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uncompetitive

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51

Inhibitors & Agonists

16

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-151813
    NNMT-IN-4

    		Others Cancer
    NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
    NNMT-IN-4
  • HY-N1882
    4,5-Dimethoxycanthin-6-one

    		Cytochrome P450 Metabolic Disease
    4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae) .
    4,5-Dimethoxycanthin-6-one
  • HY-19966
    K858 (Racemic)

    		Kinesin Apoptosis Cancer
    K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.
    K858 (Racemic)
  • HY-113568
    CAY10581

    		Indoleamine 2,3-Dioxygenase (IDO) Cancer
    CAY10581, a pyranonaphthoquinone derivative, is a highly specific and reversible uncompetitive IDO Inhibitor with an IC50 of 55 nM .
    CAY10581
  • HY-125969
    Rtt109 inhibitor 1

    		Histone Acetyltransferase Fungal Infection
    Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site .
    Rtt109 inhibitor 1
  • HY-150621
    AS1134900

    		Others Cancer
    AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor .
    AS1134900
  • HY-162474
    BZG2

    		SARS-CoV Virus Protease Infection
    BZG2 is an allosteric inhibitor for the SARS-CoV-2 main protease (M pro), with an IC50 of 77 µM .
    BZG2
  • HY-12058
    AZD8330
    5+ Cited Publications

    ARRY-424704; ARRY-704

    		 MEK Cancer
    AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
    AZD8330
  • HY-118994
    ARN19874

    		Phospholipase Neurological Disease
    ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor with an IC50 of ~34 μM .
    ARN19874
  • HY-N0430
    Coptisine

    Coptisin

    		 Indoleamine 2,3-Dioxygenase (IDO) Metabolic Disease Cancer
    Coptisine is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM.
    Coptisine
  • HY-158021
    Tyrosinase-IN-26

    		Tyrosinase Cancer
    Tyrosinase-IN-26 (compound 13) is a uncompetitive tyrosinase inhibitor with the an IC50 value of 68.86 µM. Tyrosinase-IN-26 can suppresses melanogenesis .
    Tyrosinase-IN-26
  • HY-N0430A
    Coptisine Sulfate
    3 Publications Verification

    		 Indoleamine 2,3-Dioxygenase (IDO) Metabolic Disease Cancer
    Coptisine Sulfate is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM .
    Coptisine Sulfate
  • HY-12989
    LDN-91946

    		Deubiquitinase Neurological Disease Cancer
    LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a Ki app of 2.8 μM .
    LDN-91946
  • HY-103081
    β-Glucuronidase-IN-1

    		Bacterial Infection Cancer
    β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively .
    β-Glucuronidase-IN-1
  • HY-151338
    AChE-IN-25

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-25 is a potent, selective and uncompetitive acetylcholinesterase (AChE) inhibitor (IC50=2.95 µM). AChE-IN-25 can be used in Alzheimer's disease research .
    AChE-IN-25
  • HY-147661
    DHFR-IN-2

    		Antifolate Infection
    DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research .
    DHFR-IN-2
  • HY-W013571
    4-Isopropylbenzoic acid

    		Fungal Infection
    4-Isopropylbenzoic acid, an aromatic monoterpenoid, is isolated from the stem bark of Bridelia retusa. 4-Isopropylbenzoic acid exhibits antifungal activities. 4-Isopropylbenzoic acid is also a reversible and uncompetitive inhibitor of mushroom tyrosinase .
    4-Isopropylbenzoic acid
  • HY-15587
    L82

    		DNA/RNA Synthesis Cancer
    L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
    L82
  • HY-B0421
    Mycophenolic acid
    5+ Cited Publications

    Mycophenolate

    		 Dengue virus Apoptosis Bacterial Fungal Endogenous Metabolite Antibiotic Flavivirus Infection Inflammation/Immunology Cancer
    Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects .
    Mycophenolic acid
  • HY-B0421A
    Mycophenolic acid sodium

    Mycophenolate sodium

    		 Dengue virus Apoptosis Bacterial Fungal Antibiotic Endogenous Metabolite Flavivirus Infection Inflammation/Immunology Cancer
    Mycophenolic acid sodium is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid sodium is an immunosuppressive agent. Antiangiogenic and antitumor effects .
    Mycophenolic acid sodium
  • HY-147216A
    AXKO-0046 dihydrochloride
    2 Publications Verification

    		 Lactate Dehydrogenase Metabolic Disease Inflammation/Immunology Cancer
    AXKO-0046 dihydrochloride, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor. AXKO-0046 dihydrochloride has LDHB inhibitory activity with an EC50 value of 42 nM. AXKO-0046 dihydrochloride can be used for the research of cancer metabolism .
    AXKO-0046 dihydrochloride
  • HY-107695
    Remacemide hydrochloride

    FPL 12924AA

    		 iGluR Sodium Channel Neurological Disease
    Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na + channel, is a weak uncompetitive NMDA receptor antagonist with IC50s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively . Remacemide hydrochloride is an anticonvulsant agent .
    Remacemide hydrochloride
  • HY-147216
    AXKO-0046
    2 Publications Verification

    		 Lactate Dehydrogenase Cancer
    AXKO-0046, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor.AXKO-0046 has LDHB inhibitory activity with an EC50 value of 42 nM.AXKO-0046 can be used for the research of cancer metabolism .
    AXKO-0046
  • HY-155238
    E2730

    		GABA Receptor Neurological Disease
    E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
    E2730
  • HY-106408A
    Nelonemdaz potassium

    Salfaprodil; Neu2000 potassium

    		 iGluR Neurological Disease
    Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death .
    Nelonemdaz potassium
  • HY-146588
    NMDA receptor antagonist 4

    		iGluR Neurological Disease
    NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease .
    NMDA receptor antagonist 4
  • HY-112711
    LV-320

    		Atg4 Autophagy Cathepsin Cancer
    LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo .
    LV-320
  • HY-16946
    CP-610431

    		Acetyl-CoA Carboxylase Metabolic Disease
    CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome .
    CP-610431
  • HY-106408
    Nelonemdaz

    Salfaprodil free base; Neu2000

    		 iGluR Neurological Disease
    Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death .
    Nelonemdaz
  • HY-N7389B
    GDP-α-D-mannose disodium

    		Endogenous Metabolite Metabolic Disease
    GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
    GDP-α-D-mannose disodium
  • HY-N7389A
    GDP-D-mannose disodium

    		Endogenous Metabolite Metabolic Disease
    GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
    GDP-D-mannose disodium
  • HY-107385
    Epristeride

    ONO-9302; SKF105657

    		 5 alpha Reductase Cancer
    Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
    Epristeride
  • HY-150504
    ERAP2-IN-1

    		Others Inflammation/Immunology
    ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC50 of 27 μM and model peptide hydrolysis with an IC50 of 44 μM .
    ERAP2-IN-1
  • HY-146668
    AChE/BChE-IN-8

    		Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity .
    AChE/BChE-IN-8
  • HY-147328
    LCS3

    		Apoptosis Cancer
    LCS3 is a reversible and uncompetitive glutathione disulfide reductase (GSR) and thioredoxin reductase 1 (TXNRD1) inhibitor (IC50=3.3 µM and 3.8 µM, respectively). LCS3 shows anti-tumor activity, and induces apoptosis. LCS3 can be used in lung adenocarcinoma (LUAD) research .
    LCS3
  • HY-N0736
    Coptisine chloride
    5+ Cited Publications

    		 Indoleamine 2,3-Dioxygenase (IDO) Bacterial Influenza Virus Infection Metabolic Disease Cancer
    Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM. Coptisine chloride is a potent H1N1 neuraminidase (NA-1) inhibitor with an IC50 of 104.6 μg/mL and can be used for influenza A (H1N1) infection.
    Coptisine chloride
  • HY-15610
    GDC-0623
    5+ Cited Publications

    RG 7421; MEK inhibitor 1

    		 MEK Apoptosis Cancer
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
    GDC-0623
  • HY-N7683
    Prunetin 5-O-β-D-glucopyranoside

    		Glucosidase Metabolic Disease
    Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes .
    Prunetin 5-O-β-D-glucopyranoside
  • HY-144778
    IDO1/TDO-IN-1

    		Indoleamine 2,3-Dioxygenase (IDO) Apoptosis Bcl-2 Family Cancer
    IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
    IDO1/TDO-IN-1
  • HY-148161
    L82-G17

    		DNA/RNA Synthesis Cancer
    L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity .
    L82-G17
  • HY-N1457
    Chrysosplenetin

    		P-glycoprotein Cytochrome P450 Ferroptosis Metabolic Disease
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .
    Chrysosplenetin
  • HY-107385R
    Epristeride (Standard)

    		5 alpha Reductase Cancer
    Epristeride (Standard) is the analytical standard of Epristeride. This product is intended for research and analytical applications. Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
    Epristeride (Standard)
  • HY-116866
    Sclerotiorin

    		Lipoxygenase Fungal Infection Inflammation/Immunology
    Sclerotiorin is a reversible and uncompetitive inhibitor against soybean lipoxygenase-1 (LOX-1) (IC50: 4.2 μM). Sclerotiorin also shows antioxidant activity by scavenging free radical (ED50: 0.12 μM), and nonenzymatic lipid peroxidation inhibition activity. Sclerotiorin has antifungal activity, and also inhibits platelet aggregation. Sclerotiorin can be purified from the fermented broth of Penicillium frequentans .
    Sclerotiorin
  • HY-B0421S2
    Mycophenolic acid-13C17

    Mycophenolate-13C17

    		 Isotope-Labeled Compounds Flavivirus Cancer
    Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
    Mycophenolic acid-13C17
  • HY-128717
    GSK3368715

    EPZ019997

    		 Histone Methyltransferase Cancer
    GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
    GSK3368715
  • HY-128717A
    GSK3368715 dihydrochloride
    Maximum Cited Publications
    11 Publications Verification

    EPZ019997 dihydrochloride

    		 Histone Methyltransferase Cancer
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
    GSK3368715 dihydrochloride
  • HY-128717B
    GSK3368715 trihydrochloride

    EPZ019997 trihydrochloride

    		 Histone Methyltransferase Cancer
    GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
    GSK3368715 trihydrochloride
  • HY-N0110
    Palmatine chloride
    5+ Cited Publications

    		 Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .
    Palmatine chloride
  • HY-N0110A
    Palmatine

    		Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Palmatine is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .
    Palmatine
  • HY-N0110B
    Palmatine hydroxide
    5+ Cited Publications

    		 Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .
    Palmatine hydroxide

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