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Competitive

" in MedChemExpress (MCE) Product Catalog:

1645

Inhibitors & Agonists

1

Screening Libraries

7

Fluorescent Dye

10

Biochemical Assay Reagents

109

Peptides

4

Inhibitory Antibodies

161

Natural
Products

115

Isotope-Labeled Compounds

6

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147167
    Bz-D-Arg-pNA hydrochloride

    		Ser/Thr Protease Others
    Bz-D-Arg-pNA hydrochloride is a competitive trypsin inhibitor .
    Bz-D-Arg-pNA hydrochloride
  • HY-120182
    GR 128107

    		Melatonin Receptor Cancer
    GR 128107 is a competitive melatonin receptor antagonist (pKi: 9.6) .
    GR 128107
  • HY-P3786
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH

    		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-136344
    Simvastatin Acyl-β-D-glucuronide

    		Drug Metabolite Others
    Simvastatin Acyl-β-D-glucuronide is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
    Simvastatin Acyl-β-D-glucuronide
  • HY-136345
    (Rac)-3′-Hydroxy simvastatin

    		Drug Metabolite Others
    (Rac)-3′-Hydroxy simvastatin is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
    (Rac)-3′-Hydroxy simvastatin
  • HY-136347
    3α-Hydroxy pravastatin sodium

    		HMG-CoA Reductase (HMGCR) Drug Metabolite Cardiovascular Disease
    3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor .
    3α-Hydroxy pravastatin sodium
  • HY-P1292
    PKG inhibitor peptide

    		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-107704
    SDZ 220-040

    		iGluR Neurological Disease
    SDZ 220-040 is a competitive the mammalian NMDA receptor antagonist .
    SDZ 220-040
  • HY-129250
    AZD5213

    		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-105375
    FR 901537

    		Cytochrome P450 Cancer
    FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research .
    FR 901537
  • HY-161411
    α-Glucosidase-IN-60

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-60 (Compound 5k) exhibits a competitive inhibitory efficacy against α-Glucosidase, with IC50 of 10.8 μM .
    α-Glucosidase-IN-60
  • HY-146318
    MIF-IN-5

    		Macrophage migration inhibitory factor (MIF) Metabolic Disease Inflammation/Immunology Cancer
    MIF-IN-5 (compound 1d) is a potent and reversible macrophage migration inhibitory factor (MIF) competitive inhibitor with an IC50 of 4.8 μM and a Ki value of 3.3 μM, respectively .
    MIF-IN-5
  • HY-147879
    α-Glucosidase-IN-8

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-8 (Compound 4k) is a competitive α-glucosidase inhibitor with an IC50 of 0.18 µg/mL .
    α-Glucosidase-IN-8
  • HY-109079A
    Abeprazan hydrochloride

    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
    Abeprazan

    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-N2689
    (R)-6',7'-Dihydroxybergamottin

    (R)-6′,7′-DHB

    		 Cytochrome P450 Cancer
    (R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research .
    (R)-6',7'-Dihydroxybergamottin
  • HY-161299
    LAPTc-IN-1

    		Parasite Infection
    LAPTc-IN-1 (compound 4) is a competitive inhibitor targeting acidic M17 leucinopeptidase (LAPTc) with Ki=0.27 μM. LAPTc-IN-1 is a potential antagonist of the parasite Trypanosoma cruzi .
    LAPTc-IN-1
  • HY-149528
    MAO-B-IN-24

    		Monoamine Oxidase Cholinesterase (ChE) Cancer
    MAO-B-IN-24 (compound 11h) is a selective, reversible, competitive inhibitor of MAO-B (IC50: 1.60 μM). MAO-B-IN-24 also inhibited MAO-A (22.42 μM); at 10 μM concentration, it also reduced AChE and BChE activities to 54.58% and 88.43% .
    MAO-B-IN-24
  • HY-139145
    Etbicyphat

    Trimethylopropane phosphate

    		 GABA Receptor Neurological Disease
    Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
    Etbicyphat
  • HY-149527
    MAO-B-IN-23

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-23 (Compound 11f) is a reversible and competitive MAO-B inhibitor (IC50: 1.44 μM, Ki: 0.51 μM) .
    MAO-B-IN-23
  • HY-A0252
    Bupranolol

    		Adrenergic Receptor Inflammation/Immunology Cancer
    Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity .
    Bupranolol
  • HY-P1294
    α-Helical CRF(9-41)

    		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-12031
    U0126-EtOH
    330+ 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-19316
    NU2058

    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-P1294A
    α-Helical CRF(9-41) TFA

    		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-N2554
    Osthenol

    Ostenol

    		 Monoamine Oxidase Neurological Disease
    Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
    Osthenol
  • HY-119016
    SK1-I
    1 Publications Verification

    BML-258

    		 SphK 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-119016A
    SK1-​I hydrochloride
    1 Publications Verification

    BML-258 hydrochloride

    		 SphK Cancer
    SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity .
    SK1-​I hydrochloride
  • HY-151591
    SPAA-52

    		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-117043
    GRL0617
    5+ 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-B0334
    Sulbactam
    5+ 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-B0334A
    Sulbactam sodium
    5+ 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-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-112468
    PNU112455A hydrochloride

    		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-P0222A
    PKI(5-24) TFA

    		PKA Others
    PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
    PKI(5-24) TFA
  • HY-100414
    Soraprazan
    1 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-W013754
    S-Hexylglutathione

    		Others 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-113468A
    3-O-Methyldopa

    3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA

    		 Dopamine Receptor Endogenous Metabolite Neurological Disease
    3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine .
    3-O-Methyldopa
  • HY-110154
    NSC636819

    		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-14806
    Teneligliptin
    5+ Cited Publications

    MP-513

    		 Dipeptidyl Peptidase Metabolic Disease
    Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
    Teneligliptin
  • HY-13452
    CID-1067700
    5+ 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-10195
    Ruboxistaurin
    5+ 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-15067
    DNQX
    4 Publications Verification

    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-155374
    PP5-IN-1

    		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-10195A
    Ruboxistaurin mesylate
    5+ 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-103233
    DNQX disodium salt

    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-19435A
    GYKI-47261 dihydrochloride

    		iGluR Cytochrome P450 Neurological Disease
    GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1 .
    GYKI-47261 dihydrochloride
  • HY-124366
    Slingshot inhibitor D3

    		Others Infection Cancer
    Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
    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-149929
    EBL-3183

    		Beta-lactamase Bacterial Infection
    EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7 .
    EBL-3183

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