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uncompetitive

" in MedChemExpress (MCE) Product Catalog:

59

Inhibitors & Agonists

19

Natural
Products

2

Isotope-Labeled Compounds

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

    		Fluorescent Dye Cancer
    NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
    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-150621
    AS1134900

    		β-catenin Wnt Cancer
    AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor .
    AS1134900
  • 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-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-161761
    Urease-IN-15

    		Bacterial Infection
    Urease-IN-15 (compound 5g) is an uncompetitive inhibitor of urease in manner with the IC50 of 3.80 µM .
    Urease-IN-15
  • HY-141555
    5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione

    		Phosphodiesterase (PDE) Tyrosinase Others
    5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione is a weak inhibitor for snake venom and human recombinant phosphodiesterase 1 with IC50 of 429 and 467 μM. 5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione inhibits mushroom tyrosinase weakly, with Ki of 1.9 μM .
    5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione
  • 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-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
    5+ Cited Publications

    		 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-103081
    β-Glucuronidase-IN-1

    		β-glucuronidase 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-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-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-170608
    Urease-IN-18

    		Bacterial Infection
    Urease-IN-18 (compound 13a) is an uncompetitive urease inhibitor with an IC50 value of 1.6 μM. Urease helps maintain an alkaline environment favorable for the survival and proliferation of specific pathogens within the host .
    Urease-IN-18
  • 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-147216A
    AXKO-0046 dihydrochloride
    4 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-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
    5+ Cited Publications

    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-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-W013571
    4-Isopropylbenzoic acid

    Cuminic acid; p-Isopropyl benzoic acid

    		 Fungal Infection
    4-Isopropylbenzoic acid (Cuminic acid; p-Isopropyl benzoic 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-147216
    AXKO-0046
    4 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-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-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-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-B0365AS
    Memantine-d6 hydrochloride

    		Cytochrome P450 iGluR Autophagy Neurological Disease
    Memantine-d6 (hydrochloride) is the deuterium labeled Memantine hydrochloride. 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[1].
    Memantine-d6 hydrochloride
  • 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-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-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-107385
    Epristeride
    1 Publications Verification

    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

    		Aminopeptidase 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-B0421R
    Mycophenolic acid (Standard)

    		Dengue Virus Apoptosis Bacterial Fungal Endogenous Metabolite Antibiotic Flavivirus Infection Inflammation/Immunology Cancer
    Mycophenolic acid (Standard) is the analytical standard of Mycophenolic acid. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0421AR
    Mycophenolic acid (sodium) (Standard)

    		Dengue Virus Apoptosis Bacterial Fungal Antibiotic Endogenous Metabolite Flavivirus Infection Inflammation/Immunology Cancer
    Mycophenolic acid (sodium) (Standard) is the analytical standard of Mycophenolic acid (sodium). This product is intended for research and analytical applications. 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) (Standard)
  • 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-N7683
    Prunetin 5-O-β-D-glucopyranoside

    		Glycosidase 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-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-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-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-123914
    P516-0475

    		Bacterial Infection
    P516-0475 is an uncompetitive inhibitor against endopeptidase PepO. P516-0475 is also an agonist of the Rgg2/3 system with antibacterial activity. P516-0475 induces expression of Rgg2/3-regulated genes in the presence of short hydrophobic pheromone (SHP) for activity and leads to positive modulation of lysozyme resistance .
    P516-0475
  • 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

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