Search Result
Results for "
selective
" in MedChemExpress (MCE) Product Catalog:
9973
Inhibitors & Agonists
58
Biochemical Assay Reagents
407
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-157131
-
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TRP Channel
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Neurological Disease
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TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+ influx in macrophages, and inhibits macrophage phagocytosis .
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- HY-132217
-
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Cannabinoid Receptor
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Neurological Disease
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CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2 .
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- HY-149725
-
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MMP
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Neurological Disease
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proMMP-9 selective inhibitor-1 (compound 33) is a highly potent and selective inhibitor of proMMP-9 activation .
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-
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- HY-161021
-
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Adenylate Cyclase
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Others
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AC2 selective-IN-1 (compound 14) is a? potent (IC50=4.45 μM), non-toxic, and selective mAC2 inhibitor .
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-
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- HY-153990
-
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FKBP
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Neurological Disease
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FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52 .
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- HY-126123
-
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iGluR
Potassium Channel
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Neurological Disease
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NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
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- HY-157520
-
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Cholinesterase (ChE)
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Others
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BChE-IN-25 (compound 4I) is a selective BChE inhibitor (IC50: 3.77μM), which is 22 times more selective for BChE than AChE .
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-
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- HY-118232
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-
-
- HY-12236B
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-
-
- HY-120973A
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-
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- HY-125980
-
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p38 MAPK
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Cancer
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LX-3 is a selective activator of the p38 MAPK signaling pathway and activates EGFP reporter genes that are silenced by DNA methylation, such as TNF, EGR1, LY6K, and ISG20 .
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-
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- HY-161294
-
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COX
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Cancer
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COX-2-IN-41 (compound 5e) is a selective inhibitor of COX-2 (IC50=1.74 μM). Compared with COX-1, the selectivity IC50 (COX-1)/IC50(COX-2) =16.32 .
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-
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- HY-171049
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-
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- HY-126333
-
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Topoisomerase
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Cancer
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Topoisomerase II inhibitor 1 (compound 89) is a highly efficient and selective topoisomerase IIα inhibitor .
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-
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- HY-139347
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-
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- HY-115273
-
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P2Y Receptor
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Others
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MRS-2179 is a selective and competitive antagonist for P2Y1 receptor, with KB of 0.177 μM .
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-
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- HY-103446
-
-
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- HY-19134
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-
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- HY-149597
-
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Monoamine Oxidase
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Cancer
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Lysyl hydroxylase 2-IN-1 (compound 12) is a selective lysyl hydroxylase 2 (LH2) Inhibitor with an IC50 of ~300 nM. Lysyl hydroxylase 2-IN-1 demonstrates selectivity for LH2 over LH1 and LH3 .
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-
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- HY-157294A
-
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Glucocorticoid Receptor
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Cancer
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(R)-GSK866 is the (R)-enantiomer of GSK866 (HY-157294). GSK866 is a selective agonist for glucocorticoid receptor with an IC50 of 4.6 nM .
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- HY-120386
-
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iGluR
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Neurological Disease
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LY382884 is a selective antagonist for GluR5 kainate receptor. LY382884 prevents the induction of NMDA receptor independent long-term potentiation (LTP) .
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- HY-164621
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Adenosine Receptor
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Others
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A3AR antagonist 5 (Compound 16) is a selective antagonist for human adenosine A3 receptor with an affinity pC of 4.542 μM .
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- HY-108530
-
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RAR/RXR
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Cancer
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MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
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- HY-171140
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PROTACs
HDAC
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Cancer
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PROTAC HDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader for HDAC6 with an IC50 of 686 nM and a DC50 of 171 nM. PROTAC HDAC6 degrader 3 promotes the acetylation of α-tubulin . (Pink: ligand for target protein (HY-171141); Blue: ligand for E3 ligase VHL (HY-150803))
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- HY-D1488
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Fluorescent Dye
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Others
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Ethyl benzo[6,7]-4-oxo-4H-quinolizine-3-carboxlate (Compound 3) is a Mg 2+ selective fluorescent indicator .
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-
![Ethyl benzo[6,7]-4-oxo-4H-quinolizine-3-carboxlate](//file.medchemexpress.com/product_pic/hy-d1488.gif)
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- HY-117139
-
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Cannabinoid Receptor
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Neurological Disease
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NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor .
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- HY-B0010B
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(±)Formoterol
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Adrenergic Receptor
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Inflammation/Immunology
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Formoterol ((±)Formoterol) is an orally active β2-selective agonist. Formoterol potently relaxes the peripheral airways through stimulating the beta 2-adrenoceptors selectively as is the case in the central airways and that it significantly inhibits IgE-mediated slow reactive substance of anaphylaxis (SRS-A) release through beta-adrenoceptor stimulation .
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- HY-162618
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Cannabinoid Receptor
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Neurological Disease
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PSB-KK1445 is a potent and selective GPR18 agonist with EC50s of 45.4 nM and 124 nM for human and mouse GPR18, respectively. PSB-KK1445 displays >200-fold selectivity versus both CB receptor subtypes, GPR55, and GPR183 .
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- HY-149761
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- HY-117442
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Sirtuin
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Cancer
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A2B57 is a selective inhibitor for SIRT 2 with an IC50 of 6.3 µM .
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- HY-12019
-
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c-Met/HGFR
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Cancer
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SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity .
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- HY-135556
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Drug Metabolite
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Neurological Disease
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Norfluoxetine is the active metabolite of antidepressant Fluoxetine (HY-B0102). Norfluoxetine is a selective inhibitor for serotonin uptake .
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- HY-134919
-
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Cyclic GMP-AMP Synthase
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Inflammation/Immunology
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CU-76 is an inhibitor for human cyclic GMP-AMP synthase (hcGAS) with an IC50 of 0.24 μM. CU-76 selectively inhibits the DNA pathway in human cells, and can be used in autoimmune research .
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- HY-111082
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Adenosine Receptor
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Others
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ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM .
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- HY-116263
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- HY-153161
-
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Caspase
Apoptosis
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Cancer
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CASP8-IN-1 (Compound 63-R) is a selective inhibitor for caspase 8 (CASP8), with an IC50 of 0.7 μM. CASP8-IN-1 inhibits FasL-induced apoptosis in cell Jurkat .
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- HY-162617
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- HY-101753A
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Cyanimipramine hydrochloride; Ro 11-2465 hydrochloride
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5-HT Receptor
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Neurological Disease
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Cianopramine hydrochloride (Cyanimipramine hydrochloride; Ro 11-2465 hydrochloride) is the hydrochloride form of Cianopramine (HY-101753). Cianopramine hydrochloride is an antidepressant, which selectively inhibits the serotonin uptake into synaptosomes .
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- HY-101355B
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CGP 20712 mesylate
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Adrenergic Receptor
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Cardiovascular Disease
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CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors .
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- HY-122359
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L-Centchroman; L-Ormeloxifene
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Estrogen Receptor/ERR
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Endocrinology
Cancer
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Levormeloxifene (L-Centchroman) is a selective estrogen receptor modulator (SERM), which prevents and ameliorates postmenopausal osteoporosis. Levormeloxifene causes multiple adverse gynecological effects .
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- HY-146480
-
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PPAR
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Cancer
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PPARγ agonist 5 (Compound 1) is a potent and selective agonist of PPARγ. PPARγ agonist 5 has the potential for the research of cancer diseases .
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- HY-145651
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Et-29
1 Publications Verification
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Sirtuin
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Cancer
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Et-29 is a potent and selective SIRT5 inhibitor (Ki=40 nM) .
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- HY-115764
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- HY-158308
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HDAC
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Cancer
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HDAC6-IN-41 (Compound E24) is a selective inhibitor for histone deacetylase 6 (HDAC6), with IC50 of 14 and 422 nM, for HDAC6 and HDAC8, respectively. HDAC6-IN-41 upregulates the acetylation of α-tubulin and histone site SMC3 .
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- HY-104061
-
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TRP Channel
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Others
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AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM .
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- HY-115413
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-
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- HY-104062
-
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TRP Channel
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Others
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AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM .
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- HY-12989
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- HY-N2554
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Ostenol
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Monoamine Oxidase
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Neurological Disease
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Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
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- HY-117570
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PDI
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Neurological Disease
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KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-10300
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SCH 900518
|
HCV
HCV Protease
SARS-CoV
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Infection
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Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease . Narlaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.3 μM .
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- HY-103384
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Casein Kinase
|
Cancer
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TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
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- HY-120232
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- HY-120949
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Opioid Receptor
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Neurological Disease
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(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .
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- HY-108056
-
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Dopamine Receptor
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Endocrinology
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PF 219061 is an selective agonist for dopamine 3 receptor with an EC50 of 15 nM. PF 219061 exhibits a rapid absorption and a good liver blood clearance, and can be used for research of female sexual dysfunction .
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- HY-103549
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mGluR
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Neurological Disease
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Z-Cyclopentyl-AP4 is a kainate-type glutamate receptor agonist (orthosteric agonist). Z-Cyclopentyl-AP4 is more selective for mGlu4 than mGlu8 .
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- HY-115575
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Neuropeptide Y Receptor
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Metabolic Disease
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tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment .
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- HY-129250
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Histamine Receptor
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Neurological Disease
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AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation .
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- HY-168339
-
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JAK
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Inflammation/Immunology
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Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, JAK1, and JAK3 with IC50s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .
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- HY-123302
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GPR55
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Neurological Disease
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CID1172084 (compound 3) is a selective GPR55 agonist (EC50=0.16 μM). CID1172084 is more than 100-fold selective for GPR55 over GPR35, CB1, and CB2. CID1172084 can be used to further explore the biological functions and signaling pathways of the GPR55 receptor .
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- HY-101972
-
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Phosphatase
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Metabolic Disease
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AZ-PFKFB3-67 is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively .
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- HY-137172
-
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Biochemical Assay Reagents
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Others
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ETH 157 is a Na + selective microelectrode based on a synthetic neutral carrier that is selective enough for K +, Ca 2+, and Mg 2+ for extracellular measurements of Na+ activity .
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- HY-147984
-
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Carbonic Anhydrase
|
Cancer
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hCAXII-IN-3 (Compound 6o) is a selective human carbonic anhydrase XII (hCAXII) inhibitor with a Ki of 10.0 nM .
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- HY-168459
-
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MAGL
|
Neurological Disease
|
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MAGL-IN-21 (Compound (S)-6) is a selective inhibitor for monoacylglycerol lipase (MAGL) with an IC50 of 1.59 nM .
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- HY-P1726
-
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- HY-120278
-
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Endogenous Metabolite
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Others
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4-Ethoxyquinazoline is a selective small molecule activator of bacterial glycoside hydrolases (AC50=3.5 mM) .
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- HY-101251
-
-
- HY-123050
-
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VEGFR
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Neurological Disease
|
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(Rac)-SAR131675 is the racemate of SAR131675. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM .
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- HY-153113
-
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DJT1116PG
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SGLT
|
Endocrinology
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Rongliflozin (DJT1116PG) is a selective and orally active inhibitor of sodium-glucose co-transporter-2 (SGLT-2). Rongliflozin can be used for the research of type 2 diabetes mellitus (T2DM) .
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- HY-P1341
-
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Orexin A (17-33) (human, mouse, rat, bovine)
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Orexin Receptor (OX Receptor)
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Neurological Disease
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OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
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- HY-12023
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GTx-007
4 Publications Verification
S-4
|
Androgen Receptor
|
Cancer
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GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
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- HY-138690
-
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Estrogen Receptor/ERR
|
Endocrinology
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Estrogen receptor modulator 6 (compound 3a) is a selective estrogen receptor (ER) β agonist (Ki=0.44 nM). Estrogen receptor modulator 6 displays 19-fold selectivity for ERβ over ERα(Ki=8.4 nM) .
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- HY-139001
-
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Glutathione Peroxidase
Ferroptosis
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Others
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JKE-1716 is a potent and selective nitrolic acid-containing GPX4 inhibitor. JKE-1716 is able of inducing ferroptosis selectively through covalent GPX4 inhibition .
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- HY-120471
-
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PI3K
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Inflammation/Immunology
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AM-0687 is a selective inhibitor for PI3Kδ with an IC50 of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC50=0.8 nM) and the phosphorylation of AKT (IC50=0.7 nM), and exhibits anti-inflammatory efficacy .
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- HY-14851
-
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Sonedenoson
|
Adenosine Receptor
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Inflammation/Immunology
|
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MRE 0094 (Sonedenoson) is a selective activator for adenosine receptor A2A, with a Ki of 490 nM. MRE 0094 exhibits anti-platelet and anti-inflammatory activities .
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- HY-123548
-
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15-PGDH
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Inflammation/Immunology
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ML148 is a potent and selective 15-PGDH inhibitor with an IC50 of 56 nM. ML148 has the potential for the research of prostaglandin-signaling pathways .
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-
- HY-P1341A
-
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Orexin A (17-33) (human, mouse, rat, bovine) TFA
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Orexin Receptor (OX Receptor)
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Neurological Disease
|
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OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
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- HY-132232
-
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Epigenetic Reader Domain
|
Cancer
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GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media .
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- HY-144105
-
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MDM-2/p53
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Cancer
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NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53 .
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- HY-107327
-
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(±)-Carazolol; DL-Carazolol; Suacron
|
Adrenergic Receptor
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Cardiovascular Disease
|
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Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
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- HY-P1300
-
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Opioid Receptor
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Neurological Disease
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[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
![[(pF)Phe4]Nociceptin(1-13)NH2](//file.medchemexpress.com/product_pic/hy-p1300.gif)
- HY-132290
-
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TGF-β Receptor
|
Inflammation/Immunology
Cancer
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TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology .
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- HY-10204
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OSI-930
4 Publications Verification
|
c-Kit
VEGFR
c-Fms
Apoptosis
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Cancer
|
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OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity .
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- HY-120662
-
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mGluR
|
Neurological Disease
|
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GSK1331268 is a selective, orally active agonist for mGluR2 with a pEC50 of 6.9. GSK1331268 exhibits good blood-brain barrier penetration. GSK1331268 regulates glutamate signaling, and can be used in research of neurodegenerative and neuropsychiatric diseases .
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- HY-131914A
-
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Sigma Receptor
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Neurological Disease
|
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EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain .
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-
- HY-161179
-
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Trk Receptor
|
Cancer
|
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TRK-IN-27 (Compound 14q) is a potent TRK inhibitor with good kinase selectivity. TRK-IN-27 effectively inhibits tumor growth .
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- HY-P1300A
-
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Opioid Receptor
|
Neurological Disease
|
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[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
![[(pF)Phe4]Nociceptin(1-13)NH2 TFA](//file.medchemexpress.com/product_pic/hy-p1300a.gif)
- HY-151540
-
|
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MMP
|
Cancer
|
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MMP-7-IN-1 is a potent and selective inhibitor of MMP-7 over MMP-1, -2, -3, -8, -9, -13 with an IC50 value of 10 nM. MMP-7 is a potential target for diseases including cancer and fibrosis .
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-
- HY-119889
-
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Sirtuin
|
Neurological Disease
|
|
A1B11 is a selective SIRT inhibitor (SIRT2:IC50=5.3 μM) that can be used in the study of neurodegenerative diseases .
|
-
- HY-114204
-
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Epigenetic Reader Domain
|
Cancer
|
|
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1 .
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- HY-107605
-
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iGluR
|
Neurological Disease
|
|
UBP296 is a potent and selective antagonist of GLUK5-containing kainate receptor in the spinal cord. UBP296 reversibly blocks ATPA-induced depressions of synaptic transmission, and affects AMPA receptor-mediated synaptic transmission directly in rat hippocampal slices .
|
-
- HY-110052
-
|
|
Casein Kinase
|
Cancer
|
|
TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases .
|
-
- HY-150692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
|
-
- HY-W371165
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C1s-IN-1 trihydrochloride (Compound A1) is the selective inhibitor for C1s protease with the Ki of 5.8 μM. C1s-IN-1 trihydrochloride inhibits cleavage of C2 by C1s with an IC50 of 85 μM, inhibits the activation of classic pathway with an IC50 of 22 μM. C1s-IN-1 trihydrochloride is the competitive inhibitor for thrombin with the Ki of 51.2 μM .
|
-
- HY-146262
-
|
|
EGFR
|
Cancer
|
|
LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .
|
-
- HY-168728
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-37 (Compound 37) is a derivative of TT01001 (HY-114520), and a selective inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 270 nM. MAO-B-IN-37 exhibits good metabolic stability in mice microsomes and good affinity with human serum albumin .
|
-
- HY-19431
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM) .
|
-
- HY-123549
-
|
|
NTPDase
|
Cancer
|
|
PSB-6426 (compund 19a) is a selective human NTPDase2 inhibitor (Ki=8.2 μM). PSB-6426 can be used in stroke and cancer research .
|
-
- HY-162919
-
|
|
CDK
|
Cancer
|
|
YK-2168 is a differentiated selective inhibitor of CDK9 .
|
-
- HY-137530
-
|
8-Methylamino-cAMP
|
PKA
|
Others
|
|
8-MA-cAMP (8-Methylamino-cAMP) is a cyclic AMP analog that acts as a site-selective PKA agonist with similar affinity for the B site of type I and type II protein kinase A. 8-MA-cAMP is used in conjunction with priming analogs that show site A preference, such as 8-piperidinyl cAMP, to achieve selective stimulation of type I .
|
-
- HY-107327R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Carazolol (Standard) is the analytical standard of Carazolol. This product is intended for research and analytical applications. Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist .
|
-
- HY-149528
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Cancer
|
|
MAO-B-IN-24 (compound 11h) is a selective, reversible, competitive inhibitor of MAO-B (IC50: 1.60 μM). MAO-B-IN-24 also inhibited MAO-A (22.42 μM); at 10 μM concentration, it also reduced AChE and BChE activities to 54.58% and 88.43% .
|
-
- HY-100256
-
|
CD5789
|
RAR/RXR
Autophagy
|
Inflammation/Immunology
|
|
Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively .
|
-
- HY-14900
-
|
GRC-10693
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .
|
-
- HY-145988
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases .
|
-
- HY-164463
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
BMI-135 is a selective estrogen mimic, that exhibits agonist activity for estrogen receptor. BMI-135 induces rapid endoplasmic reticulum stress response (UPR) and apoptosis in breast cancer cells .
|
-
- HY-116508
-
-
- HY-137892
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .
|
-
- HY-122746
-
|
|
Histone Methyltransferase
|
Cancer
|
|
E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase .
|
-
- HY-144617
-
|
|
DYRK
|
Cancer
|
|
JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines .
|
-
- HY-12104
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
PF-514273 is an orally active, selective antagonist for cannabinoid-1 receptor (CB1) with IC50 of 1 nM. PF-514273 reduces the food uptake in mice, and can be used for obesity research .
|
-
- HY-159642
-
|
|
FGFR
|
Cancer
|
|
TYRA-300 is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM in Ba/F3. TYRA-300 exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
-
- HY-114633
-
|
|
Potassium Channel
|
Others
|
|
VU625 is an inhibitor for potassium channel, that selectively inhibits mosquito Aedes aegypti inward rectifier potassium channel 1 (AeKir), with IC50 of 96.8 nM in HEK293 cell. VU625 can be used in development of insecticide .
|
-
- HY-101972A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
AZ-PFKFB3-67 quarterhydrate is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively .
|
-
- HY-173083
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models .
|
-
- HY-139310
-
|
|
LPL Receptor
|
Others
|
|
GLPG2938 is a potent and selective S1P2 antagonist. GLPG2938 can be used for the research of idiopathic pulmonary fibrosis .
|
-
- HY-103376
-
|
|
CRFR
|
Neurological Disease
|
|
NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM .
|
-
- HY-153566
-
|
|
JAK
|
Cancer
|
|
JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective JAK1 inhibitor .
|
-
- HY-P1301
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
-
![[Arg14,Lys15]Nociceptin](//file.medchemexpress.com/product_pic/hy-p1301.gif)
- HY-P1340
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
|
-
![[Ala11,D-Leu15]-Orexin B(human)](//file.medchemexpress.com/product_pic/hy-p1340.gif)
- HY-124793
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 .
|
-
- HY-139148
-
-
- HY-111246
-
|
|
Androgen Receptor
|
Cancer
|
|
MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer .
|
-
- HY-151593
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .
|
-
- HY-116033
-
|
|
Ser/Thr Protease
|
Inflammation/Immunology
|
|
BMS-363131 is a selective inhibitor for tryptase, with an IC50 <1.7 nM. BMS-363131 is hydrolytic stable at pH=7 and pH=9. BMS-363131 attenuates the astham in a guinea pig model .
|
-
- HY-145905
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-1 is a potent and selective D4R antagonist with an IC50 of 6.87 µM. D4R antagonist-1 has the potential for the research of Parkinson’s disease .
|
-
- HY-P1340A
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
|
-
![[Ala11,D-Leu15]-Orexin B(human) TFA](//file.medchemexpress.com/product_pic/hy-p1340a.gif)
- HY-P1301A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
-
![[Arg14,Lys15]Nociceptin TFA](//file.medchemexpress.com/product_pic/hy-p1301a.gif)
- HY-131335
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
|
-
- HY-117658
-
|
|
MAP3K
|
Cardiovascular Disease
|
|
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 μM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue .
|
-
- HY-103101
-
|
|
5-HT Receptor
|
Others
|
|
LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .
|
-
- HY-133145
-
-
- HY-70074
-
|
|
RGS Protein
|
Inflammation/Immunology
Cancer
|
|
CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM .
|
-
- HY-117108
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Nocardicin A is a beta-lactam antibiotic with selective antibacterial activity. Nocardicin A has moderate antibacterial activity against a broad spectrum of Gram-negative bacteria including Proteus and Pseudomonas; it has no inhibitory effect on Staphylococcus, Mycobacterium, fungi, and yeast .
|
-
- HY-131305
-
|
|
PKC
Apoptosis
|
Neurological Disease
|
|
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .
|
-
- HY-151896
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-14 is a highly selective HDAC6 (HDAC) inhibitor with an IC50 of 42 nM. HDAC6-IN-14 displays >100-fold selectivity over HDAC1/HDAC2/HDAC3/HDAC4 .
|
-
- HY-P1215
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
- HY-P1215A
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
- HY-W009048
-
|
DCH18C6; Perhydrodibenzo-18-crown-6
|
Biochemical Assay Reagents
|
Others
|
|
Dicyclohexano-18-crown-6-ether selectively extracts lysine-rich cytochrome c proteins from other cationic proteins under weakly acidic and neutral conditions, demonstrating specificity in ligand-protein interactions .
|
-
- HY-136605
-
|
|
Src
|
Cancer
|
|
DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM .
|
-
- HY-B1368
-
|
4-Chloro-DL-phenylalanine; PCPA; CP-10188
|
Tryptophan Hydroxylase
|
Neurological Disease
Cancer
|
|
Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research .
|
-
- HY-W772850
-
|
4-Chloro-DL-phenylalanine hydrochloride; PCPA hydrochloride; CP-10188 hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
Cancer
|
|
Fenclonine hydrochloride is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine hydrochloride can be used in carcinoid syndrome research .
|
-
- HY-108557
-
-
- HY-12697
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .
|
-
- HY-107606A
-
|
|
iGluR
|
Neurological Disease
|
|
UBP301 hydrochloride is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has ～30-fold selectivity of kainate receptor over AMPA receptor. UBP301 hydrochloride is the derivative of willardiine .
|
-
- HY-107606
-
|
|
iGluR
|
Neurological Disease
|
|
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine .
|
-
- HY-147986
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with Ki values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
|
-
- HY-100256R
-
|
|
RAR/RXR
Autophagy
|
Inflammation/Immunology
|
|
Trifarotene (Standard) is the analytical standard of Trifarotene. This product is intended for research and analytical applications. Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively .
|
-
- HY-101820A
-
|
|
EGFR
|
Cancer
|
|
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-123130
-
|
|
MMP
|
Cancer
|
|
ABT-770 (compound 11) is a highly selective and orally active MMP inhibitor, demonstrating over 1000-fold selectivity for MMP-2 (IC50=4 nM) compared to MMP-1 (IC50=4600 nM). ABT-770 can be utilized in studies related to tumor growth, invasion, and metastasis .
|
-
- HY-17638
-
|
DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base
|
SGLT
|
Metabolic Disease
|
|
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation .
|
-
- HY-12900
-
|
|
SphK
|
Inflammation/Immunology
Cancer
|
|
RB-005 is a selective inhibitor of sphingosine kinase 1 (SK1) (IC50=3.6 µM), with weaker inhibition of another isoenzyme, SK2. The selective inhibition of RB-005 helps to distinguish the biological functions and roles of SK1 and SK2, which can be used in the study of inflammatory diseases and cancer .
|
-
- HY-105235A
-
|
CI-977 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
|
-
- HY-105235
-
|
CI-977
|
Opioid Receptor
|
Neurological Disease
|
|
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
|
-
- HY-160696
-
|
|
CD73
|
Cancer
|
|
ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ T cell proliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
|
-
- HY-136577
-
-
- HY-P1427A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Guangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channel KV2.1 and KV2.2 with IC50 of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner .
|
-
- HY-168328
-
|
|
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
|
-
- HY-124117
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY 278584 is a potent, highly selective 5-HT3 receptor antagonist with a Ki of 1.62 nM. LY 278584 has no activity on 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, or 5-HT2 receptors .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
|
-
- HY-14250A
-
|
|
Androgen Receptor
|
Endocrinology
|
|
(Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (Rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (Rac)-PF-998425 has the potential for the research of the androgenetic alopecia .
|
-
- HY-101348
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
|
-
- HY-116808
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TPN729 is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. TPN729 affects erectile function and it can be used for the research of erectile dysfunction .
|
-
- HY-147511
-
|
|
PPAR
|
Others
|
|
PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC50, 4.34 μM) .
|
-
- HY-18345
-
-
- HY-101280
-
|
|
NAMPT
|
Cancer
|
|
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
|
-
- HY-103153
-
-
- HY-170360
-
|
|
AMPK
JAK
|
Cancer
|
|
UCB9386 is the selective and brain penetrant inhibitor for Nuak1 with a pIC50 of 10.1. UCB9386 inhibits Nuak2 and Kak2 with an inhibition rate of ca. 50% at 10 nM .
|
-
- HY-103229
-
|
|
iGluR
|
Neurological Disease
|
|
Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties .
|
-
- HY-163804
-
|
|
Cytochrome P450
Parasite
|
Others
|
|
Cyprocide-B is activated by Cytochrome P450 and converted to electrophilic metabolites that selectively kill nematodes C. elegans. Cyprocide-B is promising for research of selective nematicide .
|
-
- HY-162787
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
|
-
- HY-162647
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pKi of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC50 of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats .
|
-
- HY-120421
-
|
|
Sigma Receptor
|
Cancer
|
|
SW116 free base is a selective fluorescent ligand for sigma-2 receptor with a Ki of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research .
|
-
- HY-163184
-
|
|
Ser/Thr Protease
|
Cancer
|
|
DCLK1-IN-3 is a potent and selective doublecortin-like kinase 1 (DCLK1) inhibitor with an IC50 of 47 nM. DCLK1-IN-3 can be used for the research of cancer .
|
-
- HY-136392
-
|
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively .
|
-
- HY-122138
-
|
|
mGluR
|
Neurological Disease
|
|
VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant .
|
-
- HY-162025
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-17 (Compound 9e) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 0.68 and 1359 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 40 nM .
|
-
- HY-151216S
-
|
rel-BRL29060-d4 hydrochloride; rel-BRL29060A-d4
|
Serotonin Transporter
Autophagy
|
Inflammation/Immunology
|
|
rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
|
-
- HY-143329
-
-
- HY-162024
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-16 (Compound 9f) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 1.25 and 82 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 140 nM .
|
-
- HY-14197
-
|
M&B 9302
|
Monoamine Oxidase
|
Neurological Disease
|
|
Clorgyline (M&B 9302) is an orally active, blood-brain barrier permeable and selective monoamine oxidase A (MAO-A) inhibitor. Clorgyline's selective inhibition of MAO-A leads to reduced metabolism of neurotransmitters such as serotonin (5-hydroxytryptamine), which accumulates in the brain. Clorgyline can be used in the study of depression and neurodegenerative diseases .
|
-
- HY-162088
-
-
- HY-159642G
-
|
|
FGFR
|
Cancer
|
|
TYRA-300 GMP is TYRA-300 (HY-159642) produced by using GMP guidelines. TYRA-300 GMP is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM. TYRA-300 GMP exhibits antitumor efficacy against urothelial cancers and solid tumors .
|
-
- HY-103404
-
-
- HY-14568
-
|
|
GlyT
|
Neurological Disease
|
|
DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey .
|
-
- HY-159568
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-22 is a highly selective inhibitor of human carbonic anhydrase (hCA) isoform XII (Ki=9.7 nM) with anticancer activity .
|
-
- HY-151891
-
|
|
Potassium Channel
|
Cancer
|
|
TASK-1-IN-1 is a potent and selective TASK-1 (Potassium Channel) inhibitor with an IC50 of 148 nM. TASK-1-IN-1 shows a reduced inhibition of TASK-3 channels (IC50 of 1750 nM) and not a significant effect on other K+ channels. TASK-1-IN-1 has anticancer effects.
|
-
- HY-111570
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). PI3Kγ inhibitor AZ2 can be used for the research of inflammatory and immune diseases .
|
-
- HY-146697
-
|
|
Trk Receptor
c-Fms
PDGFR
Bcr-Abl
c-Kit
Apoptosis
|
Cancer
|
|
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
|
-
- HY-148949A
-
|
|
Kallikrein
|
Others
|
|
Kallikrein 5-IN-2 TFA is the TFA salt form of Kallikrein 5-IN-2 (HY-148949). Kallikrein 5-IN-2 TFA is a selective inhibitor for kallikrein 5 (KLK5) with pIC50 of 7.1. Kallikrein 5-IN-2 TFA is non-phototoxic (100 μg/mL) and non-irritant. Kallikrein 5-IN-2 is stable at pH 4-pH 8 under non-oxidative condition. Kallikrein 5-IN-2 is potent in ameliorating the Netherton syndrome .
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-14258
-
|
(S)-Citalopram; (S)-(+)-Citalopram
|
Serotonin Transporter
|
Neurological Disease
|
|
Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression .
|
-
- HY-122136
-
|
|
Melatonin Receptor
|
Neurological Disease
|
|
S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist .
|
-
- HY-116808B
-
|
TPN729 maleate
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction .
|
-
- HY-129800
-
|
|
ERK
|
Cancer
|
|
CGP78850 is a potent and selective competitor of Grb2 SH2-phosphopeptide interactions. CGP78850 can be used for the research of cancer .
|
-
- HY-14336A
-
|
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM) .
|
-
- HY-107589A
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
|
-
- HY-107589
-
BIO5192
1 Publications Verification
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
|
-
- HY-163185
-
|
|
Ser/Thr Protease
|
Cancer
|
|
DCLK1-IN-4 (compound D2) is a potent and selective doublecortin-like kinase 1 (DCLK1) inhibitor with an IC50 of 70 nM. DCLK1-IN-4 can be used for the research of cancer .
|
-
- HY-70068
-
-
- HY-168498
-
|
|
Glutathione S-transferase
|
Inflammation/Immunology
|
|
GJG057 is a selective, orally active inhibitor for leukotriene C4 synthase (LTC4S) with an IC50 of 44 nM. GJG057 exhibits anti-inflammatory activity in mouse skin inflammation model and mouse asthma model .
|
-
- HY-133850
-
|
|
Pim
|
Cancer
|
|
10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC50=1.28 μM) .
|
-
- HY-108620
-
|
GR259653X
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys .
|
-
- HY-101776
-
|
Desmethyl-SB2343
|
mTOR
PI3K
|
Cancer
|
|
Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure .
|
-
- HY-122203A
-
PCS1055
1 Publications Verification
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-P10876
-
|
|
Amyloid-β
|
Neurological Disease
|
|
mcK6A1 is an inhibitor for the aggregation of amyloid-β (Aβ), that selectively binds to the 16KLVFFA21 segment of Aβ42, forms an extended β-folded structure, and inhibits the formation of Aβ42 oligomers. mcK6A1 can be used in research of Alzheimer's disease and other amyloid-related diseases .
|
-
- HY-138563
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
|
-
- HY-14258A
-
|
(S)-Citalopram oxalate; (S)-(+)-Citalopram oxalate
|
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
|
-
- HY-138639
-
|
|
GPR52
|
Neurological Disease
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior .
|
-
- HY-135542
-
|
|
CRFR
|
Others
|
|
NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily .
|
-
- HY-15651A
-
|
AZD9668 tosylate
|
Elastase
|
Inflammation/Immunology
|
|
Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM .
|
-
- HY-100980
-
|
BE2254 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Cancer
|
|
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively .
|
-
- HY-125156
-
|
BMS-801576
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Dapagliflozin-3-O-β-D-glucuronide (BMS-801576) is the metabolite of Dapagliflozin (HY-10450), and is formed in the liver and kidney by uridine diphosphate glucuronosyltransferase-1A9 (UGT1A9). Dapagliflozin is a selective inhibitor for SGLT2, that can be used to improve glycemic control and attenuate type 2 diabetes .
|
-
- HY-164462
-
|
|
PKC
NF-κB
Apoptosis
|
Cancer
|
|
BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
|
-
- HY-170898
-
|
|
iGluR
|
Neurological Disease
|
|
Antidepressant agent 8 (Compound 1f) is a selective antagonist for the NMDA receptor GluN1/2A with an IC50 of 2.94 μmol/L. Antidepressant agent 8 exhibits antidepressant-like effects in Hydrocortisone (HY-N0583)-induced zebrafish depression model. Antidepressant agent 8 can cross blood-brain barrier .
|
-
- HY-P2518A
-
|
|
Protease Activated Receptor (PAR)
|
Cancer
|
|
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
|
-
- HY-139664A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-14674
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities .
|
-
- HY-103572
-
|
|
mGluR
|
Neurological Disease
|
|
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
|
-
- HY-158154
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-110 (Compound 6) is a covalent EGFR inhibitor, with pIC50 values of 9.2 and 8.7 for EGFR enzyme and EGFR cell, respectively. EGFR-IN-110 shows high EGFR potency and good kinase selectivity .
|
-
- HY-W019847
-
|
|
Cytochrome P450
|
Infection
Metabolic Disease
|
|
Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .
|
-
- HY-130628
-
|
|
PAK
|
Cancer
|
|
PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions .
|
-
- HY-101255
-
ODQ
3 Publications Verification
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells .
|
-
- HY-151230
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(-)-Erteberel is a selective estrogen receptor beta (ERβ) agonist. (-)-Erteberel can be utilized in the study of diseases mediated by estrogen receptor beta (ERβ), such as prostate cancer .
|
-
- HY-101223
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant .
|
-
- HY-100024
-
|
|
Mps1
|
Cancer
|
|
NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer .
|
-
- HY-112348
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-131868
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain .
|
-
- HY-102094
-
|
|
mGluR
|
Neurological Disease
|
|
(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist .
|
-
- HY-110202
-
-
- HY-122614
-
S29434
2 Publications Verification
NMDPEF
|
Autophagy
|
Neurological Disease
|
|
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production .
|
-
- HY-169172
-
|
|
Bcl-2 Family
Caspase
|
Cancer
|
|
Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor for Bfl-1 with an IC50 of 0.022 μM. Bfl-1-IN-5 promotes the caspase-3/7 activity with an EC50 of 0.37 μM, and inhibits the cell viability of SU-DHL-1 with an EC50 of 1.3 μM .
|
-
- HY-W007524
-
|
2-Quinolinamine
|
NO Synthase
Orthopoxvirus
|
Infection
Neurological Disease
|
|
2-Aminoquinoline (2-Quinolinamine) is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline exhibits antiviral activity against the vaccinia virus. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents .
|
-
- HY-143897
-
|
|
Pim
Apoptosis
|
Cancer
|
|
PIM1-IN-3 (Compound HL8) is a potent inhibitor of PIM1. PIM1-IN-3 shows selective inhibition for the PIM-1 enzyme. PIM1-IN-3 induces apoptosis efficiently in Colo320 cells. PIM1-IN-3 has the potential for the research of cancer diseases .
|
-
- HY-128207
-
|
|
Orphan Receptor
|
Cancer
|
|
SID7970631, as an isoquinolinone analog, is a potent and selective submicromolar SF-1 inhibitor (IC50=255 nM). SID7970631 can be used for the research of cancer .
|
-
- HY-147784
-
|
|
Btk
|
Cancer
|
|
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
|
-
- HY-108886
-
JWG-071
3 Publications Verification
|
ERK
|
Cancer
|
|
JWG-071 is the kinase-selective chemical probe for ERK5. JWG-071 inhibits ERK5 and LRRK2 with IC50 values of 88nM and 109 nM, respectively .
|
-
- HY-143258
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC50 values of 5.01 nM and 3.97 nM, respectively .
|
-
- HY-138742
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
|
-
- HY-170546
-
|
|
Haspin Kinase
|
Cancer
|
|
MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes .
|
-
- HY-116605
-
|
|
Histone Methyltransferase
|
Cancer
|
|
GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC50=0.02 μM; Ki=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research .
|
-
- HY-111616
-
|
|
PPAR
Angiotensin Receptor
|
Cardiovascular Disease
Others
|
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides . GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38) .
|
-
- HY-101327
-
|
Corwin; ICI 118587
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Xamoterol is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol has the potential for the research of arrhythmogenesis. Xamoterol has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
|
-
- HY-121037
-
|
EGM1
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
|
-
- HY-126073
-
|
|
Aquaporin
|
Inflammation/Immunology
Cancer
|
|
DFP00173 is a potent and selective aquaporin-3 (AQP3) inhibitor. DFP00173 inhibits mouse and human AQP3 with an IC50 of ∼0.1-0.4 μM. DFP00173 is selective for AQP3 over the homologous AQP isoforms AQP7 and AQP9 .
|
-
- HY-112089
-
|
LXH254
|
Raf
p38 MAPK
Bcr-Abl
|
Cancer
|
|
Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .
|
-
- HY-119350B
-
|
RUC-4 dihydrochloride
|
Integrin
|
Cardiovascular Disease
|
|
Zalunfiban (RUC-4) dihydrochloride is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban dihydrochloride can be used for the research of myocardial infarction (MI) .
|
-
- HY-139399
-
|
JNJ-67856633
|
MALT1
|
Cancer
|
|
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis .
|
-
- HY-119350
-
|
RUC-4
|
Integrin
|
Cardiovascular Disease
|
|
Zalunfiban (RUC-4) is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban can be used for the research of myocardial infarction (MI) .
|
-
- HY-116459
-
|
AF102A hydrochloride
|
mAChR
|
Neurological Disease
|
|
Trans-Cevimeline (AF102A) (hydrochloride), as a trans-isomer of AF102B, is a M1 selective cholinergic agonist. Trans-Cevimeline (AF102A) (hydrochloride) can be used for the research of Alzheimer's disease .
|
-
- HY-131035
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation .
|
-
- HY-107721
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ .
|
-
- HY-P1007
-
|
Z-VE(OMe)ID(OMe)-FMK
|
Caspase
Apoptosis
|
Cancer
|
|
Z-VEID-FMK (Z-VE(OMe)ID(OMe)-FMK) is a selective and irreversible caspase-6 peptide inhibitor. Z-VEID-FMK alleviates the S-(+)-ketamine-induced augmentation of caspase-6 activity, DNA fragmentation, and cell apoptosis .
|
-
- HY-111957
-
|
|
HPPD
|
Others
|
|
Fenquinotrione is a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor with IC50s of 27.2 and 44.7nM against rice and Arabidopsis thaliana HPPD, respectively. Fenquinotrione is an herbicide that can control a wide range of broadleaf and sedge weeds with excellent rice selectivity .
|
-
- HY-117634
-
-
- HY-136546
-
|
|
STAT
|
Cancer
|
|
Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members .
|
-
- HY-16748
-
|
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease .
|
-
- HY-148907
-
|
|
CaMK
MEK
Mixed Lineage Kinase
|
Cancer
|
|
CS640 is a selective inhibitor of calmodulin-dependent kinases. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4 and MLK3 with IC50 values of 0.08, 0.03, 0.001, 0.001, 11.2, 0.025, 5.69 and 2.75 μM, respectively. CS640 also shows inhibitory effects to CYP450 2C9 and CYP450 2C19 with IC50 values of 6 and 10 μM, respectively .
|
-
- HY-144117
-
|
|
CDK
|
Metabolic Disease
|
|
GFB-12811 is a high selective and orally active CDK5 inhibitor with an IC50 of 2.3 nM. GFB-12811 is highly selective over the other tested kinases (CDK1/2/6/7/9) .
|
-
- HY-108642B
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-108642
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-108642A
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-103162
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease .
|
-
- HY-122832
-
|
|
Wnt
|
Cancer
|
|
ABC99 is an N-hydroxyhydantoin (NHH) carbamate that selectively inhibits the Wnt-deacylating enzyme NOTUM (IC50=13 nM). ABC99 preserves Wnt3A signaling in the presence of NOTUM .
|
-
- HY-139204
-
-
- HY-101352
-
-
- HY-148518
-
|
|
SRPK
|
Cancer
|
|
MSC-1186 is a highly selective pan-SRPK inhibitor. MSC-1186 has activity for SRPK1, SRPK2 and SRPK3 with IC50 values of 2.7 nM, 81 nM and 0.6 nM, respectively. MSC-1186 can be used for the research of cancer .
|
-
- HY-100970
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM) .
|
-
- HY-113957
-
|
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM .
|
-
- HY-162431
-
|
|
Ras
|
Cancer
|
|
MK-1084 is a selective KRAS G12C inhibitor that is currently in Phase I clinical trial (NCT05067283). MK-1084 exhibits anticancer activity and can be used either alone or in combination with pembrolizumab (HY-P9902) for cancer research .
|
-
- HY-139665
-
VB124
1 Publications Verification
|
Monocarboxylate Transporter
|
Cardiovascular Disease
|
|
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism .
|
-
- HY-142704
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
|
-
- HY-161596
-
|
|
Parasite
Cathepsin
|
Infection
|
|
SmCB1-IN-1 (Compound 2h) is an inhibitor for S. mansoni cathepsin B1 (SmCB1) with an Ki of 0.05 μM . SmCB1-IN-1 exhibits selectivity toward human off-target cathepsins (29% and 37% inhibition for CatB and CatL at 20 μM). SmCB1-IN-1 inhibits 68% Schistosoma mansoni at 1 μM .
|
-
- HY-120909
-
|
|
HSP
Apoptosis
|
Cancer
|
|
YK5 is a potent and selective Hsp70 inhibitor. YK5 selectively and tightly binds to the cytosolic Hsp70s in cancer cells. YK5 has biological activity partly by interfering with the formation of active oncogenic Hsp70/Hsp90/client protein complexes .
|
-
- HY-101327A
-
|
Corwin hemifumarate; ICI 118587 hemifumarate
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr .
|
-
- HY-168905
-
|
|
Calmodulin
|
Cancer
|
|
SGC-CAMKK2-1 is the selective, inhibitor for calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) with an IC50 of 30 nM. SGC-CAMKK2-1 inhibits AMPK phosphorylation in cell C4-2 with an IC50 of 1.6 µM .
|
-
- HY-16748A
-
|
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease .
|
-
- HY-101280A
-
|
|
NAMPT
|
Cancer
|
|
LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines .
|
-
- HY-12146
-
|
|
ELOVL
|
Metabolic Disease
|
|
ELOVL6-IN-2 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-2 inhibits mouse ELOVL6 activities, with an IC50 value of 34 nM .
|
-
- HY-115953
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM) .
|
-
- HY-122666
-
|
|
GlyT
|
Metabolic Disease
|
|
Org 25935 is a potent and selective glycine transporter 1 protein (GlyT1) inhibitor with an IC50 value of 100 nM. Org 25935 can decrease ethanol (EtOH) intake and EtOH preference in rats, whereas water intake is unaffected. Org 25935 can be used for researching alcohol dependence or abuse .
|
-
- HY-108495
-
|
ML248
|
LPL Receptor
|
Cardiovascular Disease
|
|
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM .
|
-
- HY-124775
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(S)-C33 is a potent and selective PDE9 (phosphodiesterase-9) inhibitor, with an IC50 of 11 nM. (S)-C33 can be used for central nervous system diseases and diabetes research .
|
-
- HY-12819
-
-
- HY-132247
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .
|
-
- HY-161066
-
|
|
Ras
|
Cancer
|
|
KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS G13D (IC50: 0.41 nM). The selectivity for KRAS G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .
|
-
- HY-B1397A
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Cyclizine dihydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine dihydrochloride can be used for the research of nausea, vomiting, and dizziness .
|
-
- HY-B1397
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness .
|
-
- HY-125027
-
|
IB-DNQ
|
Quinone Reductase
|
Cancer
|
|
Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H:quinone oxidoreductase (NQO1). Isobutyl-deoxynyboquinone can be used for the research of anticancer .
|
-
- HY-142705
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
|
-
- HY-19630
-
|
VU0463597
|
mGluR
|
Neurological Disease
|
|
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-157364
-
|
Levine EMB Agar
|
Biochemical Assay Reagents
|
Others
|
|
Levine Eosin-Methylene Blue Agar Medium (Levine EMB Agar) is a weakly selective medium for the isolation of intestinal pathogens, especially E. coli. The composition of 1 liter of Levine Eosin-Methylene Blue Agar Medium: 10.0 g Peptone, 10.0 g lactose, 2.0 g dipotassium hydrogen phosphate, 15.0 g agar, 0.4 g eosin, 0.065 g methylene blue .
|
-
- HY-100798
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .
|
-
- HY-162857
-
|
|
Heme oxygenase (HO)
|
Neurological Disease
Cancer
|
|
Heme Oxygenase-1-IN-3 (compound 4) is a highly selective heme oxygenase-1 (HO-1) inhibitor (Kd=141 nM) that can be used in the research of cancer and neurodegenerative diseases .
|
-
- HY-110154
-
|
|
Histone Demethylase
|
Cancer
|
|
NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer .
|
-
- HY-110015
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
(-)-Chromanol 293B is a potent and selective inhibitor of the slow component of delayed rectifier K + current (IKs). (-)-Chromanol 293B can be used for the research of antiarrhythmic .
|
-
- HY-160939
-
|
|
MAP3K
|
Neurological Disease
Inflammation/Immunology
|
|
ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model .
|
-
- HY-107479
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects .
|
-
- HY-171236
-
|
|
Opioid Receptor
|
|
|
FEKAP is a brain-penetrant and selective kappa opioid receptor (KOR) agonist (Ki = 0.43 nM) which isotope labeled form exhibits excellent imaging properties. 11C-FEKAP can be utilized as a radiotracer for imaging KOR .
|
-
- HY-108616
-
|
|
Phospholipase
|
Cancer
|
|
VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research .
|
-
- HY-133148
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2 .
|
-
- HY-137820
-
|
|
DNA/RNA Synthesis
|
Others
|
|
Brr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC50 value of 1.3 μM .
|
-
- HY-P1216A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats .
|
-
- HY-12753A
-
|
SR35021 hydrochloride
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-116908
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-272183 is a selective 5-HT1A, 5-HT1B and 5-HT1D receptor antagonist. In addition, SB-272183 is also a potent and selective ligand for 5-HT1A, 5-HT1B and 5-HT1D receptors in human recombinant and native tissues with pKi values ??of 8.0, 8.1 and 8.7, respectively. SB-272183 can be used in antidepressant research .
|
-
- HY-W440039
-
|
|
Herbicide
|
Inflammation/Immunology
|
|
Methyl 2-(2,4-dihydroxyphenyl)acetate, a phenolic ester, is isolated from Nigella damascena seeds with selective phytotoxic effects .
|
-
- HY-110286
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer .
|
-
- HY-141677
-
|
|
Histone Demethylase
|
Cancer
|
|
INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia .
|
-
- HY-141677A
-
|
|
Histone Demethylase
|
Cancer
|
|
INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia .
|
-
- HY-131065
-
|
|
c-Met/HGFR
|
Cancer
|
|
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity .
|
-
- HY-137813
-
|
|
PERK
|
Neurological Disease
Metabolic Disease
Cancer
|
|
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .
|
-
- HY-N1377
-
-
- HY-126248
-
|
|
PARP
|
Cancer
|
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
|
-
- HY-149297
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
|
-
- HY-132811
-
-
- HY-123838
-
-
- HY-109144
-
|
DWP-16001
|
SGLT
|
Metabolic Disease
|
|
Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor .
|
-
- HY-131972
-
|
|
PI3K
|
Cancer
|
|
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy .
|
-
- HY-D2415
-
|
|
Fluorescent Dye
|
Others
|
|
BODIPY-FL staurosporine (Compound 8a) is a fluorescence probe based on staurosporine, exhibiting high specificity towards tyrosine kinases (TK) and tyrosine kinase-like (TKL) family kinases. BODIPY-FL staurosporine has the potential to develop binding assays for kinases that are not recommended for use with Kinase Tracer 236, such as PIM3, CDC42BPG, MAP2K7, TXK, and SIK3. BODIPY-FL staurosporine can be a powerful tool for analyzing kinase selectivity in kinase drug discovery .
|
-
- HY-145628
-
|
|
Sigma Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
|
-
- HY-123058
-
|
|
PI3K
Autophagy
|
Cancer
|
|
Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components .
|
-
- HY-147216
-
|
|
Lactate Dehydrogenase
|
Cancer
|
|
AXKO-0046, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor.AXKO-0046 has LDHB inhibitory activity with an EC50 value of 42 nM.AXKO-0046 can be used for the research of cancer metabolism .
|
-
- HY-B1871
-
|
|
Herbicide
|
Others
|
|
Metolachlor is a pre-emergent selective, chloroacetanilide herbicide for the control of a variety of annual grass and broad leaf weeds in corn and other crops. Metolachlor is a chiral herbicide consisting of four stereoisomers .
|
-
- HY-143465
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
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 .
|
-
- HY-162656
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-19 (Compound 2g) is a selective inhibitor for TbDHFR with Ki of 9 nM. DHFR-IN-19 exhibits antiparasitic activity against Trypanosoma brucei with an EC50 of 14.5 μM .
|
-
- HY-146662
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
|
-
- HY-122063
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
FR260330 is a selective, orally active inhibitor for inducible nitric oxide synthase (iNOS) through suppression of iNOS dimerization. FR260330 inhibits the NO accumulation in rat splenocytes and human DLD-110 cells, with IC50 of 27 and 10 nM. FR260330 ameliorates the Lipopolysaccharides (HY-D1056)-induced inflammatory diseases in rats model .
|
-
- HY-107529
-
|
|
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases .
|
-
- HY-102057
-
|
TD-8954
|
5-HT Receptor
|
Others
|
|
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
|
-
- HY-114982
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
KEA1-97 is a selective Thioredoxin-caspase 3 interaction disruptor (IC50=10 μM). KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity .
|
-
- HY-16983
-
|
|
ROR
|
Inflammation/Immunology
|
|
GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-P10429
-
|
|
CXCR
|
Infection
|
|
RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors .
|
-
- HY-132829
-
|
GC4711
|
Reactive Oxygen Species
|
Cancer
|
|
Rucosopasem manganese (GC4711) is a selective superoxide dismutase mimetic that converts superoxide to hydrogen peroxide. Rucosopasem manganese can be used for the research of cancer .
|
-
- HY-10195
-
|
LY333531
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM .
|
-
- HY-103266
-
|
|
Aurora Kinase
|
Cancer
|
|
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
|
-
- HY-100827
-
|
LF22-0542
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
|
-
- HY-105064B
-
|
CP-597396 hydrochloride
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
|
-
- HY-105064D
-
|
CP-597396 hydrochloride hydrate
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
|
-
- HY-118402
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis .
|
-
- HY-132293
-
|
|
DNA-PK
|
Cancer
|
|
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer .
|
-
- HY-116386
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
GSK334429 is a selective and orally active non-imidazole histamine H3 receptor antagonist with a pKi of 9.49 against human H3 receptor. GSK334429 can be utilized in neurological research .
|
-
- HY-10195A
-
|
LY333531 mesylate
|
PKC
|
Cardiovascular Disease
Metabolic Disease
|
|
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes .
|
-
- HY-151434
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis .
|
-
- HY-162620
-
|
|
Adrenergic Receptor
|
Cancer
|
|
α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
|
-
- HY-15067
-
|
FG 9041
|
iGluR
|
Cancer
|
|
DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
|
-
- HY-141520
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- HY-77493
-
|
(rel)-ARQ 197; (rel)-(3R,4R)-ARQ 198
|
c-Met/HGFR
|
Cancer
|
|
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-145861
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells .
|
-
- HY-121383
-
|
AH5158; Sch-15719W free base
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-12753AS
-
|
SR35021-d7 hydrochloride
|
Thyroid Hormone Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-144642
-
|
|
PARP
|
Cancer
|
|
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model .
|
-
- HY-124366
-
|
|
Others
|
Infection
Cancer
|
|
Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
|
-
- HY-115977
-
|
|
Aldose Reductase
|
Inflammation/Immunology
|
|
Aldose reductase-IN-3 (Compound 5) is a potent and moderately selective inhibitor of aldose reductase (AR) with an IC50 of 3.99 μM. Aldose reductase has recently emerged as a molecular target that is involved in various inflammatory diseases, including sepsis. Aldose reductase-IN-3 has the potential for the research of sepsis .
|
-
- HY-U00443
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease .
|
-
- HY-132297
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer .
|
-
- HY-108661A
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF546 (hydrate) is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 (hydrate) stimulates release of interleukin-8 from human monocyte-derived dendritic cells .
|
-
- HY-132297A
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer .
|
-
- HY-103233
-
|
FG 9041 disodium salt
|
iGluR
|
Cancer
|
|
DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
|
-
- HY-124793A
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2 .
|
-
- HY-108661
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells .
|
-
- HY-170361
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
MTHFD2-IN-5 (Compound 16e) is a selective inhibitor for MTHFD2 with an IC50 of 66 nM. MTHFD2-IN-5 inhibits the proliferation of MOLM-14 with a GI50 of 720 nM. MTHFD2-IN-5 exhibits antitumor efficacy in mouse models .
|
-
- HY-124373
-
|
|
MMP
|
Metabolic Disease
|
|
ND-336 is a selective inhibitor of matrix metalloproteinase (MMP)-2, MMP-9, and MMP-14, with Kis of 85, 150, and 120 nM, respectively. ND-336 accelerates diabetic wound healing in mice by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound .
|
-
- HY-14431A
-
|
SAM-531 hydrochloride; PF-05212365 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Cerlapirdine hydrochloride is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine hydrochloride has the potential for researching the Alzheimer's disease .
|
-
- HY-123911
-
-
- HY-146267
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .
|
-
- HY-12245
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation .
|
-
- HY-103123
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases .
|
-
- HY-141898
-
|
|
Fluorescent Dye
|
Others
|
|
Biotin-4-aminophenol is a biotin-phenol analog. Biotin-4-aminophenol generates free radicals and conjugates to tyrosine residues in proteins more efficiently and selectively than the previously reported BP1 .
|
-
- HY-112094S
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
|
-
- HY-14753
-
|
|
Cannabinoid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosonabant is a selective antagonist for cannabinoid receptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder .
|
-
- HY-144391
-
|
|
Fungal
Antibiotic
|
Inflammation/Immunology
|
|
Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor (IC50=0.12 mM). Chitin synthase inhibitor 1 has potent antifungal activity against drug-resistant fungi variants .
|
-
- HY-103155
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease .
|
-
- HY-13775
-
XL019
5 Publications Verification
|
JAK
Apoptosis
|
Cancer
|
|
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
|
-
- 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-137451
-
|
S-600918
|
P2X Receptor
|
Neurological Disease
|
|
Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect .
|
-
- HY-108659
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research .
|
-
- HY-146371
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-13 (compound 13e) is a potent and selective inhibitor of COX-2 with an IC50 of 0.98 μM. COX-2-IN-13 is an anti-inflammatory agent. COX-2-IN-13 shows safety in-vivo acute toxicity study .
|
-
- HY-146370
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-12 (compound 3b) is a potent and selective inhibitor of COX-2 with an IC50 of 19.98 μM. COX-2-IN-12 is an anti-inflammatory agent. COX-2-IN-12 shows safety in-vivo acute toxicity study .
|
-
- HY-134885
-
|
RM-023
|
SHP2
Ras
|
Cancer
|
|
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction .
|
-
- HY-132283
-
PF-9363
1 Publications Verification
CTx-648
|
Histone Acetyltransferase
|
Cancer
|
|
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer .
|
-
- HY-136735
-
|
|
IRE1
|
Neurological Disease
Cancer
|
|
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) .
|
-
- HY-D0976
-
|
|
P2X Receptor
HIV
|
Infection
|
|
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
|
-
- HY-N1377R
-
|
|
Carboxylesterase
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Nevadensin (Standard) is the analytical standard of Nevadensin. This product is intended for research and analytical applications. Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive .
|
-
- HY-101911
-
5-BDBD
4 Publications Verification
|
P2X Receptor
|
Neurological Disease
|
|
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG) .
|
-
- HY-151519
-
|
|
Sirtuin
|
Cancer
|
|
SIRT2-IN-9 (compound 12) is a selective inhibitor of SRIT2 with an IC50 value of 1.3 μM. SIRT2-IN-9 inhibits proliferative activity of MCF-7 breast cancer cells. SIRT2-IN-9 can be used for the research of cancer .
|
-
- HY-70050C
-
|
GR 68755C; GR 68755 Hydrochloride; GR 68755X Hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-70050A
-
|
GR 68755; GR 68755X
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-120088
-
|
|
PCSK9
|
Cardiovascular Disease
|
|
PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region .
|
-
- HY-P1095
-
|
Caspase-3 Inhibitor VII
|
Caspase
|
Cardiovascular Disease
Neurological Disease
|
|
Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases .
|
-
- HY-145072
-
|
|
CDK
|
Cancer
|
|
BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .
|
-
- HY-136679
-
|
|
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
TD114-2 (cmpound 29) is a potent and highly selective inhibitor of glycogen synthase kinase-3β (GSK-3β) (IC50=48 nM). TD114-2 is associated with the hydrogen bond formation of arginine 141 (ARG141) specific to GSK-3β, an amino acid that is often a negatively charged residue in other kinases, which determines the high selectivity of GSK-3β. TD114-2 can be used in the study of diabetes, neurodegenerative diseases and other diseases associated with GSK-3β .
|
-
- HY-146792
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
|
-
- HY-145693
-
|
|
CDK
|
Others
|
|
CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively .
|
-
- HY-12960
-
|
FLT3-IN-1
|
FLT3
c-Kit
Apoptosis
|
Cancer
|
|
SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
|
-
- HY-119017
-
|
|
HDAC
|
Cancer
|
|
SB-429201 is a potent and selective HDAC1 (IC50~1.5 μM). SB-429201 displays at least a 20-fold preference for HDAC1 inhibition over HDAC3 and HDAC8 .
|
-
- HY-B1287
-
|
(±)-Citalopram hydrobromide; Lu 10-171
|
Serotonin Transporter
Autophagy
|
Neurological Disease
Cancer
|
|
Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
|
-
- HY-148316
-
|
|
VEGFR
|
Cancer
|
|
hVEGF-IN-2 (compound 19) is a selective VEGF (Flk-1) receptor tyrosine kinases (RTK) inhibitor with an IC50 value of 2.5 μM. hVEGF-IN-2 inhibits PDGF RTK activity with an IC50 value of 33.1 μM. hVEGF-IN-2 can be used for the development of RTK-specific agents .
|
-
- HY-158342
-
|
|
PROTACs
YAP
|
Cancer
|
|
PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
|
-
- HY-19263
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor .
|
-
- HY-108908
-
-
- HY-162671
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-12 is a selective BuChE inhibitor (IC50=0.52 µM) that acts via affecting CAS and PAS sites and has potential effects against oxidative stress. BuChE-IN-12 can be used in the study of Alzheimer's disease .
|
-
- HY-148060
-
|
|
JAK
|
Cancer
|
|
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively .
|
-
- HY-14362
-
|
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
|
-
- HY-119435
-
|
|
Herbicide
|
Others
|
|
Triallate is a selective preemergence herbicide for the control of wild oats in barley, spring wheat, Durum wheat, winter wheat, and sugar beets. Triallate inhibits fatty acid elongation and surface lipid (wax) biosynthesis .
|
-
- HY-142691
-
-
- HY-142692
-
-
- HY-107712
-
|
|
iGluR
|
Neurological Disease
|
|
TCN 213 is a selective, surmountable, glycine-dependentlly GluN1/GluN2A NMDAR antagonist with IC50s of 0.55, 3.5, 40 μM in the presence of 75, 750, 7500 nM glycine, respectively. TCN 213 can be used to monitor, pharmacologically, the switch in NMDAR expression in developing cortical neurones .
|
-
- HY-164397
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC50s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .
|
-
- HY-100543
-
|
ICI-118551
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Zenidolol (ICI-118551) is a selective β2 adrenergic receptor antagonist. Zenidolol inhibits β2-, β1- and β3-adrenergic receptor with Ki values of 0.7, 49.5 and 611 nM, respectively. Zenidolol can be used as an ocular hypotensive agent used for ophthalmic disease research .
|
-
- HY-12583
-
A-366
4 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-15546
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis .
|
-
- HY-B1871R
-
|
|
Herbicide
|
Others
|
|
Metolachlor (Standard) is the analytical standard of Metolachlor. This product is intended for research and analytical applications. Metolachlor is a pre-emergent selective, chloroacetanilide herbicide for the control of a variety of annual grass and broad leaf weeds in corn and other crops. Metolachlor is a chiral herbicide consisting of four stereoisomers .
|
-
- HY-122560A
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 μM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 μM) at -120 mV .
|
-
- HY-143900
-
|
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity .
|
-
- HY-122560
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV .
|
-
- HY-135456
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro4368554 is a brain-penetrant and selective 5-HT6 antagonist that reverses memory deficits induced by scopolamine and tryptophan depletion. Ro4368554 can be utilized in research related to memory deficits .
|
-
- HY-122482
-
-
- HY-101232
-
|
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .
|
-
- HY-19933
-
|
MK-4618
|
Adrenergic Receptor
|
Others
|
|
Vibegron (MK-4618) is a potent, highly selective and orally active β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder .
|
-
- HY-120738
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects .
|
-
- HY-123460
-
|
|
Somatostatin Receptor
|
Cancer
|
|
BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research .
|
-
- HY-101250
-
|
MDL11939
|
Serotonin Transporter
|
Neurological Disease
|
|
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
|
-
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
-
- HY-115905
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 9 (Compound 11) is a potent antimalarial agent. Antimalarial agent 9 is a quinoline-imidazole derivative compound. Antimalarial agent 9 exhibits significant antimalarial efficacy in-vitro against both CQ-sensitive (IC50-0.14 μM) and MDR strain (IC50-0.41 μM) with minimal cytotoxicity and high selectivity .
|
-
- HY-10656
-
|
|
Urotensin Receptor
|
Inflammation/Immunology
|
|
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
|
-
- HY-121383R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (Standard) is the analytical standard of Labetalol. This product is intended for research and analytical applications. Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-148198
-
-
- HY-111207
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity .
|
-
- HY-14431
-
|
SAM-531; PF-05212365
|
5-HT Receptor
|
Neurological Disease
|
|
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease .
|
-
- HY-136578
-
-
- HY-132857A
-
|
|
PROTACs
|
Neurological Disease
|
|
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells .
|
-
- HY-141514
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide .
|
-
- HY-170402
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
|
-
- HY-12501A
-
ITI-214
3 Publications Verification
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .
|
-
- HY-50687
-
|
(3S,4S)-ARQ 197; ARQ 198
|
c-Met/HGFR
|
Cancer
|
|
(3S,4S)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (3S,4S)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-12811
-
|
|
Sodium Channel
|
Neurological Disease
|
|
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
|
-
- HY-103459
-
|
PD156707
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration .
|
-
- HY-12072
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis .
|
-
- HY-144031S
-
-
- HY-139979
-
|
|
Deubiquitinase
|
Cancer
|
|
USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate .
|
-
- HY-146735
-
|
|
MNK
Apoptosis
|
Cancer
|
|
MNK1/2-IN-6 is a potent and selective MNK1/2 inhibitor with IC50s of 2.3 nM and 3.4 nM for MNK1 and MNK2, respectively. MNK1/2-IN-6 induces apoptosis in a concentration-dependent manner .
|
-
- HY-121018
-
|
BM-13505; SKF 96148
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury .
|
-
- HY-105182
-
|
LY-246708
|
mAChR
|
Neurological Disease
|
|
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
|
-
- HY-105318
-
|
|
Androgen Receptor
|
Metabolic Disease
Endocrinology
|
|
LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction .
|
-
- HY-141680
-
CPS2
1 Publications Verification
|
PROTACs
CDK
|
Cancer
|
|
CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia .
|
-
- HY-11011
-
|
|
Src
|
Inflammation/Immunology
|
|
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection .
|
-
- HY-132231
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
|
-
- HY-128129
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-100195
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
|
-
- HY-100516
-
|
UR-8880
|
COX
|
Inflammation/Immunology
|
|
Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar .
|
-
- HY-145843
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes .
|
-
- HY-162173
-
|
|
COX
|
Inflammation/Immunology
|
|
WYZ90 ((compound 6a) is a potent and selective COX-2 inhibitor with IC50 values of 75, 5734, 19940 nM for COX-2, COX-1 and DPPH, respectively. WYZ90 shows antioxidant and analgesic activity .
|
-
- HY-133747
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research .
|
-
- HY-108254
-
|
Arcyriarubin A
|
PKC
CMV
|
Infection
|
|
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM) . Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM .
|
-
- HY-163548
-
|
|
Sialyltransferase
|
Cancer
|
|
SPP-002 is a sulfate analogue that acts as a potential Sialyltransferase (ST) inhibitor. SPP-002 selectively inhibits n-glycosialylation with inhibition at least an order of magnitude greater than that of unmodified parental cholic acid (LCA). SPP-002 reduces tumor cell migration and invasion by inhibiting the integrin /FAK/Paxillin signaling pathway. SPP-002 can be used in the study of tumor metastasis .
|
-
- HY-134188
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders .
|
-
- HY-114231B
-
|
ELX-02 disulfate; NB-124 disulfate
|
Others
|
Metabolic Disease
|
|
Exaluren (ELX-02) disulfate is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). Exaluren disulfate is being developed as a therapy for genetic diseases caused by nonsense mutations .
|
-
- HY-114231C
-
|
ELX-02 sulfate; NB-124 sulfate
|
Others
|
Metabolic Disease
|
|
Exaluren (ELX-02) sulfate is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). Exaluren sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations .
|
-
- HY-156532C
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
(-)-5-HT2C agonist-3 (compound (–)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values ??for 5-HT2 receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research .
|
-
- HY-12501
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .
|
-
- HY-151413
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
|
-
- HY-117378
-
|
KRP-204
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
N-5984 (KRP-204) is a potent and selective agonist of β3-adrenergic receptor. N-5984 has the potential for developing as one of the clinically effective drugs for obesity and diabetes mellitus .
|
-
- HY-110201
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
|
-
- HY-141521
-
|
NX-13
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
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NX-13 is a first-in-class, orally active and gut-restricted agent that selectively targets and activates the NLRX1 pathway to induce immunometabolic changes. NX-13 results in lower inflammation and responses in inflammatory bowel disease. NX-13 can be used for the research of crohn's disease and ulcerative colitis .
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- HY-114322
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VZ185
1 Publications Verification
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PROTACs
Epigenetic Reader Domain
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Cancer
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VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively .
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- HY-105215
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Neurokinin Receptor
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Inflammation/Immunology
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FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
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- HY-P10571
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Melanocortin Receptor
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Endocrinology
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GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
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- HY-148243
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STL5-T-0057
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Aldehyde Dehydrogenase (ALDH)
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Cancer
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IGUANA-1 free base (STL5-T-0057) is an selective ALDH1 B1 inhibitor with an IC50 value of 30 nM. IGUANA-1 free base inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC50 values of 2.46 and 0.39 μM, respectively. IGUANA-1 free base can be used for the research of cancer .
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- HY-P1135
-
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Neuropeptide Y Receptor
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Neurological Disease
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M1145, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 has an additive effect on the signal transduction of galanin .
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- HY-107642
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Motilin Receptor
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Metabolic Disease
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MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility .
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- HY-137955
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P2Y Receptor
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Cardiovascular Disease
Others
Neurological Disease
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MRS 2211 sodium hydrate is a competitive P2Y13 receptor antagonist (pIC50= 5.97). MRS 2211 sodium hydrate is highly selective to the P2Y13 receptor, showing more than 20-fold selectivity compared to the P2Y1 and P2Y12 receptors. MRS 2211 sodium hydrate can be used to further investigate the role of the P2Y13 receptor in different physiological and pathological processes, such as its function in blood cells, the nervous system and the immune system .
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- HY-151460
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Eukaryotic Initiation Factor (eIF)
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Cancer
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GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo .
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- HY-19706
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ARS-853
4 Publications Verification
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Ras
Apoptosis
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Cancer
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ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
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- HY-70050B
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GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)
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5-HT Receptor
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Neurological Disease
Inflammation/Immunology
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Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
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- HY-70050
-
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GR 68755 (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))
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5-HT Receptor
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Neurological Disease
Inflammation/Immunology
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|
Alosetron (GR 68755) Hydrochloride(1:X) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride(1:X) is used for the research of irritable bowel syndrome (IBS). Alosetron Hydrochloride(1:X) blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride(1:X) attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
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- HY-P1135A
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Neuropeptide Y Receptor
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Neurological Disease
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M1145 TFA, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 TFA shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 TFA has an additive effect on the signal transduction of galanin .
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- HY-146074
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Proton Pump
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Cancer
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RUVBL1/2 ATPase-IN-1 (compound 18) is a potent and selective inhibitor of RUVBL1/2 ATPase with IC50 values of 6.0 and 7.7 μM, respectively. RUVBL1 and RUVBL2 are highly conserved AAA ATPases (ATPases Associated with various cellular Activities) and highly relevant to the progression of cancer. RUVBL1/2 ATPase-IN-1 has the potential for the research of cancer diseases .
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- HY-120290
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Histone Acetyltransferase
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Cancer
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PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity .
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- HY-142283BS
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EGFR
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Cancer
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N-Desmethyl dosimertinib-d5 is the deuterium labeled Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
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- HY-142283CS
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EGFR
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Cancer
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N-Methyl-dosimertinib-d5 is the deuterium labeled of Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
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- HY-163771
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Pyruvate Carboxylase (PC)
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Metabolic Disease
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Pyruvate Carboxylase-IN-5 (compound 6m) is a pyruvate carboxylase inhibitor with high selectivity and permeability. Pyruvate carboxylase is a mitochondrial enzyme that catalyzes the carboxylation of pyruvate to oxaloacetate, a process that plays an important role in maintaining steady-state levels of Krebs cycle intermediates, which are precursors for the synthesis of biomacromolecules such as amino acids, fatty acids, and glucose .
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- HY-15011
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Oxytocin Receptor
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Others
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L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
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- HY-158762
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SHP2
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Cancer
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TK-642 is a highly active, selective, orally activity SHP2 inhibitor based on pyrazole and pyrazine (IC50=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer .
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- HY-N1638
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Monoamine Oxidase
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Neurological Disease
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1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC50 and Ki values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS .
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- HY-19553
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Epigenetic Reader Domain
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Inflammation/Immunology
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LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells .
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- HY-14180
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IKK
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Inflammation/Immunology
|
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PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation .
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- HY-152671
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Monoamine Oxidase
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Neurological Disease
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hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
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- HY-169402
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Phosphodiesterase (PDE)
NO Synthase
Reactive Oxygen Species
|
Inflammation/Immunology
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PDE1-IN-9 (Compound 7a) is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 exhibits good metabolic stability in rat liver microsomes .
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- HY-111262
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11β-HSD
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Neurological Disease
Metabolic Disease
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ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .
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- HY-161511
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5-HT Receptor
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Neurological Disease
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LPH-5 is a selective 5-HT2A receptor agonist (EC50=190 nM). LPH-5 works by selectively activating the 5-HT2A receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the 5-HT2A receptor. LPH-5 can be used to further explore the 5-HT2A receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders .
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- HY-101308
-
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P2Y Receptor
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Cardiovascular Disease
|
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MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium inhibits platelet aggregation .
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- HY-101308A
-
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P2Y Receptor
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Cardiovascular Disease
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MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium hydrate inhibits platelet aggregation .
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- HY-16981
-
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CXCR
|
Inflammation/Immunology
|
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SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells .
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- HY-101254
-
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N-0774
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Melatonin Receptor
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Neurological Disease
|
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Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
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- HY-145906
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Dopamine Receptor
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Neurological Disease
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|
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .
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- HY-112090
-
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|
Epigenetic Reader Domain
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
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- HY-103197
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RX821002 hydrochloride
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Adrenergic Receptor
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Neurological Disease
|
|
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2) .
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- HY-12248A
-
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CB-839 hydrochloride
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Glutaminase
Autophagy
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Cancer
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Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
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- HY-12248
-
|
CB-839
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Glutaminase
Autophagy
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Cancer
|
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Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
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- HY-133122
-
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TNF Receptor
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Inflammation/Immunology
Cancer
|
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UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer.?UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar?Kd?of 13?nM .
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- HY-144639
-
-
- HY-111548
-
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Microtubule/Tubulin
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Others
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|
Spastazoline is a selective spastin (a microtubule-severing AAA protein) inhibitor, with an IC50 of 99 nM for Human spastin. Spastazoline can be used for cell division- and intracellular vesicle transport-related research .
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- HY-13260
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Akt
Autophagy
Apoptosis
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Cancer
|
|
CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.
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- HY-10081
-
GS-6201
1 Publications Verification
CVT-6883
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Adenosine Receptor
|
Inflammation/Immunology
|
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GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) . GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
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- HY-16405
-
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-16406
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-119435R
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Herbicide
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Others
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Triallate (Standard) is the analytical standard of Triallate. This product is intended for research and analytical applications. Triallate is a selective preemergence herbicide for the control of wild oats in barley, spring wheat, Durum wheat, winter wheat, and sugar beets. Triallate inhibits fatty acid elongation and surface lipid (wax) biosynthesis .
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- HY-16758
-
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AR-12286
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ROCK
|
Neurological Disease
|
|
Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork .
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- HY-132978
-
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Biochemical Assay Reagents
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Others
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|
SulfoxFluor is a deoxyfluorination reagent that can be used in the rapid deoxyfluorination of various alcohols. SulfoxFluor plays an important role in deoxyazidation process which converts a broad range of alcohols into alkyl azides at room temperature. SulfoxFluor is shelf-stable, easy-to-handle, fluorine-economical, and highly selective
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- HY-170510
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Galectin
|
Cancer
|
|
GB2095 is a selective, orally active inhibitor for galectin-3 with Kd of 36 nM and 0.35 μM for human galectin-3 and mouse galectin-3. GB2095 exhibits antitumor efficacy in mouse models .
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- HY-109143
-
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ABBV-105
|
Btk
|
Inflammation/Immunology
|
|
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .
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- HY-101333
-
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(RS)-CPPG
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mGluR
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Neurological Disease
|
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CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors .
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- HY-141677B
-
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Histone Demethylase
|
Cancer
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INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes .
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- HY-161663
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
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- HY-168091
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NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
|
YM-I-26 is a selective NLRP3 inflammasome inhibitor. YM-I-26 enhances the phagocytosis of β-amyloid protein by mouse microglial BV2 cells and inhibits the production of IL-1β and IL-10. YM-I-26 can be used to study the immunomodulatory activity associated with inflammation .
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- HY-144863
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GnRH Receptor
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Cancer
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BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids .
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- HY-143439
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Estrogen Receptor/ERR
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Cancer
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LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
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- HY-144131
-
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Apoptosis
RET
|
Cancer
|
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RET-IN-11 is a potent and selective RET inhibitor with IC50s of 6.20 nM, 18.68 nM for RET and RET V804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis .
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- HY-14221B
-
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LU-28-179 fumarate
|
Sigma Receptor
|
Cancer
|
|
Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
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- HY-101903A
-
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FABP
|
Cardiovascular Disease
Metabolic Disease
|
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BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
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- HY-108611
-
AACOCF3
3 Publications Verification
Arachidonyl trifluoromethyl ketone
|
Phospholipase
|
Cardiovascular Disease
|
|
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease .
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-
- HY-14221
-
|
Lu 28-179
|
Sigma Receptor
|
Cancer
|
|
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
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-
- HY-101903
-
|
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FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
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-
- HY-14221A
-
|
Lu 28-179 hydrochloride
|
Sigma Receptor
Ferroptosis
|
Cancer
|
|
Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
|
-
- HY-P1435
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-18054A
-
|
|
11β-HSD
|
Inflammation/Immunology
|
|
BVT-2733 hydrochloride is a potent, selective and orally active nonsteroidal 11β-HSD1 inhibitor. BVT-2733 hydrochloride is more potent against mouse 11β-HSD1 enzyme (IC50=96 nM) than against human 11β-HSD1 enzyme (IC50=3341 nM). BVT-2733 hydrochloride has the potential to be used in the study of arthritis and obesity-related diseases .
|
-
- HY-163476
-
|
|
Phosphatase
|
Inflammation/Immunology
Cancer
|
|
PIP5K1C-IN-1 (Compound 30) is a potent PIP5K1C inhibitor, with an IC50 of 0.80 nM. PIP5K1C-IN-1 exhibits low total clearance in mice and high levels of kinase selectivity. PIP5K1C-IN-1 can be used for the research of cancer and chronic pain .
|
-
- HY-105896
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties .
|
-
- HY-69172
-
-
- HY-123532
-
|
VUF6002
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively .
|
-
- HY-13335
-
|
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε) .
|
-
- HY-19747
-
HPOB
3 Publications Verification
|
HDAC
Apoptosis
|
Cancer
|
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
|
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
- HY-117829
-
UNC9994
1 Publications Verification
|
Dopamine Receptor
5-HT Receptor
Histamine Receptor
Arrestin
|
Neurological Disease
|
|
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
|
-
- HY-123976A
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
MPT0G211 mesylate is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 mesylate can penetrate the blood-brain barrier. MPT0G211 mesylate ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 mesylate has anti-metastatic and neuroprotective effects. Anticancer activities .
|
-
- HY-123976
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291?nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities .
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
|
-
- HY-107558
-
|
VUF6002 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively .
|
-
- HY-103444
-
|
|
MMP
|
Cancer
|
|
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM) .
|
-
- HY-107732
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors .
|
-
- HY-118301
-
|
|
GABA Receptor
|
Neurological Disease
|
|
ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .
|
-
- HY-147775
-
|
|
Ceramidase
|
Inflammation/Immunology
|
|
NAAA-IN-3 (Compound 17a) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-3 has the potential for the research of inflammation and pain .
|
-
- HY-147773
-
|
|
Ceramidase
|
Inflammation/Immunology
|
|
NAAA-IN-1 (Compound 1) is a potent and selective inhibitor of NAAA with an IC50 of 7 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-1 has the potential for the research of inflammation and pain .
|
-
- HY-132817
-
|
ICP-192
|
FGFR
|
Cancer
|
|
Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer . Gunagratinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
|
-
- HY-P10280
-
|
|
ATM/ATR
|
Cancer
|
|
ATR kinase substrate peptide (compound 45) is a potent and selective inhibitor of ATR (Ataxia Telangiectasia and Rad3 related) protein kinase (Ki=6 nM). ATR kinase substrate peptide inhibits ATR activity by competing with ATR kinase ATP-binding sites to block ATR mediated signaling. ATR kinase substrate peptide can be used to study the role of ATR kinase in DNA damage response .
|
-
- HY-103258
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM) .
|
-
- HY-144309
-
|
|
Cytochrome P450
|
Neurological Disease
|
|
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier .
|
-
- HY-106168
-
|
NB1011
|
Thymidylate Synthase
|
Cancer
|
|
Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin) .
|
-
- HY-13260A
-
|
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity .
|
-
- HY-155079
-
|
|
EGFR
|
Cancer
|
|
DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
|
-
- HY-12331
-
-
- HY-P99004
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family .
|
-
- HY-122140
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
ACG548B (compound 24) is a potent inhibitor of acetyl- and butyrylcholinesterase (AChE and BChE) with IC50s of 1.78 and 0.496 μM, respectively. ACG548B has higher AChE affinity and selectivity over BChE and ChoK (choline kinase) .
|
-
- HY-13556
-
|
LY353381; SERM III
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile .
|
-
- HY-139300
-
|
HMPL-813
|
EGFR
|
Cancer
|
|
Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer . Epitinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-132308
-
|
|
DYRK
|
Neurological Disease
|
|
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe .
|
-
- HY-169884
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
MCI-INI-3 is a selective competitive inhibitor of human ALDH1A3 (with a Ki value of 0.55 μM for ALDH1A3 and a Ki value of 78.2 μM for ALDH1A1). MCIINI-3 inhibits the biosynthesis of retinoic acid and reduces the viability of GSC-83 and GSC-326 glioblastoma cells .
|
-
- HY-115996
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity .
|
-
- HY-124569
-
|
|
iGluR
|
Neurological Disease
|
|
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .
|
-
- HY-107425
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively .
|
-
- HY-158763
-
|
TG0205221
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
|
MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .
|
-
- HY-114436
-
|
|
Ras
|
Cancer
|
|
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
|
-
- HY-120184
-
|
AZ13713945
|
mAChR
|
Neurological Disease
|
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
|
-
- HY-164036
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Lolamicin is a Gram-negative specific antibiotic. Lolamicin is active against more than 130 multidrug-resistant clinical isolates, has shown efficacy in multiple mouse models of acute pneumonia and sepsis infection, and protects the gut microbiome of mice against secondary infection with Clostridium difficile. The selective killing of pathogenic gram-negative bacteria by Lolamicin is a result of the low sequence homology of pathogenic bacteria and symbiotic bacteria. Lolamicin can be used in the study of infection caused by Gram-negative pathogens .
|
-
- HY-170499
-
|
BI02982816
|
mGluR
|
Neurological Disease
|
|
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
|
-
- HY-156419A
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-16 free base is the free base form of PARP7-IN-16 (HY-156419). PARP7-IN-16 free base is a selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-D1601
-
|
|
Fluorescent Dye
|
Others
|
|
N-Aminofluorescein is a fluorescein hydrazide with spiro form, a highly selective and sensitive fluorescence probe for Cu 2+. N-Aminofluorescein has no selective fluorescence response to other common metal ions, can be used for direct detection of Cu 2+ in biological systems with λex/em=495/516 nm .
|
-
- HY-145855
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis .
|
-
- HY-18969
-
|
|
CDK
|
Cancer
|
|
LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment .
|
-
- HY-144316
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease .
|
-
- HY-147695
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
|
-
- HY-133012
-
|
|
TRP Channel
|
Neurological Disease
|
|
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
|
-
- HY-143885
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells .
|
-
- HY-139300A
-
|
HMPL-813 succinate
|
EGFR
|
Cancer
|
|
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145697
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis .
|
-
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
-
- HY-144127
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-109012A
-
|
JNJ-42847922 hydrochloride
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
|
-
- HY-123981
-
|
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
- HY-131040
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) .
|
-
- HY-118944
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
L-748328 is a potent and selective human β3-adrenergic receptor antagonist. L-748328 has a Ki of 3.7 nM against human cloned β3-AR expressed in Chinese hamster ovary (CHO) cells. In addition, L-748328 inhibits the lipolytic response induced by the β3-AR agonist L-742791 in isolated non-human primate adipocytes .
|
-
- HY-19057
-
|
MK-467; L-659066
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
|
-
- HY-126323
-
|
|
Parasite
|
Infection
|
|
TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM) .
|
-
- HY-126323B
-
|
|
Parasite
|
Infection
|
|
TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC50=320 nM) .
|
-
- HY-14171
-
|
LGD1069
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
|
-
- HY-134283
-
|
|
PKA
Apoptosis
|
Others
|
|
8-Benzylthio-cAMP is a derivative of cyclic adenosine monophosphate (cAMP). 8-Bn-cAMP is a site-selective activator of cAMP-dependent protein kinases. Compared with cyclic adenosine monophosphate, it is more stable to phosphodiesterase (PDE) hydrolysis and has higher membrane permeability. 8-Bn-cAMP can be used to study the role of cAMP in regulating cell proliferation, differentiation and apoptosis .
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-
- HY-132300
-
|
|
β-catenin
|
Cancer
|
|
ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM .
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-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
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-
- HY-W107024
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively .
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-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
|
-
- HY-101292
-
|
|
PPAR
|
Metabolic Disease
|
|
FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes .
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-
- HY-155693
-
|
|
Topoisomerase
Parasite
|
Infection
|
|
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research .
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-
- HY-120350
-
BI-1347
1 Publications Verification
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CDK
|
Cancer
|
|
BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity .
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-
- HY-149136
-
|
|
Integrin
TGF-beta/Smad
|
Inflammation/Immunology
|
|
MORF-627 is a selective, orally active inhibitor for integrin αvβ6 with an IC50 of 9.2 nM measuring by human serum ligand binding assay. MORF-627 inhibits αvβ6-mediated TGF-β1 activation with an IC50 of 2.63 nM, inhibits SMAD2/3 phosphorylation with an IC50 of 8.3 nM. MORF-627 ameliorates the Bleomycin (HY-108345)-induced mouse lung fibrosis .
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-
- HY-14363
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity . TUG-424 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145080
-
|
|
Dynamin
|
Neurological Disease
|
|
Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis . CME: Clathrin mediated endocytosis
|
-
- HY-151537
-
|
|
Fluorescent Dye
|
Infection
Inflammation/Immunology
|
|
Gol-NTR is a Golgi-targetable probe with high selectivity and sensitivity. Gol-NTR is Nitroreductase (NTR)-activated and has visualization acute lung injury (ALI) and repair function. Gol-NTR has a low detection limit of 54.8 ng/mL. Gol-NTR can be used for the research for monitoring and assessing research response of sepsis-induced ALI .
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-
- HY-106684A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
|
-
- HY-118091
-
|
|
5 alpha Reductase
|
Endocrinology
|
|
LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1 .
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-126323A
-
|
|
Parasite
|
Infection
|
|
TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC50=320 nM) .
|
-
- 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-106684
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
|
-
- HY-164145
-
|
|
TGF-β Receptor
|
Others
Cancer
|
|
CDD-1653 is a potent and selective BMPR2 inhibitor (IC50=2.8 nM). CDD-1653 reduces the ability of ATP to bind to the kinase domain of BMPR2, thereby affecting the phosphorylation of SMAD1/5/8 transcription factors, which play a key role in the BMP signaling pathway. CDD-1653 can be used to study diseases related to the BMP signaling pathway .
|
-
- HY-132305
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth .
|
-
- HY-101189
-
|
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
|
-
- HY-101189B
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
|
-
- HY-12830
-
|
|
Pim
|
Cancer
|
|
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM .
|
-
- HY-151578
-
|
|
Dipeptidyl Peptidase
Carbonic Anhydrase
|
Metabolic Disease
|
|
DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively .
|
-
- HY-151425
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo .
|
-
- HY-120159
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity .
|
-
- HY-132300A
-
|
|
β-catenin
|
Cancer
|
|
ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM .
|
-
- HY-109012
-
|
JNJ-42847922
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
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-
- HY-144660
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
|
-
- HY-100360
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-100360A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-115986
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD) .
|
-
- HY-162712
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX-201 is a selective agonist for OX2R with an EC50 of 8 nM. Pathological proteins produced by neurons are released into the interstitial fluid (ISF) in a manner dependent on neuronal activity and are cleared from the brain via lymphatic pathways. The outflow of pathological proteins to the ISF is related to the arousal state of neurons. OX-201 can induce neuronal awakening and promote the release of tau into the hippocampal ISF. Although OX-201 does not alter hippocampal tau levels, it has potential applications for Alzheimer's disease (AD) associated with sleep/wake rhythm disturbances .
|
-
- HY-18071A
-
|
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-135783
-
AT 1001
1 Publications Verification
|
nAChR
|
Neurological Disease
|
|
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
|
-
- HY-11009
-
|
|
CDK
PKC
|
Cancer
|
|
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
|
-
- HY-18071
-
BI-9627
2 Publications Verification
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-111790
-
M3258
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
|
-
- HY-121852
-
|
SCH-225336
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice .
|
-
- HY-19599
-
|
(+)-Vorozole; R83842
|
Cytochrome P450
|
Cancer
|
|
Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor . Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer .
|
-
- HY-158981
-
|
|
Herbicide
|
Others
|
|
Herbicide safener-3 is a compound that increases the selectivity of herbicides. Herbicide safener-3 is often used together with herbicides, particularly those that can be harmful to crops. Herbicide safener-3 reduces the negative effects of herbicide on the crop by regulating metabolic differences between the crop and the weed while still allowing the herbicide to be effective on the weed. Herbicide safener-3 can be used in research that improves herbicide application effectiveness and crop safety .
|
-
- HY-18862
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
|
-
- HY-14171R
-
|
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene (Standard) is the analytical standard of Bexarotene. This product is intended for research and analytical applications. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
|
-
- HY-16635
-
|
ACT-129968; KYTH-105
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis .
|
-
- HY-A0037
-
|
CP-336156
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
|
Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
|
-
- HY-144624
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
|
-
- HY-150076
-
|
|
PKA
|
Metabolic Disease
Cancer
|
|
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research .
|
-
- HY-144627
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 μM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
|
-
- HY-114419
-
|
KZR-616
|
Proteasome
|
Inflammation/Immunology
|
|
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases .
|
-
- HY-145838
-
|
|
AAK1
|
Neurological Disease
|
|
AAK1-IN-4 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 4.6 nM, Filt Ki of 0.9 nM, and cell IC50 of 8.6 nM). AAK1-IN-4 has the potential for the research for neuropathic pain .
|
-
- HY-114732
-
|
|
Adrenergic Receptor
|
Others
|
|
Procaterol is an oral selective β2 adrenergic receptor agonist. Procaterol inhibits eosinophil migration and the release of eosinophil chemotactic factor from BEAS-2B cells through a cyclic AMP-dependent mechanism. Procaterol has a large dose difference existing between the bronchodilator effect and the anabolic effect in rat, can be used for asthma research in athletes .
|
-
- HY-114419A
-
|
KZR-616 maleate
|
Proteasome
|
Inflammation/Immunology
|
|
Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases .
|
-
- HY-145839
-
|
|
AAK1
|
Neurological Disease
|
|
AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain .
|
-
- HY-130612
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-145925C
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
(S,R)-CFT8634 (compound 176) is a selective and orally active PROTAC-class BRD9 protein degrader. (S,R)-CFT8634 has the potential to study BRD9-mediated diseases, including but not limited to abnormal cell proliferation. (S,R)-CFT8634 consists of a target protein ligand (red part) BRD9 ligand-5 (HY-169988), an E3 ligase ligand (blue part) CRBN ligand-11 (HY-169989), and a PROTAC linker (black part) 1-(3,3-Difluoro-4-piperidinyl)piperazine (HY-169991). E3 ligase ligand and linker can form E3 Ligase Ligand-linker Conjugate 142 (HY-169990) .
|
-
- HY-151813
-
|
|
Fluorescent Dye
|
Cancer
|
|
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-141429C
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-144614
-
|
|
DYRK
Apoptosis
|
Neurological Disease
Cancer
|
|
JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
|
-
- HY-141429
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-110381
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
JNJ-DGAT2-A is a selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. JNJ-DGAT2-A can be used for the research of triglyceride (TG) synthesis .
|
-
- HY-101029
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
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-
- HY-148135
-
|
|
Carbonic Anhydrase
|
Neurological Disease
|
|
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy .
|
-
- HY-13001
-
|
AC220; AC708
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
|
Cancer
|
|
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
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-
- HY-125629
-
|
|
Others
|
Others
|
|
Primordazine B is a small molecule compound identified by chemical screening in zebrafish embryos with the activity of selectively destroying Primordial Germ Cells (PGCs). Primordazine B inhibits a process called Poly(A)-tail Independent Non-canonical Translation (PAINT) without inhibition of polyadenylate tail dependent typical translation (PAT). Primordazine B can be used to study translational control of cells in specific physiological or pathological states, such as gene expression regulation during cell dormancy, viral infection, or stress conditions .
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-
- HY-12363
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
U-69593 is a potent and selective κ1-opioid receptor agonist . U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
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-
- HY-11079
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter .
|
-
- HY-152171
-
|
|
Monoamine Transporter
|
Neurological Disease
|
|
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder .
|
-
- HY-115907
-
|
|
Ras
ERK
Apoptosis
|
Cancer
|
|
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
|
-
- HY-163806
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .
|
-
- HY-141429A
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-12908
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL) .
|
-
- HY-152219
-
|
|
CDK
|
Infection
Cancer
|
|
CLK1-IN-2 is metabolically stable Clk1 inhibitor. CLK1-IN-2 has selectivity for Clk1 with an IC50 value of 1.7 nM. CLK1-IN-2 can be used for the research of tumour, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza .
|
-
- HY-115989
-
|
|
HCV
|
Infection
|
|
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
|
-
- HY-10624
-
THIQ
1 Publications Verification
|
Melanocortin Receptor
|
Metabolic Disease
|
|
THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
|
-
- HY-153114
-
|
|
FXR
|
Inflammation/Immunology
|
|
HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis .
|
-
- HY-106993A
-
|
GT-2331 maleate
|
Histamine Receptor
|
Neurological Disease
|
|
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146755
-
|
|
Trk Receptor
|
Cancer
|
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
|
-
- HY-141547
-
|
|
Sodium Channel
Cytochrome P450
|
Inflammation/Immunology
|
|
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain .
|
-
- HY-106993
-
|
GT-2331
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-134990
-
|
|
Apoptosis
|
Cancer
|
|
Hematoporphyrin monomethyl ether, second generation of porphyrin-related photosensitizer, is characterized by its single form, high yield of singlet oxygen, high selectivity, and low toxicity, which has been widely used in the diagnosis and research of various tumors, including lung cancer, bladder cancer, and nevus flammeus and brain glioma .
|
-
- HY-146782
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
|
-
- HY-101029A
-
|
|
NEKs
Ribosomal S6 Kinase (RSK)
DYRK
Apoptosis
|
Cancer
|
|
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-131337
-
|
|
Bacterial
|
Infection
|
|
RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections . RhlR antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-13001R
-
|
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
Autophagy
|
Cancer
|
|
Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
|
-
- HY-14217
-
|
AC220 dihydrochloride
|
FLT3
Apoptosis
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .
|
-
- HY-10251
-
|
AC480
|
EGFR
|
Cancer
|
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
- HY-144306
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
|
-
- HY-B0233
-
|
PN 200-110
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
- HY-114436S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
|
-
- HY-145086
-
|
|
Neuromedin U Receptor (NMUR)
|
Metabolic Disease
|
|
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
|
-
- HY-103066
-
|
|
nAChR
|
Neurological Disease
|
|
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
|
-
- HY-162424
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Cancer
|
|
ZBP1/RIP3/MLKL activator 1 (compound 3a) is a synthetically derived quinoline compound. ZBP1/RIP3/MLKL Activator 1 induces DNA damage, enhances intracellular levels of reactive oxygen species (ROS), and triggers apoptosis via the caspase pathway. Furthermore, when apoptosis is inhibited, ZBP1/RIP3/MLKL Activator 1 promotes necroptotic cell death through the ZBP1-RIP3-MLKL pathway. ZBP1/RIP3/MLKL Activator 1 is utilized in oncological research, particularly in the selective targeting of cells with impaired apoptotic function .
|
-
- HY-158102
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
|
-
- HY-150752
-
|
|
Btk
Pyroptosis
|
Cancer
|
|
BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis .
|
-
- HY-112461
-
|
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 is a Gsα-selective G Protein antagonist. NF449 suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
|
-
- HY-135985
-
|
|
Fluorescent Dye
|
Cancer
|
|
DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-163783
-
|
|
Casein Kinase
|
Infection
|
|
CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
|
-
- HY-16677A
-
|
MDL72974A
|
Monoamine Oxidase
|
Neurological Disease
|
|
Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) .
|
-
- HY-A0038
-
|
CP-336156 tartrate
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM) . Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis .
|
-
- HY-145884
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-8 is a potent and selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM) .
|
-
- HY-108519
-
|
|
ROCK
|
Neurological Disease
|
|
AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
|
-
- HY-148236
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation .
|
-
- HY-14342
-
MK-5046
2 Publications Verification
|
Bombesin Receptor
|
Metabolic Disease
|
|
MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
- HY-108425
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
|
-
- HY-119101
-
|
|
CCR
Potassium Channel
P-glycoprotein
|
Inflammation/Immunology
|
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
|
-
- HY-116227
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion .
|
-
- HY-143889
-
|
|
CDK
|
Cancer
|
|
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
|
-
- HY-144605
-
|
|
EGFR
PROTACs
|
Cancer
|
|
PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
|
-
- HY-B0442C
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-150687
-
|
|
ERK
|
Metabolic Disease
|
|
ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM .
|
-
- HY-112461A
-
|
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
|
-
- HY-142723
-
|
|
Potassium Channel
|
Neurological Disease
|
|
KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype .
|
-
- HY-13499
-
|
CCR2 antagonist 5
|
CCR
|
Inflammation/Immunology
|
|
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
|
-
- HY-A0036
-
|
TSE-424 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-101343
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
|
-
- HY-100554
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
|
-
- HY-161783
-
|
|
HDAC
Keap1-Nrf2
Reactive Oxygen Species
Apoptosis
|
Neurological Disease
|
|
HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability .
|
-
- HY-B0442
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442A
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-143472
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
|
-
- HY-108462
-
ML-SA1
3 Publications Verification
|
Dengue Virus
TRP Channel
Flavivirus
|
Infection
|
|
ML-SA1, as a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral .
|
-
- HY-A0031
-
|
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-142735
-
|
|
Potassium Channel
|
Neurological Disease
|
|
KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively
|
-
- HY-N7536
-
|
|
TRP Channel
|
Others
|
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
|
-
- HY-163670
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
TLR7 agonist 21 (Compound 27B) is a selective agonist for Toll-like receptor 7(TLR7), with an EC50 of 17.53 nM (for human TLR7) and 41.7 nM (for mouse TLR7). TLR7 agonist 21 stimulates the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, IFN-α1, and IL-4. TLR7 agonist 21 acts as a vaccine adjuvant, increases levels of IgG and IgA, and protects the mouse from influenza virus infections .
|
-
- HY-127102
-
|
DDD01305143
|
Parasite
Proteasome
|
Infection
|
|
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties .
|
-
- HY-114504
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models .
|
-
- HY-130605
-
|
|
P2X Receptor
|
Neurological Disease
|
|
BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects .
|
-
- HY-162616
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
|
-
- HY-A0031A
-
|
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .
|
-
- HY-15256A
-
|
BI 201335 sodium
|
HCV Protease
|
Infection
|
|
Faldaprevir sodium is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir sodium inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir sodium has potent antiviral activity against chronic HCV infection .
|
-
- HY-146738
-
|
|
Akt
|
Cancer
|
|
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
|
-
- HY-B0442B
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0233R
-
|
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
- HY-124744
-
|
|
FAAH
|
Neurological Disease
|
|
ASP 8477 is an orally active and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 values of 3.99, 1.65, and 57.3 nM for human FAAH-1, FAAH-1 (P129T), and FAAH-2, respectively. ASP 8477 has central nervous system activity and can be used in analgesia research .
|
-
- HY-B0233S2
-
|
PN 200-110-d7
|
Calcium Channel
Autophagy
Isotope-Labeled Compounds
|
Cardiovascular Disease
Neurological Disease
|
|
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
- HY-144074
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease .
|
-
- HY-47888
-
|
|
Integrin
|
Inflammation/Immunology
|
|
PLN-1474 (compound 1) is an orally active and selective ανβ1 integrin inhibitor with an IC50 value of <50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or researching a fibrotic or cirrhotic disease or disorder.
|
-
- HY-15256
-
|
BI 201335
|
HCV Protease
|
Infection
|
|
Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection .
|
-
- HY-B0442CR
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-144126
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
|
-
- HY-130149
-
|
MRTX849
|
Ras
|
Cancer
|
|
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
|
-
- HY-P10388
-
|
|
CD47
TGF-β Receptor
|
Cancer
|
|
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
|
-
- HY-164384
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
|
-
- HY-19927A
-
|
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
|
-
- HY-146226
-
|
|
Enterovirus
|
Infection
|
|
Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity .
|
-
- HY-14342A
-
|
|
Bombesin Receptor
|
Metabolic Disease
|
|
(R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
- HY-131879
-
|
|
Sodium Channel
|
Neurological Disease
|
|
NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits .
|
-
- HY-145384
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca 2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases .
|
-
- HY-161392
-
|
|
CRM1
|
Cancer
|
|
CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
|
-
- HY-161391
-
|
|
CRM1
|
Cancer
|
|
CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
|
-
- HY-134581
-
|
M5049
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
|
-
- HY-139920A
-
|
SH-1028 mesylate
|
EGFR
|
Cancer
|
|
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
|
-
- HY-A0036R
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-A0031R
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-103151A
-
|
|
5-HT Receptor
|
Others
|
|
CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. CP94253 binds to the 5-HT1B, 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors, with Kis of 2, 89, 49, 860 and 1600 nM. CP94253 causes satiety, anorexia, weight loss and hyperlocomotion in rats model .
|
-
- HY-B0442R
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442AS
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Isotope-Labeled Compounds
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-151928
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
|
-
- HY-150109
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia .
|
-
- HY-158102A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ORIC-944 TFA is the TFA salt form of ORIC (HY-158102). ORIC-944 TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .
|
-
- HY-103308
-
|
|
Potassium Channel
|
Neurological Disease
|
|
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease .
|
-
- HY-143877
-
|
|
HDAC
|
Cancer
|
|
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
|
-
- HY-145408
-
|
|
CDK
|
Cancer
|
|
CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer .
|
-
- HY-118827
-
|
Quadrisol; CERM 10202; PM 150
|
COX
|
Inflammation/Immunology
|
|
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
|
-
- HY-B0442BR
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-16079
-
AZD3514
3 Publications Verification
|
Androgen Receptor
|
Cancer
|
|
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
|
-
- HY-D1456
-
|
|
Pyruvate Kinase
|
Cancer
|
|
TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe. TEPC466 shows a high degree of selectivity and sensitivity for the detection of PKM2 protein via the AIE effect. EPC466 can be used for the detection of PKM2. TEPC466 is successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. TEPC466 is a useful tool for cancer diagnosis and research .
|
-
- HY-144338
-
|
|
Epigenetic Reader Domain
PARP
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .
|
-
- HY-100277
-
|
SR-202
|
PPAR
|
Metabolic Disease
|
|
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-105685
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders .
|
-
- HY-W013712
-
|
|
Potassium Channel
|
Neurological Disease
|
|
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
|
-
- HY-148258
-
-
- HY-144433
-
|
|
DNA Methyltransferase
|
Infection
|
|
DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A, with KI values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis) .
|
-
- HY-144293
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma .
|
-
- HY-148794
-
|
IkT-148009
|
c-Met/HGFR
Bcr-Abl
|
Neurological Disease
Cancer
|
|
Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively. Risvodetinib suppresses c-Abl activation and substantially protects dopaminergic neurons from degeneration in mouse models of both inherited and sporadic Parkinson’s disease (PD), which is promising for research in the field of PD .
|
-
- HY-107669
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-115993
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM) .
|
-
- HY-14939A
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a Ki of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED50 is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED50 is 0.51-1.4 mg/kg) in rats .
|
-
- HY-145814
-
|
|
HSP
Fungal
|
Infection
|
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
|
-
- HY-100277R
-
|
|
PPAR
|
Metabolic Disease
|
|
Mifobate (Standard) is the analytical standard of Mifobate. This product is intended for research and analytical applications. Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-46531
-
|
|
Ligands for E3 Ligase
|
Inflammation/Immunology
Cancer
|
|
Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1) .
|
-
- HY-115906
-
|
|
FLT3
MNK
Apoptosis
|
Cancer
|
|
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .
|
-
- HY-125864
-
|
|
Interleukin Related
NF-κB
|
Inflammation/Immunology
|
|
Fibrinogen (Bovine) is a selective proteolytic molecule that can be activated by thrombin to assemble fibrin clots. Fibrinogen can regulate the activation of NF-KB in endothelial cells and upregulate the expression of inflammatory chemokines MCP-1 and MCP-1. Fibrinogen plays a key role in blood clotting, thrombosis, atherosclerosis and the pathological development of venous grafts, and can be used in the study of blood clotting and vascular diseases .
|
-
- HY-115987
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
|
-
- HY-124284
-
-
- HY-118827R
-
|
|
COX
|
Inflammation/Immunology
|
|
Vedaprofen (Standard) is the analytical standard of Vedaprofen. This product is intended for research and analytical applications. Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
|
-
- HY-17623
-
|
CJ-12420; RQ-00000004
|
Proton Pump
Potassium Channel
Na+/K+ ATPase
|
Inflammation/Immunology
|
Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H +/K +-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H +/K +-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-149844
-
|
|
Fungal
|
Infection
|
|
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections .
|
-
- HY-161398
-
|
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
|
TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research .
|
-
- HY-146980
-
|
|
Apoptosis
GLUT
|
Cancer
|
|
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity .
|
-
- HY-158400
-
-
- HY-170503
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-20 (Compound A49) is an inhibitor for methionine adenosyltransferase 2A (MAT2A) with an IC50 ≤50 nM. MAT2A-IN-20 inhibits human UGT1A1 with an IC50 of 28.45 μM. MAT2A-IN-20 exhibits antitumor in mouse models .
|
-
- HY-158343
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-CH2 is a conjugate of E3 ligase ligand and linker. Thalidomide-NH-PEG2-C2-CH2 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .
|
-
- HY-147985
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
|
-
- HY-161611
-
|
|
YAP
|
Others
|
|
Plant 14-3-3-IN-1 (Compound 2) is an inhibitor for 14-3-3 proteins in Arabidopsis thaliana, with an IC50 of 1.21 μM. Plant 14-3-3-IN-1 exhibits different inhibitory activities against different 14-3-3 isomers. Plant 14-3-3-IN-1 promotes the closure of stomata on leaves .
|
-
- HY-170498
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABA-A Receptor Ligand-1 (Compound 4) is a ligand for GABA-A receptor with a pKi of 7.27. GABA-A Receptor Ligand-1 reduces mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration. GABA-A Receptor Ligand-1 exhibits neuroprotective efficacy in rats ischemic stroke models .
|
-
- HY-111018
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
FPL 62129 is an antagonist for calcium channel. FPL 62129 reduces blood pressure and total peripheral resistance, increases the cardiac contractility and cardiac output in anarsthetised beagle model. FPL 62129 also serves as a vasodilator and a direct decelerator .
|
-
- HY-115997
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151129
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-145341
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
|
-
- HY-150582
-
|
|
c-Met/HGFR
c-Kit
FLT3
Apoptosis
|
Cancer
|
|
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
|
-
- HY-162785
-
|
|
CDK
|
Infection
|
|
XC219 (compound 43) is a cyclin-dependent kinase CDK) inhibitor, that covalently binds to CDK active site Lys. XC219 can be used in antifungal research .
|
-
- HY-153800
-
-
- HY-164151
-
|
|
ERK
|
Cancer
|
|
ERK-IN-8 (compound I-1) is an aniline pyrimidine derivative that acts as an ERK inhibitor. ERK-IN-8 has a strong inhibitory effect on ERK2 in vitro (IC50≤50 nM). ERK-IN-8 can be used in cancer research .
|
-
- HY-P3277
-
|
|
Ras
|
Cancer
|
|
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
|
-
- HY-P3277A
-
|
|
Ras
|
Cancer
|
|
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
|
-
- HY-162754
-
|
|
Proteasome
|
Inflammation/Immunology
|
|
LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits LMP7 and LMP2 with IC50 of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases .
|
-
- HY-120944
-
|
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively .
|
-
- HY-16765A
-
|
TD-1211 sulfate
|
Opioid Receptor
|
Neurological Disease
|
|
Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
|
-
- HY-P9927
-
|
AIN457
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis .
|
-
- HY-146883
-
|
|
Filovirus
|
Infection
|
|
As-358 has inhibitory effects against Ebola virus and Marburg virus, with IC50s of 47.5 μM and 3.7 μM .
|
-
- HY-17638A
-
|
DSP-3235 (sebacate); KGA-3235 (sebacate); GSK-1614235 (sebacate)
|
SGLT
|
Neurological Disease
|
|
Mizagliflozin sebacate (DSP-3235 sebacate) is a sodium-glucose cotransporter inhibitor with activity in improving vascular cognitive impairment caused by small vessel disease. Mizagliflozin sebacate improves blood flow and reverses vascular cognitive impairment by inhibiting neuronal SGLT1 activity. Mizagliflozin sebacate also showed the ability to increase the survival rate of IL-1β-treated PC12HS cells. Mizagliflozin sebacate promotes improvements in spatial learning and memory caused by small vessel disease in mouse models .
|
-
- HY-16765
-
|
TD-1211
|
Opioid Receptor
|
Neurological Disease
|
|
Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
|
-
- HY-112304
-
-
- HY-W076042
-
|
Sodium tetrakis(4-fluorophenyl)borate dihydrate
|
Biochemical Assay Reagents
|
Others
|
|
Cesibor dihydrate is an additive salt used in ion-selective electrodes (ISEs) and micro ion-selective field effect transistors (μ-ISFETs) to enhance or modulate their selective responses to specific ions .
|
-
- HY-15555
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
|
-
- HY-157381
-
-
- HY-126831
-
SBFI-AM
2 Publications Verification
|
Fluorescent Dye
|
Others
|
|
SBFI-AM is a Na + selective fluorescent indicator. SBFI-AM shows selectivity for Na + over K + .
|
-
- HY-19945
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
|
-
- HY-14398
-
|
SC 58635
|
COX
|
Inflammation/Immunology
Cancer
|
|
Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
|
-
- HY-112198
-
|
|
ATM/ATR
|
Cancer
|
|
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer .
|
-
- HY-163271
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
XL-126 (Compound 33) is a potent BD1-selective BET inhibitor, with a Kd of 8.9 nM. XL-126 leads to both the preservation of platelets and potent anti-inflammatory efficacy by BD1 selectivity .
|
-
- HY-12750
-
-
- HY-U00022
-
-
- HY-103456
-
-
- HY-15224
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
|
-
- HY-B2010
-
|
|
Herbicide
|
Others
|
|
Fomesafen is a type of efficient and selective protoporphyrinogen IX oxidase (PPO) inhibitor. Fomesafen is a herbicide and has the advantages of low toxicity and high selectivity .
|
-
- HY-162767
-
|
|
HSP
|
Neurological Disease
|
|
KUNG65 is a selective inhibitor of Grp94, with a target Kd of 540 nM and at least 73 fold selectivity vs. the other Hsp90 isoforms .
|
-
- HY-130800
-
-
- HY-168734
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model .
|
-
- HY-13506G
-
|
D 237 (GMP); MS 344 (GMP)
|
HDAC
|
Cancer
|
|
M344 (GMP) (D 237) (GMP) is the GMP level of M344 (HY-13506). GMP level of small molecules can be used as auxiliary reagents in cell therapy. M344 is a kind of histone acetylation enzyme inhibitor .
|
-
- HY-155154A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT4-IN-3 (compound 56) is a potent inhibitor of class I protein arginine methyltransferase (PRMT), targeting PRMT4 (IC50: 37 nM) and PRMT4 (IC50: 253 nM) .
|
-
- HY-16758A
-
|
AR-12286 hydrochloride
|
ROCK
|
Others
|
|
Verosudil hydrochloride (AR-12286 hydrochloride) is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is an inhibitor for Rho-kinase (ROCK) with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. Verosudil hydrochloride lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork .
|
-
- HY-135317F
-
|
CA-4948 phosphate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib phosphate exhibits antitumor activity in mouse model .
|
-
- HY-157302
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-21 (compound 54) is a c-met inhibitor with an IC50 value of 0.45? nM, and shows anti-tumor efficacy in vivo .
|
-
- HY-135317E
-
|
CA-4948 maleate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model .
|
-
- HY-145284
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
|
-
- HY-168899
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
|
-
- HY-170895
-
|
|
HSP
Na+/K+ ATPase
|
Cancer
|
|
Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
|
-
- HY-132309
-
BRD0639
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
|
-
- HY-135317C
-
|
CA-4948 tosylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model .
|
-
- HY-155154
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT4-IN-2 (compound 55) is a pan-inhibitor of protein arginine methyltransferase (PRMT) with IC50s of 92 nM (PRMT4), 436 nM (PRMT6), 460 nM (PRMT1), 823 nM ( PRMT8), 1.386 μM (PRMT3) .
|
-
- HY-164036R
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Flurbiprofen (sodium) (Standard) is the analytical standard of Flurbiprofen (sodium). This product is intended for research and analytical applications. Flurbiprofen sodium (dl-Flurbiprofen sodium) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory and analgesic activities. Flurbiprofen sodium is used to reduce bone resorption in periodontal disease, and it works by inhibiting carbonic anhydrase. Flurbiprofen sodium is formulated as biodegradable microspheres for use as a compound delivery system, particularly within the periodontal pocket. The release rate of flurbiprofen sodium is related to the concentration of polymer and polyvinyl alcohol used in its preparation .
|
-
- HY-135317D
-
|
CA-4948 mesylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model .
|
-
- HY-139831
-
|
|
Galectin
|
Cancer
|
|
Galectin-8-IN-1 is a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a Kd of 48 μM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins.
|
-
- HY-15557
-
|
|
ATM/ATR
|
Cancer
|
|
AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
|
-
- HY-111556
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.
|
-
- HY-100837
-
|
|
iGluR
|
Neurological Disease
|
|
5-Iodowillardiine is a potent and selective kainate receptor agonist. 5-Iodowillardiine is selective for kainate receptors composed of hGluR5 subunits .
|
-
- HY-13562
-
|
AQ4N
|
NO Synthase
|
Cancer
|
|
Banoxantrone (AQ4N), as a prototype hypoxia selective cytotoxin, can be reduced to AQ4, a potent topoisomerase II inhibitor. Banoxantrone selectively kills hypoxic cells via an iNOS-dependent mechanism. Banoxantrone shows a potent cytotoxicity and hypoxia-selective effect enhanced by radiation .
|
-
- HY-14825
-
|
SVT-40776
|
mAChR
|
Neurological Disease
|
|
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
- HY-15245
-
|
|
PI3K
|
Cancer
|
|
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
|
-
- HY-12870A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 maleate is a potent and selective estrogen receptor (ERα) antagonist with IC50 of 0.28 nM. AZD9496 maleate is an orally bioavailable selective oestrogen receptor degrader (SERD).
|
-
- HY-115867
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC50 = 7.9).
|
-
- HY-12055
-
|
|
MEK
ERK
|
Cancer
|
|
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
|
-
- HY-108246
-
|
|
OGA
Bacterial
|
Metabolic Disease
|
|
GlcNAcstatin is a selective glucoimidazole-based bacterial O-GlcNAcase inhibitor with a Ki of 4.6 pM. GlcNAcstatin shows 100000-fold selectivity over HexA/B .
|
-
- HY-12761
-
-
- HY-169960
-
|
|
mTOR
|
Cancer
|
|
2DII is a potent and selective mTORC2 inhibitor. 2DII selectively binds mSin1 PH domain and decreases the expression of AKT1 phosphorylation .
|
-
- HY-12870
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).
|
-
- HY-18271
-
|
|
CaMK
Autophagy
|
Inflammation/Immunology
|
|
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.
|
-
- HY-13531
-
|
|
PI3K
|
Cancer
|
|
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
|
-
- HY-100263
-
-
- HY-136979
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
|
RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants .
|
-
- HY-111630
-
|
|
Topoisomerase
|
Cancer
|
|
PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs) .
|
-
- HY-121933
-
|
|
Aldose Reductase
|
Metabolic Disease
|
|
IDD388 is a selective aldose reductase (ALR2) inhibitor with an IC50 of 30 nM. IDD388 displays selectivity for ALR2 over ALR1 (IC50 of 14 μM) .
|
-
- HY-16578
-
|
|
PPAR
|
Cancer
|
|
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
|
-
- HY-10871A
-
|
CP 945598 Hydrochloride
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Otenabant Hydrochloride is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
|
-
- HY-120448
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
QTX125 is a potent and highly selective HDAC6 inhibitor. QTX125 exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects .
|
-
- HY-13227
-
|
|
TGF-β Receptor
|
Cancer
|
|
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
|
-
- HY-14339
-
|
SB-742457; GSK-742457; RVT-101
|
5-HT Receptor
|
Neurological Disease
|
|
Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.
|
-
- HY-13990
-
|
TNKS656
|
PARP
Apoptosis
|
Cancer
|
|
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
|
-
- HY-110018
-
-
- HY-10871
-
|
CP-945598
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
|
-
- HY-12472
-
-
- HY-77113
-
|
|
Raf
|
Cancer
|
|
B-Raf IN 11 (ZINC72115182) is a selective B-Raf V600E inhibitor (IC50=76 nM), shows selectivity for
B-Raf V600E over B-Raf WT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research
|
-
- HY-138064
-
|
|
Biochemical Assay Reagents
|
Others
|
|
4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes .
|
-
- HY-130493
-
|
HDAC6 inhibitor HPB
|
HDAC
|
Cancer
|
|
HPB (HDAC6 inhibitor HPB) is a selective HDAC6 inhibitor with an IC50 of 31 nM. HPB exhibits >30-flod selectivity for HDAC6 over HDAC1 .
|
-
- HY-157941
-
|
|
ATM/ATR
|
Cancer
|
|
ART0380 is a potent and selective ATR kinase inhibitor. ART0380 has selective antitumor activity that can be used for the research of Ataxia-Telangiectasia Mutated (ATM) aberrant cancers .
|
-
- HY-103028A
-
GSK963
1 Publications Verification
|
RIP kinase
|
Others
|
|
GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro .
|
-
- HY-P99302
-
|
Humanized Anti-CD28 Recombinant Antibody
|
CD28
|
Inflammation/Immunology
|
|
Lulizumab (Humanized Anti-CD28 Recombinant Antibody) is a selective CD28 blockade, Lulizumab prevents T cell activation by selectively targeting CD28 signaling .
|
-
- HY-107568
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [ 125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM) .
|
-
- HY-70044
-
|
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-15797
-
UNC2250
2 Publications Verification
|
TAM Receptor
|
Cancer
|
|
UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
|
-
- HY-U00220
-
-
- HY-100263B
-
-
- HY-136460
-
|
ETH 1001
|
Calcium Channel
|
Others
|
|
Calcium ionophore I (ETH 1001) is a selective Ca 2+ ionophore for biological membranes. Calcium ionophore I can be used in Ca2+-selective microelectrodes that can be used for quantitative intracellular measurements of resting Ca2+-activities and of slowly changing Ca2+-levels .
|
-
- HY-10406
-
|
SCIO-469
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-10406A
-
|
SCIO-469 hydrochloride
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-14383
-
-
- HY-P3473
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Evybactin is a DNA gyrase inhibitor. Evybactin is a selective inhibitor of Mycobacterium tuberculosis with a MIC value of 0.25 µg/mL. Evybactin is the first antimicrobial compound found to employ this unusual mechanism of selectivity .
|
-
- HY-10539
-
|
LY317615 dihydrochloride
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .
|
-
- HY-14825A
-
|
SVT-40776 D-tartrate
|
mAChR
|
Neurological Disease
|
|
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
- HY-120448A
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects .
|
-
- HY-107498
-
|
|
iGluR
|
Neurological Disease
|
|
GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons .
|
-
- HY-10342
-
|
LY317615
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .
|
-
- HY-13071
-
|
ST-1435; Elcometrine
|
Progesterone Receptor
|
Endocrinology
|
|
Nestoron (ST-1435) is a 19-norprogesterone derivative with high affinity and selectivity for progesterone receptors. Nestoron is a highly selective and potent progestogen that can be used as a hormonal contraceptive .
|
-
- HY-13266A
-
|
|
CDK
|
Cancer
|
|
BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
|
-
- HY-163146
-
|
|
Fluorescent Dye
|
Cancer
|
|
TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
|
-
- HY-D2186
-
|
|
Biochemical Assay Reagents
|
Others
|
|
BTD probe-1 is a benzothiazine-based chemoselective probe for selective labeling of protein S-sulfenic acids in vitro. BTD probe-1 selectively modify sulfenic acid residues in proteins .
|
-
- HY-158190
-
|
Rose Bengal Medium
|
Bacterial
|
Infection
|
|
Rose-Bengal Chloramphenicol Agar is a selective medium for the enumeration of yeasts and moulds from a wide variety of foodstuffs. The medium has a neutral pH and chloramphenicol is used as a selective agent to suppress the growth of bacteria .
|
-
- HY-112304A
-
-
- HY-112910
-
|
|
HSP
|
Inflammation/Immunology
Cancer
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α .
|
-
- HY-14398R
-
|
SC 58635 (Standard)
|
COX
|
Inflammation/Immunology
Cancer
|
|
Celecoxib (Standard) is the analytical standard of Celecoxib. This product is intended for research and analytical applications. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
|
-
- HY-112217A
-
|
|
nAChR
|
Neurological Disease
|
|
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively .
|
-
- HY-15270
-
|
|
JAK
|
Cancer
|
|
BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).
|
-
- HY-100716
-
|
IPI-549
|
PI3K
|
Cancer
|
|
Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases .
|
-
- HY-101835
-
-
- HY-108936
-
-
- HY-106910
-
-
- HY-13724
-
-
- HY-101574
-
-
- HY-145919
-
-
- HY-118918
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease .
|
-
- HY-142694
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation .
|
-
- HY-101030
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-12646A
-
|
|
Ras
Apoptosis
|
Cancer
|
|
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
|
-
- HY-12646
-
|
|
Ras
Apoptosis
|
Cancer
|
|
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
|
-
- HY-134957
-
VT107
5 Publications Verification
|
YAP
|
Cancer
|
|
VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer .
|
-
- HY-101030A
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice .
|
-
- HY-12341
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
|
-
- HY-15472A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
|
-
- HY-P2246
-
|
|
JNK
|
Cancer
|
|
JTP10-△-TATi TFA is a selective JNK2 peptide inhibitor, with an IC50 of 92 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3 .
|
-
- HY-103246
-
|
|
Androgen Receptor
|
Cancer
|
|
TFM-4AS-1 is a selective androgen receptor modulator (SARM), and a potent androgen receptor (AR) ligand with an IC50 of 38 nM. TFM-4AS-1 is a gene-selective agonist .
|
-
- HY-117393
-
|
|
PKC
|
Cancer
|
|
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .
|
-
- HY-164394
-
|
|
c-Met/HGFR
|
Cancer
|
|
EMD 1204831 is a potent and highly selective c-Met inhibitor which selectively suppresses the c-Met receptor tyrosine kinase activity with an IC50 of 9 nM. EMD 1204831 can be utilized in cancer research .
|
-
- HY-14398S1
-
|
SC 58635-d3
|
COX
|
Inflammation/Immunology
Cancer
|
|
Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM[1][2].
|
-
- HY-15472
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
|
-
- HY-14398S
-
|
SC 58635-d7
|
COX
|
Inflammation/Immunology
Cancer
|
|
Celecoxib-d7 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM[1][2].
|
-
- HY-112815
-
|
|
TGF-β Receptor
|
Cancer
|
|
ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3 .
|
-
- HY-10539B
-
|
LY317615 hydrochloride
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) hydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .
|
-
- HY-P3876
-
-
- HY-B1355
-
|
|
Bacterial
COX
|
Infection
Inflammation/Immunology
|
|
Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis .
|
-
- HY-108432
-
|
|
CCR
|
Inflammation/Immunology
|
|
BMS-741672 is a selective and orally active CCR2 antagonist with an IC50 of 1.1 nM. BMS-741672 shows >700-fold selective for CCR2 than CCR5 .
|
-
- HY-14398GL
-
|
SC 58635 (GMP Like)
|
COX
|
Inflammation/Immunology
|
|
Celecoxib (SC 58635) GMP Like is a GMP-class Celecoxib (HY-14398). Celecoxib, a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
|
-
- HY-B1355A
-
-
- HY-119935
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs .
|
-
- HY-12875
-
|
|
Ras
|
Cancer
|
|
BQU57 selectively inhibits Ral, with higher selectivity than Ras or Rho. The IC50 values of BQU57 on H2122 and H358 cells are 2.0 μM and 1.3 μM respectively.
|
-
- HY-119493
-
|
|
Fluorescent Dye
|
Others
|
|
MSBN is a highly selective fluorogenic probe for thiols. MSBN can be used to image thiols in live cells selectively and specifically label protein thiols with a signal to determine various reversible protein thiol modifications .
|
-
- HY-100012
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis .
|
-
- HY-116097
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
PSB-1491 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.386 nM for hMAO-B. PSB-1491 shows >25000-fold selective versus MAO-A .
|
-
- HY-137187
-
FB23
1 Publications Verification
|
Fat Mass and Obesity-associated Protein (FTO)
|
Cancer
|
|
FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N 6-methyladenosine (m6A) demethylase activity .
|
-
- HY-12970A
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer .
|
-
- HY-120530
-
|
|
mGluR
|
Neurological Disease
|
|
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) .
|
-
- HY-157134
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Y08262 is a potent and selective CBP bromodomain inhibitor. Y08262 selectively inhibits the CBP bromodomain with an IC50 value of 73.1 nM. Y08262 can be used for the research of acute myeloid leukemia (AML) .
|
-
- HY-163285
-
-
- HY-161171
-
|
|
Parasite
Ephrin Receptor
|
Cancer
|
|
Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7 .
|
-
- HY-12652
-
|
|
mTOR
|
Cancer
|
AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K .
|
-
- HY-153045
-
BAY-805
2 Publications Verification
|
Deubiquitinase
|
Cancer
|
|
BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .
|
-
- HY-135827A
-
|
MSC2360844 hemifumarate; IOA-244 hemifumarate
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
Roginolisib (MSC2360844) hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib hemifumarate shows highly selective against a panel of 278 additional kinases .
|
-
- HY-12970
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer .
|
-
- HY-141865
-
|
|
Adenosine Receptor
|
Cancer
|
|
Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aR than A2bR.
|
-
- HY-103164A
-
|
CSC
|
Endogenous Metabolite
|
Neurological Disease
|
|
8-(3-Chlorostyryl)caffeine (CSC) is an adenosine antagonist with selective activity at the A2a adenosine receptor. 8-(3-Chlorostyryl)caffeine showed 520-fold selectivity in radioligand binding experiments in rat brain. Antagonism of adenylylase by 8-(3-Chlorostyryl)caffeine shows 22-fold selectivity in rat chromaffin cells When 8-(3-Chlorostyryl)caffeine is co-administered with the A1-selective antagonist CPX, It can also further increase exercise activity. 8-(3-Chlorostyryl)caffeine exhibits good MAO-B inhibitory activity in primate mitochondria. 8-(3-Chlorostyryl)caffeine also has excellent A2A receptor affinity .
|
-
- HY-B1581A
-
|
|
NO Synthase
|
Cancer
|
|
L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.
|
-
- HY-100903
-
|
nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
|
-
- HY-19756
-
|
Calixarene 0118; PTX008
|
Galectin
|
Cancer
|
|
OTX008 is a selective inhibitor of galectin-1.
|
-
- HY-132927
-
-
- HY-118734
-
-
- HY-19673
-
-
- HY-B1847
-
-
- HY-101801
-
|
|
FAP
|
Cancer
|
|
Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.
|
-
- HY-118262
-
-
- HY-13209
-
-
- HY-100245
-
-
- HY-151898
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases .
|
-
- HY-134904
-
|
RM-006
|
mTOR
|
Cancer
|
|
RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors .
|
-
- HY-152153
-
|
|
HSP
|
Cancer
|
|
GRP78-IN-3 (Compound 8) is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM) .
|
-
- HY-121088
-
|
|
P-glycoprotein
|
Cardiovascular Disease
Others
|
|
Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
|
-
- HY-11003
-
|
GW843682
|
Polo-like Kinase (PLK)
|
Cancer
|
|
GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.
|
-
- HY-145310
-
-
- HY-14248
-
|
CGS 20267
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- HY-P2247
-
|
|
JNK
|
Cancer
|
|
JTP10-△-R9 TFA is a selective JNK2 peptide inhibitor, with an IC50 of 89 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3 .
|
-
- HY-135827
-
|
MSC2360844; IOA-244
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases .
|
-
- HY-12470
-
|
|
Casein Kinase
|
Others
|
|
PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
|
-
- HY-B2010R
-
|
|
Herbicide
|
Others
|
|
Fomesafen (Standard) is the analytical standard of Fomesafen. This product is intended for research and analytical applications. Fomesafen is a type of efficient and selective protoporphyrinogen IX oxidase (PPO) inhibitor. Fomesafen is a herbicide and has the advantages of low toxicity and high selectivity .
|
-
- HY-144440
-
|
|
JAK
|
Cancer
|
|
JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC50 of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more .
|
-
- HY-157478
-
|
|
Casein Kinase
|
Infection
|
|
CSNK2A-IN-1 (compound 7C) is a selective CSNK2A inhibitor. CSNK2A-IN-1 has antiviral activity and improved selectivity over PIM3 .
|
-
- HY-12837
-
|
|
Others
|
Others
|
|
EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC50 of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation .
|
-
- HY-161079
-
|
|
Parasite
|
Infection
|
|
TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent Plasmodium falciparum (Pf20S) inhibitor. TDI-8304 shows highly selective for Pf20S over human proteasomes .
|
-
- HY-128594
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer’s disease .
|
-
- HY-102063
-
|
Pyridoxol, cyclic 3,4-hydrogen phosphate
|
P2X Receptor
|
Neurological Disease
|
|
MRS 2219 (Pyridoxol) is a selective pharmacological probe of P2X1 receptor. MRS 2219 selectively potentiated ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM .
|
-
- HY-128044
-
|
B581
|
Farnesyl Transferase
|
Cancer
|
|
Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras) .
|
-
- HY-162555
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
BMS-986308 is a selective and orally active renal outer medullary potassium (ROMK) channel inhibitor. BMS-986308 is selective for ROMK over hERG. BMS-986308 can be used for heart failure research .
|
-
- HY-139609
-
|
RP-3500; ATR inhibitor 4
|
ATM/ATR
mTOR
|
Cancer
|
|
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
|
-
- HY-101764
-
|
SR 27897
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .
|
-
- HY-162082
-
|
|
DNA Methyltransferase
|
Cancer
|
|
METTL1-WDR4-IN-2 (compound 6) is a selective methyltransferase Like 1 (METTL1)-WDR4 inhibitor with an IC50 of 41 μM. METTL1-WDR4-IN-2 shows remarkable selectivity against METTL3-14 and slightly selective also against METTL16 .
|
-
- HY-14873
-
|
BG 9928
|
Adenosine Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure .
|
-
- HY-132993
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Hcyb1 is a highly selective, orally active PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling .
|
-
- HY-116507
-
|
|
nAChR
|
Neurological Disease
|
|
AZD0328 is a selective α7 nAChR partial agonist. AZD0328 selectively enhances midbrain dopaminergic neuronal activity and enhances cortical dopamine levels in rats. AZD0328 improves cognitive performance .
|
-
- HY-145817A
-
|
RP-6306
|
Wee1
|
Cancer
|
|
lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects .
|
-
- HY-B0034
-
|
E2020
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-101320
-
|
ICI-D 7114
|
Adrenergic Receptor
|
Endocrinology
|
|
ZD-7114 is a potent and selective agonist of β3-adrenergic. ZD-7114 is a selective thermogenic agent in vivo. ZD-7114 can be used in study obesity and diabetes .
|
-
- HY-103210
-
|
Neurotoxin DSP 4 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
DSP-4 hydrochloride is a highly and selective adrenergic neurotoxin. DSP-4 hydrochloride can cross the blood brain barrier. DSP-4 hydrochloride can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons .
|
-
- HY-16508
-
|
CDB-2914
|
Progesterone Receptor
Autophagy
|
Endocrinology
Cancer
|
|
Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma .
|
-
- HY-116213
-
-
- HY-12080
-
|
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-100538
-
DTP3
1 Publications Verification
|
DNA/RNA Synthesis
JAK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway .
|
-
- HY-101320A
-
|
ICI-D 7114 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
ZD-7114 hydrochloride is a potent and selective agonist of β3-adrenergic. ZD-7114 hydrochloride is a selective thermogenic agent in vivo. ZD-7114 hydrochloride can be used in study obesity and diabetes .
|
-
- HY-50098
-
|
PF-2545920
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier .
|
-
- HY-135608
-
|
|
Sigma Receptor
|
Others
|
|
BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.
|
-
- HY-10290
-
|
|
Cathepsin
|
Metabolic Disease
|
|
MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S .
|
-
- HY-50098A
-
|
PF-2545920 hydrochloride
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier .
|
-
- HY-16684
-
|
IRX-5183; VTP-195183; NRX-195183
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (Kd=3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.
|
-
- HY-163883
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-34 is a potent and selective butyrylcholinesterase (BChE) inhibitor with an IIC50 of 25 nM. BChE-IN-34 shows excellent selectivity against BChE over acetylcholinesterase. BChE-IN-34 has neuroprotective and antioxidant effects .
|
-
- HY-153556
-
|
|
CDK
VEGFR
Src
|
Others
|
|
GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively .
|
-
- HY-13428
-
|
|
Beta-lactamase
HDAC
Virus Protease
|
Cancer
|
|
Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
|
-
- HY-19329
-
-
- HY-151412
-
-
- HY-B0102A
-
-
- HY-U00234
-
-
- HY-U00129
-
-
- HY-U00239
-
-
- HY-14917
-
-
- HY-110110
-
-
- HY-19998
-
-
- HY-B0375
-
-
- HY-108054A
-
-
- HY-103576
-
-
- HY-18973
-
-
- HY-112620
-
-
- HY-17354
-
-
- HY-112562
-
-
- HY-14864A
-
-
- HY-107602
-
-
- HY-132927A
-
-
- HY-17618
-
-
- HY-112859
-
-
- HY-14864
-
-
- HY-156993
-
-
- HY-19488A
-
|
|
Bacterial
|
Infection
|
|
Ribocil-C is a highly selective inhibitor of bacterial riboflavin riboswitches.
|
-
- HY-100969
-
-
- HY-19362
-
-
- HY-16316
-
-
- HY-101858
-
-
- HY-137145
-
|
|
SGLT
|
Others
|
|
Galacto-dapagliflozin is a selective inhibitor for hSGLT2 with Ki of 25 nM .
|
-
- HY-101745
-
-
- HY-14260
-
-
- HY-168505
-
|
|
YAP
|
Cancer
|
|
MSC-5046 is a selective TEAD1 inhibitor .
|
-
- HY-P4306
-
-
- HY-P1013
-
-
- HY-B0375A
-
|
MD-805 monohydrate; MCI-9038 monohydrate; Argipidine monohydrate
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Argatroban (monohydrate) (MD-805 (monohydrate)) is a direct, selective thrombin inhibitor.
|
-
- HY-P5999
-
-
- HY-15444
-
-
- HY-100220
-
-
- HY-12080A
-
|
ZK-811752 hydrochloride
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-148778
-
|
|
FGFR
|
Cancer
|
|
FGFR3-IN-4 is a selective FGFR3 inhibitor, with an IC50 value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1 .
|
-
- HY-12861
-
|
|
p97
|
Cancer
|
|
CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM .
|
-
- HY-100565
-
SGC2085
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
|
-
- HY-107550
-
|
|
HDAC
|
Cancer
|
|
TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .
|
-
- HY-10896
-
-
- HY-10721
-
|
AKT protein kinase inhibitor
|
Akt
|
Cancer
|
|
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
|
-
- HY-163182
-
|
|
Casein Kinase
|
Infection
|
|
CSNK2A-IN-2 (compound 6c) is a selective CSNK2A inhibitor with antiviral activity. CSNK2A-IN-2 exhibits an inhibitory effect on viral replication and is selective for PIM3 .
|
-
- HY-120004
-
|
|
mAChR
|
Infection
|
|
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
|
-
- HY-P2261
-
|
|
PKA
|
Infection
|
|
STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
|
-
- HY-158078
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 21 (Compound 5h) is a selective carbonic anhydrase (hCA IX) inhibitor, with a Ki of 15.1 nM, and is highly selective against other investigated isoform. Carbonic anhydrase inhibitor 21 can be used for anticancer research .
|
-
- HY-100565A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
|
-
- HY-137478
-
KB-0742
1 Publications Verification
|
CDK
|
Cancer
|
|
KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity .
|
-
- HY-137478A
-
|
|
CDK
|
Cancer
|
|
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity .
|
-
- HY-15249
-
JZL 184
5 Publications Verification
|
MAGL
|
Neurological Disease
|
|
JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH .
|
-
- HY-123846
-
|
|
Phosphatase
|
Cardiovascular Disease
|
|
MLS-0437605 is a selective dual-specificity phosphatase 3 (DUSP3) inhibitor with an IC50 of 3.7 μM. MLS-0437605 is more selective for DUSP3 than DUSP22 and other protein tyrosine phosphatases (PTPs) .
|
-
- HY-B1320
-
-
- HY-117554
-
|
|
HDAC
|
Cancer
|
|
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs .
|
-
- HY-100518
-
T-26c
2 Publications Verification
|
MMP
|
Inflammation/Immunology
|
|
T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes .
|
-
- HY-123971
-
|
|
HDAC
PROTACs
|
Cancer
|
|
HDAC6 degrader-4 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research .
|
-
- HY-134138
-
|
|
COX
|
Inflammation/Immunology
|
|
Indomethacin N-octyl amide (Compound 2) is a potent and selective COX-2 inhibitor with an IC50 of 40 nM. Indomethacin N-octyl amide shows >1000-fold selectivity against COX-1 (IC50 of 66 µM) .
|
-
- HY-124060
-
|
|
PDK-1
|
Cancer
|
|
PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 .
|
-
- HY-14442
-
-
- HY-152155
-
|
|
PI5P4K
|
Inflammation/Immunology
Cancer
|
|
ARUK2001607 is a selective phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with a Kd of 7.1 nM. ARUK2001607 shows high selectivity over other >150 kinases .
|
-
- HY-U00216
-
-
- HY-137980
-
-
- HY-13201
-
-
- HY-100532
-
-
- HY-14164
-
-
- HY-107756
-
-
- HY-14778
-
-
- HY-13254A
-
|
|
Akt
|
Cancer
|
|
A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM.
|
-
- HY-P1286
-
-
- HY-114530
-
-
- HY-14233
-
-
- HY-12683
-
|
|
Glutaminase
|
Cancer
|
|
BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
|
-
- HY-P1561
-
-
- HY-15085
-
-
- HY-156992
-
-
- HY-50948
-
-
- HY-19626
-
-
- HY-13495
-
ML281
3 Publications Verification
|
STK33
|
Cancer
|
|
ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM.
|
-
- HY-17354A
-
|
Arbaclofen hydrochloride; STX 209 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
(R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist .
|
-
- HY-33353
-
-
- HY-112045
-
|
PRI-724
|
Wnt
|
Cancer
|
|
PRI-724 is a selective inhibitor of the CBP/β-catenin interaction.
|
-
- HY-118503
-
-
- HY-10069
-
|
|
ROCK
|
Cancer
|
|
Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
|
-
- HY-16763
-
-
- HY-13842
-
BX517
2 Publications Verification
|
PDK-1
|
Cancer
|
|
BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
|
-
- HY-50686
-
|
ARQ 197; (3R,4R)-ARQ 198
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Tivantinib is a highly selective c-Met tyrosine kinase inhibitor with a Ki of 355 nM.
|
-
- HY-59047
-
|
MLR-1023
|
Src
|
Metabolic Disease
|
|
Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
|
-
- HY-13201A
-
-
- HY-116859
-
-
- HY-134434
-
|
|
Cathepsin
|
Others
|
|
Z-Arg-Arg-AMC hydrochloride is a selective substrate of cathepsin B .
|
-
- HY-U00240
-
-
- HY-10892
-
|
|
HIV
|
Infection
|
|
HEPT is a potent and selective anti-HIV-1 agent .
|
-
- HY-15603
-
-
- HY-11000
-
|
|
ROCK
|
Cancer
|
|
GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
|
-
- HY-P4369
-
-
- HY-139825
-
-
- HY-10934
-
|
LY451395
|
iGluR
|
Neurological Disease
|
|
Mibampator (LY451395) is a potent and highly selective potentiator of the AMPA receptors.
|
-
- HY-U00038
-
|
ENS 213-163; Sandoz ENS 163 phosphate; Thiopilocarpine phosphate
|
mAChR
|
Neurological Disease
|
|
ENS-163 phosphate is a selective muscarinic M1 receptor agonist.
|
-
- HY-10287
-
-
- HY-101807
-
-
- HY-101602
-
-
- HY-103704
-
-
- HY-132862
-
|
|
PROTACs
|
Cancer
|
|
ZXH-4-137 is a potent and selective CRBN degrader (PROTAC).
|
-
- HY-117777
-
-
- HY-19973
-
-
- HY-145444
-
-
- HY-W013375
-
-
- HY-116238
-
|
|
ROCK
|
Others
|
|
ROCK-IN-D2 is a potent and selective ROCK inhibitor .
|
-
- HY-112909
-
-
- HY-18101A
-
-
- HY-19693
-
-
- HY-116080
-
-
- HY-136200
-
|
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 2 is a potent and selective trypanosoma brucei inhibitor .
|
-
- HY-13240A
-
|
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
|
-
- HY-110186
-
|
|
Adenosine Receptor
|
Metabolic Disease
|
|
PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction .
|
-
- HY-10792
-
|
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-111509
-
|
|
ROR
|
Inflammation/Immunology
|
|
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ) .
|
-
- HY-13240
-
|
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
|
-
- HY-15144B
-
|
(S)-TSA
|
HDAC
|
Cancer
|
|
(S)-Trichostatin A ((S)-TSA) is a HDAC6-selective inhibitor with IC50s of 9.88 nM and 11.1 nM for Zebrafish HDAC6 and Human HDAC6, respectively. (S)-Trichostatin A weakly inhibits other human HDACs .
|
-
- HY-111455
-
LP-211
1 Publications Verification
|
5-HT Receptor
|
Neurological Disease
|
|
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
|
-
- HY-107559
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .
|
-
- HY-137056
-
|
|
Opioid Receptor
|
Others
|
|
LY164929 is a highly selective ligand for the lower affinity [3H]D-Ala2-D-Leu-5-enkephalin binding site, exhibiting 1,986-fold selectivity compared to other ligands.
|
-
- HY-122134
-
|
|
Fungal
|
Infection
|
|
SC-58272 is a potent and selective dipeptide N-myristoyltransferase (Nmt) inhibitor with an IC50 of 56 nM for C. albicans (strain B311) Nmt. SC-58272 shows 250-fold selective for the fungal enzyme compared to human enzyme .
|
-
- HY-P1278A
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-106278
-
|
|
PPAR
|
Metabolic Disease
|
|
GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia .
|
-
- HY-15370
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors .
|
-
- HY-101457
-
|
|
MAGL
|
Metabolic Disease
|
|
JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL) .
|
-
- HY-B1950
-
|
(R)-Quizalofop ethyl; Quinofop-ethyl
|
Herbicide
|
Others
|
|
Quizalofop-P-ethyl is a low-toxicity herbicide, a highly selective new type of post-emergence herbicide for dryland crops, with high selectivity between gramineous weeds and dicotyledonous crops, and it has good control efficacy against gramineous weeds in broadleaf crop fields.
|
-
- HY-15370A
-
|
SB-269970A
|
5-HT Receptor
|
Neurological Disease
|
|
SB-269970 hydrochloride is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors .
|
-
- HY-P1278
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively .
|
-
- HY-131247
-
|
|
Bcl-2 Family
|
Inflammation/Immunology
Cancer
|
|
Bcl-2-IN-2 is a potent and selective Bcl-2 inhibitor with an IC50 of 0.034 nM and also inhibits Bcl-xL with an IC50 of 43 nM, showing >1000-fold selectivity for Bcl-2 over Bcl-xL .
|
-
- HY-P1123
-
|
|
ATP Citrate Lyase
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120 .
|
-
- HY-160096
-
|
|
ATM/ATR
|
Cancer
|
|
M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC50 of 0.25 nM. M3541 shows remarkable selectivity against other protein kinases. M3541 suppresses double-strand breaks (DSB) repair and has antitumor activities .
|
-
- HY-W028690
-
DNMDP
3 Publications Verification
|
Phosphodiesterase (PDE)
|
Cancer
|
|
DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity .
|
-
- HY-101310
-
|
|
iGluR
|
Neurological Disease
|
|
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively .
|
-
- HY-119572
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
Sodium zirconium cyclosilicate is an orally administered, non-absorbed, novel, inorganic microporous zirconium silicate compound, is a highly selective cation exchanger that selectively removes excess K + in vivo. Sodium zirconium cyclosilicate can be used in research of chronic kidney disease (CKD) .
|
-
- HY-110046
-
|
|
MMP
|
Others
|
|
CL-82198 hydrochloride is a selective inhibitor of MMP-13. CL-82198 hydrochloride binds to the entire S1’ pocket of MMP-13, which is the basis of its selectivity against MMP-1, MMP-9, and TACE .
|
-
- HY-101355A
-
-
- HY-110129
-
|
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-131339
-
SP-96
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
SP-96 is a?highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
|
-
- HY-116254
-
|
|
Farnesyl Transferase
|
Others
|
|
L-739750 is a selective protein farnesyltransferase (PFTase) inhibitor (IC50: 0.4 nM). PFTase utilizes farnesyl diphosphate to farnesylate the cysteine residue of protein substrates having a C-terminal CAAX motif. L-739750 is a selective CAAX peptidomimetic .
|
-
- HY-125286
-
|
|
CD73
|
Cancer
|
|
AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
|
-
- HY-12768
-
|
BLZ945
|
c-Fms
|
Cancer
|
|
Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs .
|
-
- HY-139807
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16) .
|
-
- HY-B1416A
-
-
- HY-12365
-
|
CF-102; 2-Cl-IB-MECA
|
Adenosine Receptor
|
Cancer
|
|
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .
|
-
- HY-109121
-
|
CK-2127107
|
Calcium Channel
|
Cardiovascular Disease
|
|
Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model .
|
-
- HY-19414
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).
|
-
- HY-162257
-
|
|
Btk
|
Cancer
|
|
BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .
|
-
- HY-131342
-
|
|
Btk
|
Inflammation/Immunology
|
|
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research .
|
-
- HY-P3854
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
|
-
- HY-149836A
-
|
|
Fluorescent Dye
|
Others
|
|
3-MeOARh-NTR chloride is an activatable imaging probe with high selectivity, and good stability. 3-MeOARh-NTR chloride possesses high selectivity and high signal-to-noise ratio for nitroreductase (NTR) detection, and serves as an efficient molecular tool for endogenous NTR detection .
|
-
- HY-12768A
-
|
BLZ945 hydrochloride
|
c-Fms
|
Cancer
|
|
Sotuletinib (BLZ945) hydrochloride is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs .
|
-
- HY-19353
-
SR7826
1 Publications Verification
|
LIM Kinase (LIMK)
|
Neurological Disease
Cancer
|
|
SR7826 is a class of bis-aryl urea derived potent, selective and orally active LIM kinase (LIMK) inhibitor with an IC50 of 43 nM for LIMK1. SR7826 is >100-fold more selective for LIMK1 than ROCK and JNK kinases .
|
-
- HY-149836
-
|
|
Fluorescent Dye
|
Others
|
|
3-MeOARh-NTR is an activatable imaging probe with high selectivity, and good stability. 3-MeOARh-NTR possesses high selectivity and high signal-to-noise ratio for nitroreductase (NTR) detection, and serves as an efficient molecular tool for endogenous NTR detection .
|
-
- HY-B1978S
-
|
|
Fungal
Reactive Oxygen Species
|
Infection
|
|
Iprodione-d5 is the deuterium labeled Iprodione[1]. Iprodione, a dicarboximide fungicide, has a highly specific action, with a capacity to cause oxidative damage through production of free oxygen radicals (ROS). Iprodione does not appear to be species selective[2].
|
-
- HY-122592
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research .
|
-
- HY-113973
-
|
|
LPL Receptor
|
Cancer
|
|
LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM) .
|
-
- HY-10010
-
|
|
BCRP
|
Cancer
|
|
Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters .
|
-
- HY-76612
-
-
- HY-135714
-
|
EKZ-001
|
HDAC
Microtubule/Tubulin
|
Neurological Disease
Cancer
|
|
Bavarostat (EKZ-001) is a BBB-penetrable and selective HDAC6 inhibitor (IC50: 0.06 μM). Bavarostat modulates tubulin acetylation selectively over histone acetylation. Bavarostat can be used for research of cancers and central nervous system (CNS) disorders .
|
-
- HY-15532
-
|
MK-8776
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively .
|
-
- HY-108229
-
|
6β-Hydroxynaltrexone
|
Drug Metabolite
Opioid Receptor
|
Neurological Disease
|
|
6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
|
-
- HY-111589
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research .
|
-
- HY-W021879
-
|
5-Iodoisoquinoline
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. DSRM-3716 is selective against other NAD +-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection .
|
-
- HY-P99816
-
|
|
PCSK9
|
Metabolic Disease
|
|
Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke .
|
-
- HY-13500
-
-
- HY-157294
-
-
- HY-15604
-
-
- HY-42849
-
-
- HY-10284
-
-
- HY-22437
-
|
(±)-UK-88525
|
mAChR
|
Neurological Disease
Cancer
|
|
(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist .
|
-
- HY-14720
-
-
- HY-107986
-
-
- HY-W100249
-
-
- HY-119776
-
-
- HY-B1199A
-
-
- HY-125366
-
|
|
FAP
|
Cancer
|
|
ARI-3099 is potent and selective inhibitor of FAP with a Ki value of 9 nM .
|
-
- HY-15487
-
-
- HY-19661
-
-
- HY-107399
-
-
- HY-P1336
-
-
- HY-70061
-
-
- HY-145782
-
-
- HY-15227
-
-
- HY-107657
-
|
|
Myosin
|
Others
|
|
(+)-Blebbistatin is the inactive enantiomer of (–)-Blebbistatin. (–)-Blebbistatin is a selective inhibitor of myosin II ATPase .
|
-
- HY-15607A
-
|
|
Bcl-2 Family
|
Cancer
|
|
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
|
-
- HY-101846
-
-
- HY-112264
-
-
- HY-115717
-
|
|
METTL3
|
Cancer
|
|
UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM.
|
-
- HY-125339
-
-
- HY-153122A
-
-
- HY-106875
-
-
- HY-160997
-
-
- HY-101274
-
-
- HY-125145
-
-
- HY-19737A
-
|
|
PPAR
|
Cancer
|
|
DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.
|
-
- HY-13300
-
SR-3677
1 Publications Verification
|
ROCK
Autophagy
|
Cancer
|
|
SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
|
-
- HY-100273
-
|
|
RAR/RXR
Autophagy
|
Cancer
|
|
AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
|
-
- HY-144991
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
|
-
- HY-112909A
-
-
- HY-119136
-
|
|
Others
|
Others
|
|
BFF-122 is a compound that selectively inhibits mammalian kynurenine aminotransferase II.
|
-
- HY-101502A
-
-
- HY-169822
-
-
- HY-E70204
-
|
AluI
|
DNA Methyltransferase
|
Cancer
|
|
AluI Methyltransferase (AluI) is a methyltransferase used as the interference enzymes to investigate the selectivity .
|
-
- HY-16656
-
-
- HY-U00432
-
-
- HY-B1860
-
|
|
Herbicide
|
Others
|
|
Imazapic is a selective herbicide used to control perennial grasses and some broadleaf weeds.
|
-
- HY-121427
-
-
- HY-12280
-
THZ2
3 Publications Verification
|
CDK
|
Cancer
|
|
THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM.
|
-
- HY-112285
-
-
- HY-111068
-
-
- HY-17622
-
-
- HY-12663
-
-
- HY-103650
-
-
- HY-18778
-
|
TA-8995; DEZ-001
|
CETP
|
Metabolic Disease
|
|
TA-8995 is a new and selective cholesteryl ester transfer protein (CETP) inhibitor.
|
-
- HY-13439
-
-
- HY-21098A
-
-
- HY-12114
-
-
- HY-50663
-
MK 0893
5 Publications Verification
|
GCGR
|
Metabolic Disease
|
|
MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.
|
-
- HY-42849A
-
-
- HY-123484
-
|
|
ROCK
|
Others
|
|
ROCK-IN-D1 serves as a highly effective and selective inhibitor of ROCK.
|
-
- HY-15832
-
|
|
Phosphatase
|
Cancer
|
|
GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.
|
-
- HY-12701
-
-
- HY-N12651
-
|
|
Others
|
Others
|
|
Bipolaroxin is a selective phytotoxin. Bipolaroxin can be isolated from Bipolaris cynodontis .
|
-
- HY-15737
-
DB07268
5 Publications Verification
|
JNK
|
Cancer
|
|
DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM.
|
-
- HY-P1018
-
-
- HY-12236A
-
-
- HY-12802
-
-
- HY-A0066
-
-
- HY-12829
-
-
- HY-15227A
-
-
- HY-P1286A
-
-
- HY-P1782
-
-
- HY-15604A
-
-
- HY-13646
-
-
- HY-N2260
-
|
(-)-Cephaeline dihydrochloride; NSC 32944
|
Cytochrome P450
|
Infection
|
|
Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
|
-
- HY-U00018
-
-
- HY-14163
-
-
- HY-15607
-
-
- HY-B1110A
-
-
- HY-N2143
-
-
- HY-15150
-
|
R428; BGB324
|
TAM Receptor
|
Cancer
|
|
Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM .
|
-
- HY-12734
-
-
- HY-106956
-
-
- HY-12285
-
|
MLN1117; INK1117; TAK-117
|
PI3K
|
Cancer
|
|
Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
|
-
- HY-101973
-
-
- HY-B0374A
-
-
- HY-P1013A
-
-
- HY-14992
-
-
- HY-112442
-
|
|
JAK
|
Cancer
|
|
AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
|
-
- HY-144793
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Deac-SS-Biotin is a potent antitumor agent with improved tumor targeting effects and reduced off-target toxicities. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
|
-
- HY-113294
-
|
3-Hydroxy-DL-kynurenine
|
Endogenous Metabolite
Apoptosis
|
Neurological Disease
|
|
3-Hydroxykynurenine, a?metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis .
|
-
- HY-149298
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice .
|
-
- HY-151279
-
-
- HY-12130
-
|
|
CRFR
|
Neurological Disease
|
|
CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 has anxiolytic activities .
|
-
- HY-119163
-
-
- HY-122312
-
|
|
Monocarboxylate Transporter
|
Cancer
|
|
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity .
|
-
- HY-162100
-
|
|
ULK
Autophagy
|
Cancer
|
|
MR-2088 is a selective ULK1/ULK2 inhibitor with pEC50 values of 8.3 and 8.7, respectively. MR-2088 selectively inhibits autophagy through ULK1/2 mediated inhibition .
|
-
- HY-14877
-
-
- HY-124029
-
|
MMP13-IN-3
|
MMP
|
Inflammation/Immunology
|
|
BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM ) for the potential treatment of osteoarthritis . BI-4394 is >1000 selective over other MMPs .
|
-
- HY-136241
-
|
|
NAMPT
Caspase
|
Cancer
|
|
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and?induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies .
|
-
- HY-141609
-
|
AHR antagonist 5 free base
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
IK-175 is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. IK-175 effectively blocks AHR from translocating from the cytoplasm to the nucleus. IK-175 is highly selective for AHR over other receptors, transporters, and kinases .
|
-
- HY-111791
-
|
|
HDAC
|
Cancer
|
|
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
|
-
- HY-133024
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic .
|
-
- HY-126325
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity .
|
-
- HY-110148
-
|
|
Carboxylesterase
|
Metabolic Disease
|
|
WWL113 is a selective and orally active Ces3 and Ces1f inhibitor, with IC50 values of 120 nM and 100 nM for Ces3 and Ces1f, respectively. WWL113 appears to show excellent selectivity for the 60-kDa serine hydrolase (or hydrolases) .
|
-
- HY-14853
-
|
YM150
|
Factor Xa
Ser/Thr Protease
|
Cardiovascular Disease
|
|
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects .
|
-
- HY-122422A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Gepirone is a selective 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
|
-
- HY-122422
-
|
|
5-HT Receptor
|
Others
|
|
Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .
|
-
- HY-118532
-
|
AG30
|
EGFR
|
Cancer
|
|
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts .
|
-
- HY-12129
-
|
|
CFTR
|
Neurological Disease
|
|
CP 154526 hydrochloride is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 hydrochloride has anxiolytic activities .
|
-
- HY-101199
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function .
|
-
- HY-152107
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes .
|
-
- HY-14877A
-
|
SK-0403 hydrochloride
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
Metabolic Disease
|
|
Anagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively .
|
-
- HY-101724
-
|
NNC-05-1869 hydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
|
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
|
-
- HY-10427
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitory activity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction .
|
-
- HY-151569
-
|
|
HDAC
Apoptosis
|
Inflammation/Immunology
|
|
SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM), shows a 10- to 47-fold selectivity for HDAC6 compared to HDAC 1, 2, 3, and 8. SAHA-OH shows anti-inflammatory activity, and attenuates macrophage apoptosis .
|
-
- HY-16755
-
|
GSK-2586184; GLPG-0778
|
JAK
|
Inflammation/Immunology
|
|
Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
|
-
- HY-125286A
-
|
|
CD73
|
Cancer
|
|
AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
|
-
- HY-18947
-
|
|
HDAC
|
Cancer
|
|
SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.
|
-
- HY-124447
-
|
|
c-Myc
|
Cancer
|
|
BTYNB is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA (IC50=5 μM). BTYNB exhibits selectivity and effectiveness against IMP1-postive cancer cell lines. BTYNB can be used for cancer research .
|
-
- HY-12949
-
ML204
5 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels .
|
-
- HY-10505
-
|
TAK-700
|
Cytochrome P450
|
Cancer
|
|
Orteronel (TAK-700) is a highly selective?inhibitor of human?17,20-lyase (CYP17) with?IC50?of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4 .
|
-
- HY-120697
-
|
|
Wnt
β-catenin
|
Cancer
|
|
MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells .
|
-
- HY-101382
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
GR 103691 is a potent, selective dopamine D3 receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D3 over hD4 and hD1 sites .
|
-
- HY-120652
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors .
|
-
- HY-141716
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro .
|
-
- HY-100469
-
|
|
LXR
|
Cardiovascular Disease
|
|
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis .
|
-
- HY-122856
-
|
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-100607A
-
|
ONO1101 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist .
|
-
- HY-10898
-
-
- HY-125473
-
|
|
Endogenous Metabolite
|
Infection
|
|
IDX375 is a novel non-nucleoside inhibitor with selective inhibitory activity against HCV NS5B. IDX375 has good selectivity for genotypes 1a and 1b. The structure and binding site of IDX375 were confirmed by X-ray cocrystal studies .
|
-
- HY-B2010S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Fomesafen-d3 is the deuterium-labeled Fomesafen (HY-B2010). Fomesafen-d3 is a type of efficient and selective protoporphyrinogen IX oxidase (PPO) inhibitor. Fomesafen-d3 is a herbicide and has the advantages of low toxicity and high selectivity .
|
-
- HY-100607
-
-
- HY-139664
-
|
|
DNA Methyltransferase
|
Cancer
|
|
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-101980
-
|
HTL1071; AZD4635
|
Adenosine Receptor
|
Cancer
|
|
AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors .
|
-
- HY-102050
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
|
-
- HY-14398G
-
|
SC 58635
|
COX
|
Inflammation/Immunology
|
|
Celecoxib (GMP) is Celecoxib (HY-14398) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
|
-
- HY-12436
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM) .
|
-
- HY-101296
-
|
|
FGFR
Autophagy
|
Cancer
|
|
PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
|
-
- HY-14247
-
|
CGS 16949A; (Rac)-FAD286 hydrochloride
|
Cytochrome P450
|
Endocrinology
Cancer
|
|
Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
|
-
- HY-15226
-
-
- HY-101836
-
-
- HY-108458
-
-
- HY-U00428A
-
|
|
MAP4K
|
Cancer
|
|
GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
|
-
- HY-P10002
-
|
|
Proteasome
|
Cancer
|
|
EWFW-ACC is the tetrapeptide substrate for the immunoproteasome and has selectivity for the LMP7 subunits .
|
-
- HY-16069
-
|
Irbinitinib; ARRY-380; ONT-380
|
EGFR
|
Cancer
|
|
Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
|
-
- HY-11092
-
-
- HY-100520
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
|
-
- HY-76520
-
-
- HY-13079
-
|
GDC-0973 (R-enantiomer); XL-518 (R-enantiomer)
|
MEK
|
Cancer
|
|
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
|
-
- HY-59105
-
SC-560
2 Publications Verification
|
COX
|
Cancer
|
|
SC-560 is a potent and selective COX-1 inhibitor with an IC50 of 9 nM.
|
-
- HY-15709
-
-
- HY-145343
-
-
- HY-112570
-
|
|
ERK
|
Cancer
|
|
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
|
-
- HY-14164A
-
-
- HY-B1991
-
|
|
Herbicide
|
Others
|
|
Terbutryn is a selective herbicide and triazine compound that is absorbed by roots and leaves, acting as a photosynthesis inhibitor.
|
-
- HY-15467
-
|
|
VEGFR
|
Cancer
|
|
ZM323881 is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
|
-
- HY-158145
-
|
|
Phospholipase
|
Cancer
|
|
DS55980254 is a potent and selective phosphatidylserine synthase 1 (PTDSS1) inhibitor .
|
-
- HY-103060
-
-
- HY-21098
-
-
- HY-112604
-
-
- HY-50949
-
-
- HY-P5987
-
|
Myr-CaMKIINtide
|
CaMK
|
Neurological Disease
|
|
Calmodulin Kinase IINtide, Myristoylated (Myr-CaMKIINtide) is a selective and noncompetitive inhibitor of CaMKII .
|
-
- HY-15269
-
|
|
mTOR
PI3K
|
Cancer
|
|
PP30, a TORKinib, is a potent, selective, and ATP-competitive inhibitor of mTOR with an IC50 of 80 nM.
|
-
- HY-121895
-
|
|
Aurora Kinase
|
Cancer
|
|
BI 831266 is a potent and selective inhibitor of Aurora kinase B with antitumor activity .
|
-
- HY-111085
-
-
- HY-169139
-
-
- HY-111453
-
-
- HY-117364
-
|
|
DAPK
|
Others
|
|
HS148 (compound 22) is a selective DAPK3 inhibitor with an Ki value of 119 nM .
|
-
- HY-110037
-
-
- HY-A0229A
-
-
- HY-11077
-
-
- HY-12236
-
-
- HY-160107
-
-
- HY-139685
-
|
|
Cathepsin
|
Others
|
|
ABP 25 is an activity-based probe for cathepsin K imaging with excellent potency and selectivity.
|
-
- HY-109074
-
-
- HY-103482
-
|
|
MMP
|
Cancer
|
|
JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
|
-
- HY-139881
-
|
|
Btk
|
Cancer
|
|
BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
|
-
- HY-143518
-
-
- HY-B2042
-
|
|
Herbicide
|
Others
|
|
Butachlor is an herbicide of the acetanilide class. Butachlor is used as a selective pre-emergent herbicide .
|
-
- HY-145230
-
|
|
FGFR
|
Others
|
|
FGFR2-IN-1 is a selective FGFR2 inhibitor with an IC50 of 140 nM.
|
-
- HY-123744
-
-
- HY-18080
-
-
- HY-13441
-
-
- HY-142868
-
-
- HY-N3891
-
-
- HY-101525
-
|
|
Parasite
|
Infection
|
|
MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.
|
-
- HY-15193
-
-
- HY-139871
-
-
- HY-12704
-
-
- HY-117452
-
-
- HY-15341
-
BAM7
2 Publications Verification
|
Bcl-2 Family
|
Cancer
|
|
BAM7 is a direct and selective activator of proapoptotic BAX with an IC50 of 3.3 μM.
|
-
- HY-112703
-
-
- HY-75957
-
-
- HY-157348
-
-
- HY-163460
-
-
- HY-120559
-
-
- HY-15300
-
-
- HY-145238
-
-
- HY-18227
-
|
|
Raf
|
Cancer
|
|
B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
|
-
- HY-50864
-
|
|
Raf
|
Cancer
|
|
GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
|
-
- HY-168153
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-80 (compund 5) is a selective class I HDAC inhibitor .
|
-
- HY-107582
-
-
- HY-10180
-
|
|
Aurora Kinase
|
Cancer
|
|
MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
|
-
- HY-18013
-
|
|
FAAH
|
Metabolic Disease
|
|
JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor .
|
-
- HY-15226A
-
-
- HY-100615A
-
-
- HY-18293
-
|
|
JAK
Autophagy
|
Cancer
|
|
NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM .
|
-
- HY-136842
-
-
- HY-101778
-
|
EU-5346
|
Bcl-2 Family
|
Cancer
|
|
ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.
|
-
- HY-104005
-
-
- HY-100327
-
-
- HY-12510
-
-
- HY-101164
-
-
- HY-17495A
-
-
- HY-112645
-
-
- HY-B0102D
-
-
- HY-15574A
-
-
- HY-X0150
-
|
|
CDK
|
Cancer
|
|
JSH-150 is a highly selective and potent CDK9 inhibitor with an IC50 of 1 nM.
|
-
- HY-100836
-
-
- HY-U00178
-
-
- HY-13261
-
A66
4 Publications Verification
|
PI3K
|
Cancer
|
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- HY-79593
-
-
- HY-101582
-
-
- HY-19684
-
-
- HY-14390
-
-
- HY-U00083
-
|
ZK 38997; CGP 28238
|
COX
|
Inflammation/Immunology
|
|
Flosulide is a potent and selective COX-2 inhibitor, used for the treatment for inflammatory diseases.
|
-
- HY-50912
-
-
- HY-P0209
-
-
- HY-112298
-
-
- HY-134125
-
-
- HY-B0662A
-
|
KRP-197 hydrochloride; ONO-8025 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Imidafenacin hydrochloride is a potent and selective inhibitor of M3 receptors with a Kb of 0.317 nM .
|
-
- HY-107216
-
-
- HY-154846
-
|
|
COX
|
Others
|
|
4'-Aarboxylic acid imrecoxib is a metabolite of Imrecoxib, a selective COX-II inhibitor .
|
-
- HY-111512
-
-
- HY-12375
-
-
- HY-G0012
-
-
- HY-123657
-
-
- HY-15000
-
|
|
Kinesin
|
Cancer
|
|
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
|
-
- HY-12787
-
|
|
Raf
Autophagy
|
Cancer
|
|
L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.
|
-
- HY-108054
-
-
- HY-103577
-
|
|
Androgen Receptor
|
Cancer
|
|
LG-121071 is an orally active and selective androgen receptor modulator with a Ki of 17 nM .
|
-
- HY-120277
-
-
- HY-19468
-
-
- HY-15467A
-
|
|
VEGFR
|
Cancer
|
|
ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
|
-
- HY-138128
-
-
- HY-U00207
-
-
- HY-153122
-
-
- HY-50691
-
-
- HY-103335
-
-
- HY-109562A
-
|
GRK2-IN-1 hydrochloride
|
G Protein-coupled Receptor Kinase (GRK)
|
Cardiovascular Disease
|
|
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research .
|
-
- HY-170380
-
|
|
Epigenetic Reader Domain
Apoptosis
AMPK
c-Myc
PAK
Bcl-2 Family
|
Cancer
|
|
XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
|
-
- HY-109562
-
|
GRKs-IN-1
|
G Protein-coupled Receptor Kinase (GRK)
|
Cardiovascular Disease
|
|
CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research .
|
-
- HY-123824
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders .
|
-
- HY-113345R
-
|
|
Endogenous Metabolite
ROR
|
Cancer
|
|
Oxyphenbutazone (monohydrate) (Standard) is the analytical standard of Oxyphenbutazone (monohydrate). This product is intended for research and analytical applications. Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis .
|
-
- HY-15419
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-146170
-
|
|
Reactive Oxygen Species
EGFR
Apoptosis
|
Cancer
|
|
Anticancer agent 69 (Compound 34), a potent and selective anticancer agent , potently and selectively inhibits human prostate cancer cell line PC3 (IC50=26 nM). Anticancer agent 69 increases ROS level, down-regulates EGFR and induces apoptosis .
|
-
- HY-13406
-
TAK-779
2 Publications Verification
Takeda 779
|
CCR
HIV
CXCR
|
Infection
Inflammation/Immunology
Endocrinology
|
|
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
|
-
- HY-P1419
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
AP 811 is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 displays >20000-fold selectivity for NPR3 over NPR1. AP 811 abolishes ANP-induced pump stimulation .
|
-
- HY-13988
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2 .
|
-
- HY-111678
-
|
CID44640177; SID 88095709
|
BCRP
|
Cancer
|
|
ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively .
|
-
- HY-137377
-
|
|
Aurora Kinase
|
Cancer
|
|
TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites .
|
-
- HY-111304
-
-
- HY-13026
-
|
CAL-101; GS-1101
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
|
-
- HY-110157
-
|
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
|
-
- HY-19533
-
|
|
Adenosine Receptor
|
Cancer
|
|
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively .
|
-
- HY-16578S
-
|
|
Isotope-Labeled Compounds
PPAR
|
Cancer
|
|
GW9662-d5 is the deuterium labeled GW9662. GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively[1][2].
|
-
- HY-150513
-
|
|
SphK
|
Cancer
|
|
SLP9101555 (compound 14c) is a potent and selective SphK2 (sphingosine kinase 2) inhibitor (Ki=90 nM) with 200-fold selectivity over SphK1. SLP9101555 markedly decreases extracellular S1P (sphingosine 1-phosphate) levels .
|
-
- HY-102041
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
SMS2-IN-1 is a potent and highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM and a Kd of 37 nM. SMS2-IN-1 shows 150-fold selectivity for SMS2 over SMS1 (IC50 of 1000 nM) .
|
-
- HY-50859
-
|
INCB018424 sulfate
|
JAK
Autophagy
|
Cancer
|
|
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
|
-
- HY-12949A
-
|
|
TRP Channel
|
Neurological Disease
|
|
ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels .
|
-
- HY-B1355R
-
|
|
Bacterial
COX
|
Infection
Inflammation/Immunology
|
|
Oxyphenbutazone (monohydrate) (Standard) is the analytical standard of Oxyphenbutazone (monohydrate). This product is intended for research and analytical applications. Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis .
|
-
- HY-P1419A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation .
|
-
- HY-120972
-
|
|
Fluorescent Dye
|
Others
|
|
Pentafluorobenzenesulfonyl fluorescein is a H2O2-selective sensor that can be used to detect H2O2 levels in cells. Pentafluorobenzenesulfonyl fluorescein is normally non-fluorescent but fluoresces upon perhydrolysis of the sulfonyl linkage by H2O2 .
|
-
- HY-15419A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-157914
-
|
6,6-Dibenzyl-1,4,8,11-tetraoxacyclotetradecane
|
Biochemical Assay Reagents
|
Others
|
|
Dibenzyl-14-crown-4 (6,6-Dibenzyl-1,4,8,11-tetraoxacyclotetradecane) is a crown ether derivate, which serves as neutral carrier in PVC ion-selective electrode, improves the Li + selectivity against Na + and K + .
|
-
- HY-10449
-
|
TS 071
|
SGLT
|
Metabolic Disease
|
|
Luseogliflozin (TS 071) is a potent, selective, orally active sodium-dependent glucose cotransporter (SGLT) 2 inhibitor, with an IC50 of 2.26 nM, about 1765-fold selectivity over SGLT1 (IC50, 3990 nM). Luseogliflozin has the protential for researching type 2 diabetes .
|
-
- HY-P10216
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
CAQK peptide selectively binds to injured mouse brain. CAQK peptide selectively targets demyelinating areas and it is absent from healthy tissue. The CAQK peptide target is a proteoglycan complex upregulated in brain injuries and is used for drug delivery. CAQK peptide can penetrate the blood-brain barrier .
|
-
- HY-126346
-
|
|
GPR84
|
Inflammation/Immunology
|
|
DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe .
|
-
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-100345
-
|
|
TRP Channel
|
Neurological Disease
Cancer
|
|
AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV) .
|
-
- HY-151811
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
|
-
- HY-118279
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors .
|
-
- HY-15597
-
|
Procoxacin
|
Bacterial
Wnt
β-catenin
Mitophagy
Autophagy
Apoptosis
Antibiotic
Parasite
|
Cancer
|
|
Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells .
|
-
- HY-17416S
-
-
- HY-13225
-
|
RJR-2403 oxalate; (E)-Metanicotine oxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-126145
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4 .
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- HY-148381
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Epigenetic Reader Domain
PROTACs
Apoptosis
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Cancer
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A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer .
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- HY-111245
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- HY-18086
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SC 204330
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Pim
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Cancer
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TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM) .
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- HY-P1219
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β-TRTX-Cj1α
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Sodium Channel
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Neurological Disease
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Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
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- HY-162561
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Galectin
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Cancer
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GB1908 is a selective and orally active galectin-1 inhibitor with Ki values of 57 nM and 72 nM for human and mouse galectin-1, respectively. GB1908 displays >50-fold selectivity over galectin-3. GB1908 can be used for the study of lung cancer .
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- HY-13225B
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RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate
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nAChR
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Neurological Disease
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Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
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- HY-15951
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CID44968231; NCGC00188654
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CDK
DYRK
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Cancer
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ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B .
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- HY-123621
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Epigenetic Reader Domain
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Cancer
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GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin .
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- HY-101359
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GABA Receptor
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Neurological Disease
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TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .
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- HY-123038
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Adenosine Receptor
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Inflammation/Immunology
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CVT-5440 is a xanthine based, selective, high affinity A2B adenosine receptors (AdoR) antagonist with a Ki of 50 nM (selectivity A1> 200; A2A>200; A3>167). CVT-5440 has the potential for asthma research .
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