitor of insulin-like growth factor 1 receptor, occupies a novel region of the GRK active site cleft and may be used to achieve more Selectivity. However, both compounds inhibited GRK no more potently than their original targets. These data provide a basis for the rational design of more effective and selective GRK inhibitors in the future .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0039
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Bombesin Receptor
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Cancer
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BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. BIM-26226 inhibits BN- or GRP-stimulated amylase release with IC50s in the nanomolar range. BIM-26226 can be used for the research of cancer .
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- HY-P2274
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Parasite
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Infection
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Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
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- HY-P5914A
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WaTx TFA
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TRP Channel
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Neurological Disease
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Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
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- HY-P2265A
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Ras
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Cancer
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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-137392
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1-Naphthalenesulfonyl-Ile-Trp-CHO
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Cathepsin
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Others
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Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations .
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- HY-P2138
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Peptides
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Others
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U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
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- HY-P10331
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Peptides
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Cancer
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KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
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- HY-P5914
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WaTx
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TRP Channel
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Neurological Disease
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Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
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- HY-P2265
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Ras
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Cancer
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SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-P10548
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Bacterial
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Infection
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Cyclic L27-11 is a cyclic peptide-like antibiotic with strong antibacterial activity against specific bacteria such as Pseudomonas sp. Cyclic L27-11 shows nanomolar antibacterial activity against Pseudomonas sp., especially Pseudomonas aeruginosa. Cyclic L27-11 interferes with the function of bacterial outer membrane protein LptD, preventing the normal transport of lipopolysaccharide (LPS), leading to the accumulation of membrane-like substances in bacterial cells, which in turn affects the survival of bacteria. Cyclic L27-11 can be used in the development of antibacterial agents .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99294
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AMG 479; Human Anti-IGF1R Recombinant Antibody
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IGF-1R
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Cancer
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Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-135581S1
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Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
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- HY-135582S1
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Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
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- HY-135582S
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Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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| Cat. No. |
Product Name |
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Classification |
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- HY-134813
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective 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 .
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- HY-167690
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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