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competitive

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3121

Inhibitors & Agonists

5

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17

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30

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184

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22

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353

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218

Isotope-Labeled Compounds

10

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14

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9

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12031
    U0126-EtOH
    455+ Cited Publications

    MEK Autophagy Mitophagy Influenza Virus Cancer
    U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
    U0126-EtOH
  • HY-13452
    CID-1067700
    10+ Cited Publications

    ML282

    Ras Inflammation/Immunology
    CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
    CID-1067700
  • HY-B0334
    Sulbactam
    10+ Cited Publications

    CP45899

    Bacterial Antibiotic Infection
    Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
    Sulbactam
  • HY-15067
    DNQX
    10+ Cited Publications

    FG 9041

    iGluR Cancer
    DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
    DNQX
  • HY-109079A

    DWP14012 hydrochloride; Fexuprazan hydrochloride

    Proton Pump Metabolic Disease
    Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
    Abeprazan hydrochloride
  • HY-109079

    DWP14012; Fexuprazan

    Proton Pump Metabolic Disease
    Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
    Abeprazan
  • HY-B0334A
    Sulbactam sodium
    10+ Cited Publications

    CP45899 sodium

    Bacterial Antibiotic Infection
    Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
    Sulbactam sodium
  • HY-117043
    GRL0617
    10+ Cited Publications

    Deubiquitinase SARS-CoV Infection
    GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome .
    GRL0617
  • HY-100414
    Soraprazan
    2 Publications Verification

    BYK61359

    Proton Pump Metabolic Disease
    Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases .
    Soraprazan
  • HY-10195
    Ruboxistaurin
    10+ Cited Publications

    LY333531

    PKC Metabolic Disease
    Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM .
    Ruboxistaurin
  • HY-B1582A

    Aldadiene potassium; SC-14266

    Mineralocorticoid Receptor Cardiovascular Disease
    Canrenoate (Aldadiene) potassium, a proagent that releases canrenone, is a potent, competitive mineralocorticoid receptor (aldosterone receptor) antagonist. Potassium canrenoate, as a diuretic, is used for the research of hypertension .
    Canrenoate potassium
  • HY-P0222
    PKI(5-24)
    3 Publications Verification

    PKA Others
    PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
    PKI(5-24)
  • HY-101964
    SPI-112
    1 Publications Verification

    SHP2 Phosphatase Cancer
    SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively .
    SPI-112
  • HY-100606

    (-)-Pindolol; (S)-(-)-Pindolol; S-Pindolol

    5-HT Receptor Adrenergic Receptor Neurological Disease
    l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease .
    l-Pindolol
  • HY-N2554

    Ostenol

    Monoamine Oxidase PI3K Akt Apoptosis Infection Neurological Disease Cancer
    Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC50=0.74 μM, Ki=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer .
    Osthenol
  • HY-138568

    MAP4K Inflammation/Immunology
    HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs) .
    HPK1-IN-3
  • HY-118177

    Elastase Thrombin Ser/Thr Protease Inflammation/Immunology Cancer
    Neutrophil elastase inhibitor 1 (Compound 5b) is a competitive, pseudoirreversible inhibitor for neutrophil elastase with an IC50 of 7 nM .
    Neutrophil elastase inhibitor 1
  • HY-114991

    HPPD Others
    Leptospermone is a competitive, reversible inhibitor for p-Hydroxyphenylpyruvate dioxygenase (HPPD), with an IC50 of 12.1 μM. Leptospermone exhibits herbicidal activity for its bleaching effect .
    Leptospermone
  • HY-P1294

    CRFR Neurological Disease
    α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
    α-Helical CRF(9-41)
  • HY-110154

    Histone Demethylase Cancer
    NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer .
    NSC636819
  • HY-N6057

    Monoamine Oxidase Neurological Disease
    Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression .
    Obtusin
  • HY-P1292
    PKG inhibitor peptide
    2 Publications Verification

    PKG Cancer
    PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
    PKG inhibitor peptide
  • HY-10450S

    BMS-512148-d5

    Isotope-Labeled Compounds SGLT Metabolic Disease Cancer
    Dapagliflozin-d5 is a deuterium labeled Dapagliflozin (HY-10450). Dapagliflozin is a competitive SGLT2 inhibitor .
    Dapagliflozin-d5
  • HY-119016
    SK1-I
    1 Publications Verification

    BML-258

    SphK CaMK Cancer
    SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 μM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .
    SK1-I
  • HY-W013754

    Glutathione S-transferase Others
    S-Hexylglutathione is an S-substituted glutathione in which the hydrogen of the thiol has been replaced by a hexyl group. S-Hexylglutathione is also an competitive inhibitor against glutathione-S-transferase. S-Hexylglutathione can be used as an affinity chromatographic ligand for glutathione-S-transferase and glutathione peroxidase .
    S-Hexylglutathione
  • HY-155374

    Phosphatase Apoptosis Cancer
    PP5-IN-1 (Compound P053) is a competitive inhibitor of Serine/threonine protein phosphatase-5 (PP5) that binds to its catalytic domain and causes apoptosis in renal cancer .
    PP5-IN-1
  • HY-124366

    Phosphatase Infection Cancer
    Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
    Slingshot inhibitor D3
  • HY-132309
    BRD0639
    1 Publications Verification

    Histone Methyltransferase Cancer
    BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
    BRD0639
  • HY-127024

    Thyroid Hormone Receptor Metabolic Disease
    Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
    Thyroid hormone receptor antagonist (1-850)
  • HY-123517

    Enterovirus Infection
    DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM .
    DC07090 dihydrochloride
  • HY-19361

    Prostaglandin Receptor Neurological Disease
    L-826266 is a selective and competitive EP3 receptor antagonist. L-826266 can be used for convulsive disorders research .
    L-826266
  • HY-P1294A

    CRFR Neurological Disease
    α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
    α-Helical CRF(9-41) TFA
  • HY-19316

    O6-(Cyclohexylmethyl)guanine

    CDK Cancer
    NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
    NU2058
  • HY-P11112

    β-catenin Wnt Inflammation/Immunology
    PTD-DBM is a competitive peptide that blocks the CXXC5-Dvl interaction and induces the expression of β-catenin, α-SMA, and type I collagen. PTD-DBM has skin wound healing activity .
    PTD-DBM
  • HY-112468

    CDK Cancer
    PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively .
    PNU112455A hydrochloride
  • HY-162485

    Dengue Virus Virus Protease Infection
    DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
    DV-B-120
  • HY-103233
    DNQX disodium salt
    10+ Cited Publications

    FG 9041 disodium salt

    iGluR Cancer
    DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
    DNQX disodium salt
  • HY-158417

    LPL Receptor Inflammation/Immunology
    KSI-6666 is an orally active, competitive antagonist for sphingosine 1-phosphate receptor 1 (S1PR1), with an IC50 of 6.4 nM. KSI-6666 exhibits anti-inflammatory efficacy in autoimmune encephalomyelitis model and T cell transfer colitis model .
    KSI-6666
  • HY-115273

    P2Y Receptor Others
    MRS-2179 is a selective and competitive antagonist for P2Y1 receptor, with KB of 0.177 μM .
    MRS-2179
  • HY-129250

    Histamine Receptor Neurological Disease
    AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation .
    AZD5213
  • HY-W371165

    Complement System Inflammation/Immunology
    C1s-IN-1 trihydrochloride (Compound A1) is the selective inhibitor for C1s protease with the Ki of 5.8 μM. C1s-IN-1 trihydrochloride inhibits cleavage of C2 by C1s with an IC50 of 85 μM, inhibits the activation of classic pathway with an IC50 of 22 μM. C1s-IN-1 trihydrochloride is the competitive inhibitor for thrombin with the Ki of 51.2 μM .
    C1s-IN-1 trihydrochloride
  • HY-122203A
    PCS1055
    2 Publications Verification

    mAChR Cholinesterase (ChE) Neurological Disease
    PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
    PCS1055
  • HY-151591

    Phosphatase Metabolic Disease
    SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research .
    SPAA-52
  • HY-B0437AS

    MJ 1999-d6 hydrochloride

    Adrenergic Receptor Potassium Channel Cardiovascular Disease Endocrinology
    Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels .
    Sotalol-d6 hydrochloride
  • HY-10195A
    Ruboxistaurin mesylate
    10+ Cited Publications

    LY333531 mesylate

    PKC Cardiovascular Disease Metabolic Disease
    Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes .
    Ruboxistaurin mesylate
  • HY-N7536

    TRP Channel Others
    Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
    Voacangine
  • HY-P10877

    PAI-1 Cancer
    Bicyclic UK18 is a competitive inhibitor for human urokinase-type plasminogen activator (uPA) with a Ki of 53 nM .
    Bicyclic UK18
  • HY-P3786

    PKA PKC Cancer
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor .
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH
  • HY-A0252

    Adrenergic Receptor Inflammation/Immunology Cancer
    Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity .
    Bupranolol
  • HY-100782

    2-APH; 2-Amino-7-phosphonoheptanoic acid

    iGluR Neurological Disease
    DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice .
    DL-AP7

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