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Noncompetitive inhibition

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

6

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N3394
    Lecanoric acid

    		Others Infection
    Lecanoric acid is a histidine-decarboxylase inhibitor isolated from fungus. The inhibition by lecanoric acid is competitive with histidineand noncompetitive with pyridoxal phosphate. Lecanoric acid did not inhibit aromatic amino acid decarboxylase .
    Lecanoric acid
  • HY-120566
    PSB-16131

    		NTPDase Neurological Disease Inflammation/Immunology Cancer
    PSB-16131 is a potent inhibitor of human NTPDase2, showing non-competitive inhibition with an IC50 of 539 nM. PSB-16131 can be used in the study of inflammation, neurodegenerative diseases and cancer .
    PSB-16131
  • HY-103562
    DMeOB

    3,3'-Dimethoxybenzaldazine

    		 mGluR Neurological Disease
    DMeOB (3,3'-Dimethoxybenzaldazine) is a mGluR5 receptor negative allosteric modulator with an IC50 of 3 μM. DMeOB displays reversible non-competitive inhibition of mGlu5-mediated responses .
    DMeOB
  • HY-122142
    Pyr-​Pro-​Arg-​pNA

    S-2366

    		 APC Factor XI Biochemical Assay Reagents Others
    Pyr-Pro-Arg-pNA (S2366) is a chromogenic peptide substrate for Factor XI and Activated protein C (APC). Pyr-Pro-Arg-pNA can induce noncompetitive inhibition of factor XI activation through occupancy of the active site of the factor XIa-light chain. Pyr-Pro-Arg-pNA can be used for measurement of APC amidolytic activity .
    Pyr-​Pro-​Arg-​pNA
  • HY-N12427
    Litchinol B

    		Tyrosinase Cancer
    Litchinol B (compound 2) is a non-competitive tyrosinase inhibitor with an inhibition constant of 5.70 μM .
    Litchinol B
  • HY-139158
    Ainuovirine

    		HIV Infection
    Ainuovirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). Ainuovirine inhibits HIV replication by non-competitively binding to HIV reverse transcriptase and blocking the reverse transcription process of viral RNA. Ainuovirine can be used for human immunodeficiency virus (HIV) type 1 infection .
    Ainuovirine
  • HY-N3136
    Onitin

    		Histamine Receptor Others
    Onitin is a natural product, that can be isolated from Onychium siliculosum. Onitin is also a non-competitive antagonist of histamine. Onitin shows activity in blocking the peristaltic reflex of the guinea-pig ileum, in inhibition of the responses of guinea-pig ileum to histamine and of inhibition of the responses of guinea-pig tracheal muscle to histamine .
    Onitin
  • HY-148545
    SHMT-IN-3

    		SHMT Cancer
    SHMT-IN-3 (Hit 1) is a SHMT1 and SHMT2 inhibitor with an IC50 of 0.53 µM for human SHMT1. SHMT-IN-3 exhibits noncompetitive inhibition against serine .
    SHMT-IN-3
  • HY-101370
    2-Methylthio-ATP tetrasodium

    		P2X Receptor Metabolic Disease
    2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation .
    2-Methylthio-ATP tetrasodium
  • HY-B0690
    Fosinopril

    SQ28555 free acid

    		 Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Fosinopril (SQ28555 free acid) is the ester proagent of angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an Ki value of 1.675 μM .
    Fosinopril
  • HY-15185
    Nirogacestat
    Maximum Cited Publications
    15 Publications Verification

    PF-3084014

    		 γ-secretase Apoptosis Cancer
    Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
    Nirogacestat
  • HY-146142
    AChE/BuChE-IN-2

    		Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB .
    AChE/BuChE-IN-2
  • HY-15185B
    Nirogacestat dihydrobromide
    Maximum Cited Publications
    15 Publications Verification

    PF-3084014 dihydrobromide; PF-03084014 dihydrobromide

    		 γ-secretase Apoptosis Cancer
    Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
    Nirogacestat dihydrobromide
  • HY-121787
    OX1a

    OLC20

    		 Olfactory Receptor Others
    OX1a (OLC20) is an Orco antagonist with non-competitive activity that inhibits the activation of oxygen odor receptors (ORs). OX1a is able to reduce the activation of ORs by competitively inhibiting the effects of Orco agonists. OX1a also shows non-competitive inhibition of odor molecules, which may affect the olfactory-mediated behavior of insects. Through structural optimization, OX1a analogs have shown higher antagonistic potency, indicating that this type of compound may have application potential in a wide range of insect species .
    OX1a
  • HY-13965
    Parmodulin 2
    3 Publications Verification

    ML161

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM . Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo .
    Parmodulin 2
  • HY-N13917
    Argyrin B

    		Proteasome Bacterial Infection Cancer
    Argyrin B, a natural product cyclic peptide, is a reversible, non-competitive immunoproteasome inhibitor. Argyrin B shows selective inhibition of the β5i and β1i sites of the immunoproteasome over the β5c and β1c sites of the constitutive proteasome with nearly 20-fold selective inhibition of β1i over the homologous β1c. Argyrin B has antibacterial effects .
    Argyrin B
  • HY-15185R
    Nirogacestat (Standard)

    		γ-secretase Apoptosis Cancer
    Nirogacestat (Standard) is the analytical standard of Nirogacestat. This product is intended for research and analytical applications. Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
    Nirogacestat (Standard)
  • HY-10572A
    (R)-Efavirenz

    (R)-DMP 266; (R)-EFV; (R)-L-743726

    		 Reverse Transcriptase Infection
    (R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
    (R)-Efavirenz
  • HY-B0690S
    Fosinopril-d5

    SQ28555-d5 free acid

    		 Isotope-Labeled Compounds Apoptosis Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Fosinopril-d5 (SQ28555-d5 (free acid)) is deuterium labeled Fosinopril. Fosinopril (SQ28555 free acid) is the ester proagent of angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an Ki value of 1.675 μM .
    Fosinopril-d5
  • HY-162073
    ZIKV-IN-8

    		Influenza Virus Infection
    ZIKV-IN-8 (Compound 9b) is a noncompetitive Zika virus (ZIKV) inhibitor. ZIKV-IN-8 shows the best anti-ZIKV activity with a selectivity index of 22.4. ZIKV-IN-8 has significant inhibition of ZIKV with an IC50 value of 25.6 μM. ZIKV-IN-8 can be used for the research of ZIKV infection .
    ZIKV-IN-8
  • HY-117769
    GSK837149A

    		Fatty Acid Synthase (FASN) Metabolic Disease
    GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .
    GSK837149A
  • HY-W719041
    1,6-Di-O-galloyl-β-D-glucose

    		HIV Reverse Transcriptase Infection
    1,6-Di-O-galloyl-β-D-glucose is a compound found in the fruit of Phyllanthus emblica. 1,6-Di-O-galloyl-β-D-glucose has HIV-1 reverse transcriptase (RT) inhibitory activity with an IC50 value of 270 μM. The inhibitory mechanism of 1,6-Di-O-galloyl-β-D-glucose is competitive inhibition of the template primer and non-competitive inhibition of the substrate (dTTP). 1,6-Di-O-galloyl-β-D-glucose can be used in anti-HIV research .
    1,6-Di-O-galloyl-β-D-glucose
  • HY-144267
    Glucosylceramide synthase-IN-2

    		Glucosylceramide Synthase (GCS) Neurological Disease Metabolic Disease
    Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research .
    Glucosylceramide synthase-IN-2
  • HY-116973
    L 738372

    		HIV Infection
    L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
    L 738372
  • HY-118061
    VCC234718

    		Bacterial Infection
    VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
    VCC234718
  • HY-156078
    α-Glucosidase-IN-32

    		Glycosidase Metabolic Disease
    α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
    α-Glucosidase-IN-32
  • HY-N7536
    Voacangine

    		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-150260
    SA09-Cu

    		Bacterial Infection
    SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance .
    SA09-Cu
  • HY-403733A
    (–)-JJ-450

    		Androgen Receptor Cancer
    (-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
    (–)-JJ-450
  • HY-12031B
    (2Z,3Z)-U0126

    		MEK Inflammation/Immunology
    (2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
    (2Z,3Z)-U0126
  • 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-162633
    USP1-IN-9

    		Deubiquitinase Cancer
    USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
    USP1-IN-9
  • HY-W015490R
    1,4-Naphthoquinone (Standard)

    		DNA/RNA Synthesis NF-κB Monoamine Oxidase TNF Receptor Bacterial Infection Inflammation/Immunology Cancer
    1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
    1,4-Naphthoquinone (Standard)
  • HY-W015490
    1,4-Naphthoquinone
    3 Publications Verification

    		 DNA/RNA Synthesis NF-κB Monoamine Oxidase TNF Receptor Bacterial Infection Inflammation/Immunology Cancer
    1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
    1,4-Naphthoquinone
  • HY-W015490S
    1,4-Naphthoquinone-d6

    		Isotope-Labeled Compounds DNA/RNA Synthesis NF-κB Monoamine Oxidase TNF Receptor Bacterial Infection Inflammation/Immunology Cancer
    1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone. 1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
    1,4-Naphthoquinone-d6

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