1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-122277
    1'-Hydroxy bufuralol
    1'-Hydroxy bufuralol, the main metabolite of bufuralol, can reflect CYP2D activity.
    1'-Hydroxy bufuralol
  • HY-116214
    Cyprodinil
    Inducer 99.25%
    Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil
  • HY-D0932
    Sudan IV
    Activator 98.0%
    Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.
    Sudan IV
  • HY-W006230
    Anthraflavic acid
    Inhibitor 99.51%
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
    Anthraflavic acid
  • HY-N1201R
    Apigenin (Standard)
    Inhibitor
    Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
    Apigenin (Standard)
  • HY-B1462R
    Chlorzoxazone (Standard)
    Modulator
    Chlorzoxazone (Standard) is the analytical standard of Chlorzoxazone. This product is intended for research and analytical applications.
    Chlorzoxazone (Standard)
  • HY-D0149
    4-(Trifluoromethyl)umbelliferone
    98.69%
    4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes.
    4-(Trifluoromethyl)umbelliferone
  • HY-B0105A
    (+)-Ketoconazole
    Inhibitor 99.79%
    (+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
    (+)-Ketoconazole
  • HY-B2015
    Carbosulfan
    Inhibitor 98.0%
    Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers).
    Carbosulfan
  • HY-113062
    20α-Dihydroprogesterone
    Inhibitor
    20α-Dihydroprogesterone is the metabolite of Progesterone (HY-N0437). 20α-Dihydroprogesterone inhibits cell proliferation and migration in breast tissue. 20α-Dihydroprogesterone inhibits aromatase in cell MCF-7aro with IC50 about 5 μM.
    20α-Dihydroprogesterone
  • HY-16718
    Dagrocorat
    Inhibitor 99.90%
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.
    Dagrocorat
  • HY-12035
    AMG-208
    Inhibitor 99.86%
    AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity.
    AMG-208
  • HY-134988
    EDP-305
    Inhibitor
    EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.
    EDP-305
  • HY-N7136
    α-​Terpinyl acetate
    Inhibitor
    α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
    α-​Terpinyl acetate
  • HY-18063
    ML252
    Inhibitor 99.65%
    ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant .
    ML252
  • HY-150775
    CYP19A1-IN-2
    Inhibitor 98.88%
    CYP19A1-IN-2 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). CYP19A1-IN-2 has potential for breast cancer research. CYP19A1-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CYP19A1-IN-2
  • HY-W392925
    (R)-(+)-Aminoglutethimide
    Inhibitor
    (R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer.
    (R)-(+)-Aminoglutethimide
  • HY-A0296
    Chlormethiazole hydrochloride
    Inhibitor 99.94%
    Clomethiazole hydrochloride is a potent and orally active GABAA agonist. Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Chlormethiazole hydrochloride
  • HY-B0859
    MCPA
    Activator 98.17%
    MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds.
    MCPA
  • HY-131452
    1-Ethynylpyrene
    Inhibitor
    1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC50s of 0.18, 0.32, and 0.04 μM, respectively. 1-Ethynylpyrene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    1-Ethynylpyrene
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