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Targets Recommended: PTEN SGK ATM/ATR SNIPER

Results for "Antagonists and inhibitors Inhibitors" in MCE Product Catalog:

295

Inhibitors & Agonists

26

Peptides

21

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-107430
    Oxythiamine

    Hydroxythiamin

    Others Cancer
    Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
  • HY-P1376
    G-Protein antagonist peptide

    mAChR Adrenergic Receptor
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-P1376A
    G-Protein antagonist peptide TFA

    mAChR Adrenergic Receptor
    G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
  • HY-109565
    ASTX660

    IAP Cancer
    ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
  • HY-14656
    Diltiazem hydrochloride

    CRD-401

    Calcium Channel Cardiovascular Disease
    Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
  • HY-113960
    ERRα antagonist-1

    Estrogen Receptor/ERR Cancer
    ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
  • HY-B0310
    Nizatidine

    Histamine Receptor Inflammation/Immunology Endocrinology
    Nizatidine is a histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion.
  • HY-B0004
    Doxofylline

    Adenosine Receptor Phosphodiesterase (PDE) Inflammation/Immunology
    Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
  • HY-16701
    BV6

    IAP Cancer
    BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
  • HY-15277
    AM966

    LPL Receptor Inflammation/Immunology
    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).
  • HY-13541
    ADH-1

    Others Cancer
    ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
  • HY-B0128
    Diphylline

    Diprophylline

    Adenosine Receptor Phosphodiesterase (PDE) Infection
    Dyphylline acts as an adenosine receptor antagonist and phosphodiesterase inhibitor, which is used in the treatment of respiratory disorders.
  • HY-100562
    Flopropione

    5-HT Receptor COMT Neurological Disease
    Flopropione is a 5-HT receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Flopropione also as an antispasmodic agent.
  • HY-13541A
    ADH-1 trifluoroacetate

    Others Cancer
    ADH-1 trifluoroacetate is an N-cadherin antagonist, which inhibits N-cadherin mediated cell adhesion.
  • HY-B0160
    Lafutidine

    FRG-8813

    Histamine Receptor Metabolic Disease Endocrinology
    Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
  • HY-128878
    Dexloxiglumide

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).
  • HY-103009
    MSX-127

    CXCR Cancer
    MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
  • HY-103010
    MSX-130

    CXCR Cancer
    MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
  • HY-129357
    CCK-B Receptor Antagonist 2

    Cholecystokinin Receptor Metabolic Disease
    CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC50 of 1.82 μM.
  • HY-B0478
    Trazodone hydrochloride

    AF-1161

    5-HT Receptor Neurological Disease
    Trazodone (hydrochloride) (AF-1161) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
  • HY-13282
    GANT 58

    NSC 75503

    Gli Cancer
    GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
  • HY-17024
    Cyclopamine

    11-Deoxojervine

    Hedgehog Smo Endogenous Metabolite Cancer
    Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
  • HY-19969
    YM-90709

    Interleukin Related Inflammation/Immunology
    YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor.
  • HY-U00354
    CP-060

    Calcium Channel Cardiovascular Disease
    CP-​060 is a potent Ca 2+ antagonist, inhibits Ca 2+ overload and possesses antioxidant and cardioprotective activities.
  • HY-116649
    CB1 antagonist 2

    Cannabinoid Receptor Neurological Disease
    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM.
  • HY-108323
    CCR2 antagonist 4

    Teijin compound 1

    CCR Inflammation/Immunology
    CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
  • HY-103362
    CCR2 antagonist 4 hydrochloride

    Teijin compound 1 hydrochloride

    CCR Inflammation/Immunology
    CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
  • HY-15284
    Prasugrel

    PCR 4099

    P2Y Receptor Cardiovascular Disease
    Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-15284A
    Prasugrel hydrochloride

    PCR 4099 hydrochloride

    P2Y Receptor Cardiovascular Disease
    Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-U00028
    T 82

    5-HT Receptor AChE Neurological Disease
    T 82 is a potent 5-HT3 antagonist and acetylcholinesterase (AChE) inhibitor, used for treatment of Alzheimer's Disease.
  • HY-B1305
    Chloropyramine hydrochloride

    FAK Histamine Receptor VEGFR Cancer Endocrinology
    Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
  • HY-14276A
    Gallopamil hydrochloride

    Methoxyverapamil hydrochloride

    Calcium Channel Cardiovascular Disease
    Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
  • HY-14276
    Gallopamil

    Methoxyverapamil

    Calcium Channel Cardiovascular Disease
    Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
  • HY-112730
    PEO-IAA

    2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid

    Others Others
    PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
  • HY-17390
    Loxapine

    5-HT Receptor Neurological Disease
    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  • HY-104020A
    Philanthotoxin 74 dihydrochloride

    PhTx 74 dihydrochloride

    iGluR Neurological Disease
    Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
  • HY-17390A
    Loxapine succinate

    5-HT Receptor Neurological Disease
    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  • HY-100407
    JNJ16259685

    mGluR Neurological Disease
    JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
  • HY-15284B
    Prasugrel (Maleic acid)

    PCR 4099 (Maleic acid)

    P2Y Receptor Cardiovascular Disease
    Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-102004
    Rilapladib

    SB 659032

    Phosphatase Inflammation/Immunology Neurological Disease
    Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.
  • HY-101503
    HTS01037

    FABP Metabolic Disease
    HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
  • HY-19900
    ITX5061

    p38 MAPK Autophagy HCV Infection
    ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
  • HY-15676
    Idasanutlin

    RG7388

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
  • HY-113534
    MV1

    IAP Others
    MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
  • HY-103361
    SB297006

    CCR Neurological Disease Endocrinology
    SB297006 is a CCR3 antagonist, which significantly inhibits proliferation and neurosphere formation in CCL11-treated neural progenitor cells.
  • HY-133570
    17-AEP-GA

    HSP ADC Cytotoxin Cancer
    17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
  • HY-13535A
    ATN-161 trifluoroacetate salt

    ATN-161 TFA salt

    Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-19189
    Terbogrel

    BIBV 308SE

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
  • HY-19062
    SM-6586

    Calcium Channel Na+/Ca2+ Exchanger Cardiovascular Disease
    SM-6586 is a calcium channel antagonist and inhibitor of Na +/H + and Na +/Ca 2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
  • HY-101458A
    IT1t dihydrochloride

    CXCR HIV Inflammation/Immunology Endocrinology Cancer
    IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-100506
    GLPG0187

    Integrin Cancer
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
  • HY-19205A
    CMI-392

    Lipoxygenase Inflammation/Immunology
    CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
  • HY-108634
    Apafant

    WEB 2086

    Others Inflammation/Immunology
    Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
  • HY-125820
    Sigma-1 receptor antagonist 3

    Sigma Receptor Potassium Channel Neurological Disease
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain.
  • HY-12684
    CH-223191

    Aryl Hydrocarbon Receptor Cancer
    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
  • HY-B0725
    Doxepin Hydrochloride

    Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2.
  • HY-13505
    AM281

    Cannabinoid Receptor Neurological Disease
    AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM.
  • HY-16711
    SB225002

    CXCR Inflammation/Immunology Endocrinology Cancer
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
  • HY-19084
    Ro-24-0238

    Others Inflammation/Immunology
    Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
  • HY-129241
    AGX51

    Others Cancer
    AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization.
  • HY-B1789A
    Telenzepine dihydrochloride

    mAChR Neurological Disease
    Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects.
  • HY-108522
    PA452

    RAR/RXR Metabolic Disease
    PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
  • HY-120261
    GB-88

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca 2+ release with an IC50 of 2 µM.
  • HY-B0281A
    Ranitidine hydrochloride

    Histamine Receptor Cytochrome P450 Bacterial Infection Endocrinology Metabolic Disease
    Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9.
  • HY-N2003
    D-Tetrahydropalmatine

    Dopamine Receptor Metabolic Disease
    D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
  • HY-B0693
    Ranitidine

    Histamine Receptor Bacterial Cytochrome P450 Infection Endocrinology Metabolic Disease
    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine is a weak inhibitor of CYP2C19 and CYP2C9.
  • HY-117819
    TMP920

    ROR Inflammation/Immunology
    TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
  • HY-B1388
    Homatropine methylbromide

    Homatropine methobromide

    mAChR Neurological Disease
    Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
  • HY-120691A
    GSK205

    TRP Channel Metabolic Disease Inflammation/Immunology
    GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca 2+ influx.
  • HY-B0323
    Sulfisoxazole

    Sulfafurazole

    Bacterial Endothelin Receptor Antibiotic Cancer Infection Endocrinology
    Sulfisoxazole (Sulfafurazole), an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
  • HY-111534
    SBI-115

    GPCR19 Others
    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
  • HY-100760
    Toxoflavin

    Xanthothricin; Toxoflavine; PKF-118-310

    β-catenin Cancer
    Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
  • HY-A0081
    Fluphenazine dihydrochloride

    Dopamine Receptor Neurological Disease Cancer
    Fluphenazine dihydrochloride is a phenothiazine-class D1DR and D2DR inhibitor; used to deliver Fluphenazine to biological systems in studies probing the effects and metabolic fates of this commonly used dopamine antagonist.
  • HY-15894
    BQ-788 sodium salt

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
  • HY-P1104A
    FC131 TFA

    CXCR HIV Infection
    FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
  • HY-121450
    Lavoltidine

    Loxtidine; AH-234844

    Histamine Receptor Cancer
    Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
  • HY-B0725S
    Doxepin D3 Hydrochloride

    Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin D3 Hydrochloride is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2.
  • HY-13955
    Telmisartan

    BIBR 277

    Angiotensin Receptor Autophagy Cardiovascular Disease Endocrinology
    Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
  • HY-15568A
    A-317491 sodium salt hydrate

    P2X Receptor Autophagy Neurological Disease Cancer
    A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.
  • HY-B0745
    Ramatroban

    BAY u3405

    Prostaglandin Receptor Inflammation/Immunology Endocrinology Cancer
    Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
  • HY-15043
    ELN-441958

    Bradykinin Receptor Cancer Endocrinology
    ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM.
  • HY-100183
    GSK2239633A

    CCR Inflammation/Immunology Endocrinology
    GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [ 125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11.
  • HY-B0365A
    Memantine hydrochloride

    D-145 hydrochloride

    Cytochrome P450 iGluR Autophagy Neurological Disease
    Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively.
  • HY-19344
    Lifitegrast

    SAR 1118; SHP-606

    Integrin Inflammation/Immunology
    Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
  • HY-15568
    A-317491

    P2X Receptor Autophagy Neurological Disease Cancer
    A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.
  • HY-100208
    HC-067047

    TRP Channel Cancer
    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
  • HY-10309
    Sibrafiban

    RO 48-3657

    Integrin Cardiovascular Disease
    Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
  • HY-103473A
    Boc-MLF TFA

    Boc-Met-Leu-Phe-OH (TFA)

    Others Inflammation/Immunology
    Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
  • HY-107500
    UVI 3003

    RAR/RXR Autophagy Others
    UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
  • HY-108136A
    Bisindolylmaleimide X hydrochloride

    BIM-X hydrochloride; Ro31-8425 hydrochloride

    PKC CDK Cardiovascular Disease
    Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
  • HY-16952A
    Bepridil hydrochloride hydrate

    (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate

    Calcium Channel Cardiovascular Disease
    Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
  • HY-N7512
    Asimilobine

    Dopamine Receptor 5-HT Receptor Parasite Cancer Infection
    Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
  • HY-30234
    Clemizole

    Histamine Receptor HCV Protease HCV Inflammation/Immunology Endocrinology Cancer
    Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
  • HY-119093
    Halopemide

    Phospholipase Dopamine Receptor Cancer Neurological Disease
    Halopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent.
  • HY-30234A
    Clemizole hydrochloride

    Histamine Receptor HCV Protease HCV Cancer Inflammation/Immunology Endocrinology
    Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
  • HY-32329
    Setiptiline

    Org-8282

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-14136
    Rimonabant

    SR141716

    Cannabinoid Receptor Bacterial Infection Metabolic Disease Cancer
    Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
  • HY-14882A
    Cenicriviroc Mesylate

    TAK-652 Mesylate; TBR-652 Mesylate

    CCR HIV Infection Inflammation/Immunology Endocrinology
    Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
  • HY-103178
    MRE3008F20

    Adenosine Receptor Cancer
    MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
  • HY-14137
    Rimonabant Hydrochloride

    SR 141716A Hydrochloride

    Cannabinoid Receptor Bacterial Cancer Infection Metabolic Disease
    Rimonabant hHydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
  • HY-10792A
    Eplivanserin (mixture)

    SR-46349 (mixture)

    Serotonin Transporter 5-HT Receptor Neurological Disease
    Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1.
  • HY-P1263
    tcY-NH2

    (trans-Cinnamoyl)-YPGKF-NH2

    Protease-Activated Receptor (PAR) Metabolic Disease
    tcY-NH2 is a selective rat PAR4 antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced rat platelet aggregation.
  • HY-19529
    Ro 46-2005

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
  • HY-13696
    MSX-122

    CXCR Cancer Inflammation/Immunology Endocrinology
    MSX-122 is an orally active partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 has anti-inflammatory and anti-metastatic activity.
  • HY-111444
    Auxinole

    Others Others
    Auxinole is a potent auxin antagonist of TIR1/AFB receptors, binding TIR1 to block the formation of the TIR1-IAA-Aux/IAA complex and so inhibits auxin-responsive gene expression.
  • HY-100714A
    D-AP5

    D-APV; D-2-Amino-5-phosphonovaleric acid

    iGluR Neurological Disease
    D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
  • HY-12025
    Serdemetan

    JNJ-26854165

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
  • HY-18263C
    Elubrixin tosylate

    SB-656933 tosylate

    CXCR Interleukin Related Inflammation/Immunology
    Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
  • HY-P7061A
    ALX 40-4C Trifluoroacetate

    CXCR Infection Endocrinology
    ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-P1189
    Echistatin

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-107613
    R 59-022

    DKGI-I; Diacylglycerol kinase inhibitor I

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-P7061
    ALX 40-4C

    CXCR Infection Endocrinology
    ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-P1119
    WRW4

    Others Neurological Disease
    WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
  • HY-P1263A
    tcY-NH2 TFA

    (trans-Cinnamoyl)-YPGKF-NH2 TFA

    Protease-Activated Receptor (PAR) Metabolic Disease
    tcY-NH2 TFA is a selective rat PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH2-induced rat platelet aggregation.
  • HY-15450A
    INCB 3284

    CCR Endocrinology
    INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
  • HY-B1238
    Pronethalol

    (±)-Pronethalo

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
  • HY-114412A
    TD-0212 TFA

    Angiotensin Receptor Neprilysin Inflammation/Immunology
    TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.
  • HY-14406A
    L-733060 hydrochloride

    Neurokinin Receptor Cancer Neurological Disease
    L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent.
  • HY-14609
    MPEP Hydrochloride

    mGluR Neurological Disease
    MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects.
  • HY-B1238A
    Pronethalol hydrochloride

    (±)-Pronethalo hydrochloride

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs).
  • HY-12600
    AZD5582

    IAP Apoptosis Cancer
    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-14609A
    MPEP

    mGluR Neurological Disease
    MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects.
  • HY-136588
    trans-R-138727MP

    Prasugrel metabolite R-138727MP

    P2Y Receptor Cardiovascular Disease
    trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-100036
    MK-4101

    Smo Apoptosis Hedgehog Cancer
    MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
  • HY-P1189A
    Echistatin TFA

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-133529
    PA-8

    Others Inflammation/Immunology Neurological Disease
    PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.
  • HY-N6932
    Voacamine

    Cannabinoid Receptor P-glycoprotein Cancer Metabolic Disease
    Voacamine, an indole alkaloid, isolated from Voacanga Africana, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
  • HY-15071
    YM90K

    iGluR Neurological Disease
    YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions.
  • HY-136142
    Prasugrel chloride impurity

    Others Others
    Prasugrel chloride impurity is a catp impurity of Prasugrel, exacted from patent US20130345428A1, line 0053. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
  • HY-15319
    AMG 487

    CXCR Cancer Inflammation/Immunology Endocrinology
    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
  • HY-P1201
    Cyclosomatostatin

    Somatostatin Receptor Cancer
    Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
  • HY-N2510
    Myristicin

    Myristicine

    5-HT Receptor Neurological Disease
    Myristicine  act as a serotonin receptor antagonist, a weak monamine oxidase (MAO) inhibitor. Myristicine is the main component of nutmeg essential oil from Myristica fragrans Houtt. Myristicine abuse produce hallucinogenic effects, organ damage, deliriumand others.
  • HY-10858
    WAY 316606

    sFRP-1 Cancer
    WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
  • HY-B0640A
    Epinastine hydrochloride

    WAL801 hydrochloride

    Histamine Receptor Endocrinology Inflammation/Immunology
    Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action.
  • HY-119293
    K777

    Cathepsin CCR Cytochrome P450 Cancer Infection
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
  • HY-100619
    BMS-986020

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-100619A
    BMS-986020 sodium

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-14882
    Cenicriviroc

    TAK-652; TBR-652

    CCR HIV Infection Endocrinology
    Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
  • HY-108707
    LY3130481

    iGluR Neurological Disease
    LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC50 of 65 nM.
  • HY-101512
    A-395

    Histone Methyltransferase Cancer
    A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
  • HY-N2600
    Kuwanon H

    Bombesin Receptor Cancer
    Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
  • HY-B0640
    Epinastine

    WAL801

    Histamine Receptor Inflammation/Immunology Endocrinology
    Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action.
  • HY-113038
    D-α-Hydroxyglutaric acid

    (R)-2-Hydroxypentanedioic acid

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid ((R)-2-Hydroxypentanedioic acid) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-P1076
    CALP2

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
  • HY-12206
    Thioperamide

    MR-12842

    Histamine Receptor Neurological Disease
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-P1201A
    Cyclosomatostatin TFA

    Somatostatin Receptor Cancer
    Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
  • HY-U00235
    SR121566A

    Integrin Inflammation/Immunology
    SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
  • HY-121356
    Carebastine

    Histamine Receptor Cancer Endocrinology
    Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner. Carebastine suppresses the expression of macrophage migration inhibitory factor.
  • HY-17042A
    Cetirizine dihydrochloride

    P071

    Histamine Receptor Inflammation/Immunology Endocrinology
    Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-100224
    SANT-1

    Smo Hedgehog Cancer
    SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.
  • HY-120210
    XY018

    ROR Cancer Inflammation/Immunology
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
  • HY-10799
    EG00229

    Complement System Cancer
    EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.
  • HY-17042
    Cetirizine

    Histamine Receptor Inflammation/Immunology Endocrinology
    Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-16697
    CID 16020046

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
  • HY-107139
    JNJ-10229570

    Melanocortin Receptor Endocrinology
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-117407
    ALLO-2

    Smo Cancer
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  • HY-109619
    D4-abiraterone

    Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite

    Androgen Receptor Cytochrome P450 Cancer
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
  • HY-11018
    Risperidone

    R 64 766

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-A0118A
    Naloxegol oxalate

    NKTR-118 oxalate; AZ-13337019 oxalate

    Opioid Receptor Neurological Disease
    Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
  • HY-P1271
    Catestatin

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-P1076A
    CALP2 TFA

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
  • HY-15971A
    AMD 3465

    GENZ-644494

    CXCR HIV Infection Endocrinology
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-124957
    α-NETA

    Apoptosis Cancer
    α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM. α-NETA is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM). α-NETA has anti-cancer activity.
  • HY-100660A
    Cetirizine Impurity B dihydrochloride

    Others Others
    Cetirizine Impurity B dihydrochloride is an impurity of Cetirizine dihydrochloride. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-101483
    Dihydromunduletone

    DHM

    Others Cancer Neurological Disease
    Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
  • HY-13636
    Fulvestrant

    ICI 182780; ZD 9238; ZM 182780

    Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
  • HY-P1293
    Conantokin G

    iGluR Neurological Disease
    Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties.
  • HY-100661
    Cetirizine Impurity D

    Histamine Receptor Endocrinology Inflammation/Immunology
    Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
  • HY-103254
    ML221

    Others Neurological Disease
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
  • HY-P0299A
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
  • HY-11018A
    Risperidone hydrochloride

    R 64 766 hydrochloride

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-13406
    TAK-779

    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-107515
    LY367385

    mGluR Neurological Disease
    LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.
  • HY-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-14415
    SR8278

    Others Metabolic Disease
    SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
  • HY-12407
    ZK168281

    VD/VDR Metabolic Disease
    ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
  • HY-14518
    Aminopterin

    4-Aminofolic acid; APGA

    Antifolate Cancer Inflammation/Immunology
    Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.
  • HY-12011
    HA14-1

    Bcl-2 Family Cancer
    HA14-1 is a Bcl-2/Bcl-XL antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC50 of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.
  • HY-11028
    PF-02413873

    PF-2413873

    Progesterone Receptor Endocrinology
    PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.
  • HY-101283
    HCH6-1

    Others Inflammation/Immunology
    HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), an emerging therapeutic target for the discovery of drugs to treat neutrophilic inflammatory diseases. HCH6-1 is a selective FPR1 inhibitor and has protective effects against acute lung injury (ALI). HCH6-1 inhibits superoxide anion generation, elastase release, and chemotaxis in human neutrophils activated by fMLF (an FPR1 agonist).
  • HY-15971
    AMD 3465 hexahydrobromide

    GENZ-644494 hexahydrobromide

    CXCR HIV Infection Endocrinology
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-100542
    D-α-Hydroxyglutaric acid disodium

    Disodium (R)-2-hydroxyglutarate

    Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM.
  • HY-N3945
    Glaucine

    O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396

    Phosphodiesterase (PDE) Calcium Channel Adrenergic Receptor Dopamine Receptor Influenza Virus Infection Inflammation/Immunology
    Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
  • HY-125171
    IAXO-102

    Toll-like Receptor (TLR) Inflammation/Immunology
    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
  • HY-P1271A
    Catestatin TFA

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-116042
    FSCPX

    Adenosine Receptor Neurological Disease
    FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.
  • HY-16992A
    W-54011

    Complement System Reactive Oxygen Species Inflammation/Immunology
    W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
  • HY-123205
    Oxatomide

    Histamine Receptor P2X Receptor 5-HT Receptor Inflammation/Immunology
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
  • HY-11018B
    Risperidone mesylate

    R 64 766 mesylate

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-P1293A
    Conantokin G TFA

    iGluR Neurological Disease
    Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties.
  • HY-125176
    G907

    Bacterial Infection
    G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
  • HY-103460
    IRL 2500

    Endothelin Receptor Cardiovascular Disease
    IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
  • HY-15894A
    BQ-788

    Endothelin Receptor Cardiovascular Disease Endocrinology
    BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
  • HY-17042AS
    Cetirizine D4 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    Cetirizine D4 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-B1866
    Linuron

    Androgen Receptor Endocrinology
    Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
  • HY-10046
    Plerixafor

    AMD 3100; JM3100; SID791

    CXCR HIV Virus Protease Cancer Infection Endocrinology Inflammation/Immunology
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
  • HY-17042S
    Cetirizine D4

    Histamine Receptor Inflammation/Immunology
    Cetirizine D4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-17042S1
    Cetirizine D8

    Histamine Receptor Inflammation/Immunology
    Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-10119
    Vorapaxar

    SCH 530348

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
  • HY-117656
    ESI-05

    NSC 116966

    Others Others
    ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
  • HY-16322
    Minodronic acid

    YM-529

    P2X Receptor Apoptosis Cancer
    Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.
  • HY-17042AS1
    Cetirizine D8 dihydrochloride

    Histamine Receptor Inflammation/Immunology
    Cetirizine D8 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
  • HY-103354
    Proglumide sodium

    Cholecystokinin Receptor Cancer Endocrinology Neurological Disease
    Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
  • HY-133533
    O-2050

    Cannabinoid Receptor
    O-2050 is a high affinity cannabinoid CB1 receptor silent antagonist. O-2050 also acts as a partial agonist in inhibiting forksolin-induced cyclic AMP stimulation (EC50=40.4 nM). O-2050 antagonizes effects of CP-55940 in vitro.
  • HY-P2285
    AC 253

    Amyloid-β
    AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
  • HY-100912
    W-7 hydrochloride

    CaMK Phosphodiesterase (PDE) Myosin Apoptosis Cancer
    W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.
  • HY-110166
    PD 90780

    Others Neurological Disease
    PD 90780 is a non peptide antagonist of nerve growth factor (NGF) binding to the P75 NGF receptor, inhibits NGF-p75 NTR interaction with IC50s values of 23.1 µM and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .
  • HY-B1330
    Proglumide

    Cholecystokinin Receptor Cancer Endocrinology Neurological Disease
    Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities.
  • HY-101676
    RG-12525

    NID 525

    Leukotriene Receptor PPAR Cytochrome P450 Metabolic Disease
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
  • HY-B0845
    Prochloraz

    BTS 40542

    Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor
    Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s = 25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50 = 1 μM).
  • HY-103355
    YM022

    CCR Metabolic Disease
    YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
  • HY-13628
    Etalocib

    LY293111; VML 295

    Leukotriene Receptor Apoptosis Cancer Inflammation/Immunology
    Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [ 3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
  • HY-100675
    JTE-013

    LPL Receptor Apoptosis Cancer
    JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
  • HY-12143
    Vofopitant dihydrochloride

    GR 205171A

    Neurokinin Receptor Cancer Neurological Disease Endocrinology
    Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ 3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent.
  • HY-15086
    Selfotel

    CGS 19755

    iGluR Neurological Disease
    Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM.
  • HY-B0290A
    Pranlukast hemihydrate

    ONO-1078 hemihydrate

    Leukotriene Receptor Inflammation/Immunology
    Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
  • HY-15023
    Cligosiban

    PF-3274167

    Oxytocin Receptor Endocrinology
    Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents.
  • HY-B0290
    Pranlukast

    ONO-1078

    Leukotriene Receptor Inflammation/Immunology
    Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
  • HY-128694
    Foropafant

    SR27417

    Others Cardiovascular Disease
    Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets.
  • HY-135194
    Risperidone E-oxime

    Others Others
    Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
  • HY-50101A
    Mavorixafor trihydrochloride

    AMD-070 trihydrochloride

    CXCR HIV Infection Endocrinology
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-N5025
    Bullatine A

    P2X Receptor Cancer Inflammation/Immunology
    Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
  • HY-103354A
    Proglumide hemicalcium

    Cholecystokinin Receptor Cancer Endocrinology Neurological Disease
    Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities.
  • HY-112683
    V-9302

    Others Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-17611
    Etripamil

    MSP-2017; (-)-MSP-2017

    Calcium Channel Cardiovascular Disease
    Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
  • HY-18641
    Ki16198

    LPL Receptor Cancer
    Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with Ki values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo.
  • HY-112683A
    V-9302 hydrochloride

    Others Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-17377
    Vicriviroc maleate

    SCH-417690 maleate; SCH-D maleate

    CCR HIV Infection Endocrinology
    Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
  • HY-50101
    Mavorixafor

    AMD-070

    CXCR HIV Infection Endocrinology
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-14166
    MK-886

    L 663536

    FLAP Leukotriene Receptor PPAR Apoptosis Cancer
    MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
  • HY-112055
    DIM-C-pPhOH

    Apoptosis Cancer
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
  • HY-112461A
    NF449 octasodium

    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 G-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-15478
    WZ811

    CXCR Cancer Endocrinology
    WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
  • HY-121300
    Kendomycin

    (-)-TAN2162

    Antibiotic Bacterial Endothelin Receptor CGRP Receptor Cancer Infection
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
  • HY-100383
    BH3I-1

    BHI1; BH 3I1

    Bcl-2 Family MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
  • HY-19578B
    Isamoltane hemifumarate

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
  • HY-Y0265
    Isatin

    Indoline-2,3-dione

    Monoamine Oxidase Apoptosis Cancer Neurological Disease Cardiovascular Disease
    Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM). Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity. Shows effect on the serotonergic system.
  • HY-126010
    Dooku1

    Others Cardiovascular Disease
    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
  • HY-10656
    SB-657510

    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-14994
    SCH79797 dihydrochloride

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-N2359
    Chelerythrine

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
  • HY-100811
    7-Chlorokynurenic acid

    7-CKA

    iGluR Neurological Disease
    7-Chlorokynurenic acid (7-CKA) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-10797
    CJ-42794

    CJ-042794

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CJ-42794 is a selective prostaglandin E receptor subtype 4 (EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).
  • HY-111875
    SNIPER(BRD)-1

    SNIPER Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively.
  • HY-100811A
    7-Chlorokynurenic acid sodium salt

    7-CKA sodium salt

    iGluR Neurological Disease
    7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid sodium salt is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid sodium salt has potent antinociceptive actions after neuraxial delivery.
  • HY-103364A
    C-021 dihydrochloride

    CCR Inflammation/Immunology
    C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [ 35S]GTPγS from binding to the receptor with an IC50 of 18 nM.
  • HY-10341
    Fasudil Hydrochloride

    HA-1077 Hydrochloride; AT-877 Hydrochloride

    ROCK Calcium Channel Autophagy PKA PKC HIV Cancer
    Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
  • HY-117958
    HJC0197

    Others Cancer Metabolic Disease Cardiovascular Disease
    HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
  • HY-106994A
    Nebentan potassium

    YM598

    Endothelin Receptor Inflammation/Immunology
    Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
  • HY-N6962
    α-Spinasterol

    TRP Channel COX Infection Neurological Disease
    α-Spinasterol, isolated from Spinacia oleracea, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
  • HY-106994
    Nebentan

    YM598 free base

    Endothelin Receptor Inflammation/Immunology Cardiovascular Disease
    Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
  • HY-135594
    4'-Raloxifene-β-D-glucopyranoside

    Estrogen Receptor/ERR Metabolic Disease
    4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
  • HY-10341A
    Fasudil

    HA-1077; AT877

    ROCK Calcium Channel Autophagy PKA PKC Cancer
    Fasudil (HA-1077; AT877), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+channel antagonist and vasodilator.
  • HY-135595
    6-Raloxifene-β-D-glucopyranoside

    Estrogen Receptor/ERR Drug Metabolite Metabolic Disease
    6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
  • HY-N1957
    Gamma-Mangostin

    γ-Mangostin

    5-HT Receptor Metabolic Disease
    Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 µM) .
  • HY-103430
    SKF-83566 hydrobromide

    Dopamine Receptor 5-HT Receptor Adenylate Cyclase Neurological Disease
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.
  • HY-103430A
    SKF-83566

    Dopamine Receptor 5-HT Receptor Adenylate Cyclase Neurological Disease
    SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.
  • HY-100943
    Cinanserin hydrochloride

    SQ 10643

    5-HT Receptor Influenza Virus Infection Inflammation/Immunology
    Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
  • HY-B0573
    Propranolol hydrochloride

    Adrenergic Receptor Neurological Disease Endocrinology
    Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-125028
    Hck-IN-1

    Src HIV Infection
    Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.
  • HY-B0573B
    Propranolol

    Adrenergic Receptor Neurological Disease Cardiovascular Disease Endocrinology
    Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-B0135A
    Furosemide sodium

    NKCC Cancer Metabolic Disease
    Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
  • HY-B0135
    Furosemide

    NKCC Metabolic Disease Cancer
    Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
  • HY-100277
    Mifobate

    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-15724A
    Vercirnon sodium

    GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-15724
    Vercirnon

    GSK-1605786; CCX282-B; Traficet-EN

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-P1106
    K41498

    CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 can be used for hypotension study.
  • HY-107691
    GR 159897

    Neurokinin Receptor Cancer Endocrinology Neurological Disease
    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
  • HY-15342
    Timapiprant

    OC000459

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-15342A
    Timapiprant sodium

    OC000459 sodium

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-D0976
    NF279

    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-114263
    NXT629

    PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • HY-13285
    Ki16425

    Debio 0719

    LPL Receptor Neurological Disease Cancer
    Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
  • HY-P1106A
    K41498 TFA

    CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-B0573S
    Propranolol D7 hydrochloride

    Adrenergic Receptor Endocrinology Neurological Disease Cardiovascular Disease
    Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-112146
    MMG-11

    Toll-like Receptor (TLR) Inflammation/Immunology
    MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.
  • HY-112146A
    MMG-11 quarterhydrate

    Toll-like Receptor (TLR) Inflammation/Immunology
    MMG-11 quarterhydrate is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 quarterhydrate inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.
  • HY-B0822
    Fipronil

    GABA Receptor Cytochrome P450 Neurological Disease
    Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
  • HY-10895
    SB-334867

    SB 334867A

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-12882A
    Ifenprodil tartrate

    iGluR Potassium Channel Neurological Disease
    Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
  • HY-10895A
    SB-334867 free base

    SB334867A free base

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-19306
    SB-267268

    Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
  • HY-N4267
    Yangambin

    Calcium Channel Infection Cardiovascular Disease
    Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM.
  • HY-101308A
    MRS2179 tetrasodium hydrate

    P2Y Receptor Cardiovascular Disease
    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.
  • HY-108400
    SCH-23390 maleate

    R-(+)-SCH-23390 maleate

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-19545A
    SCH-23390 hydrochloride

    R-(+)-SCH-23390 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-P1110
    AF12198

    Interleukin Related Inflammation/Immunology
    AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
  • HY-19974
    TAK-220

    CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.