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-163436
    F44-A13
    Inducer
    F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.
    F44-A13
  • HY-17514S1
    Itraconazole-d3
    99.62%
    Itraconazole-d3 is the deuterium labeled Itraconazole (HY-17514)[1].
    Itraconazole-d<sub>3</sub>
  • HY-109619
    D4-abiraterone
    Inhibitor 99.75%
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
    D4-abiraterone
  • 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-144652
    IDO1-IN-19
    Inhibitor 98.52%
    IDO1-IN-19 (Compound 17) is an orally active IDO1 inhibitor with an IC50 of CYP2C9 of 8.64 μM. IDO1-IN-19 also acts funciton on cardiac channels, with IC50s of 12 μM (IKr), 40 μM (INa), 8.3 μM (ICa), respectively. IDO1-IN-19 has the potential to study cancer diseases.
    IDO1-IN-19
  • HY-106019C
    Liarozole dihydrochloride
    Inhibitor ≥99.0%
    Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.
    Liarozole dihydrochloride
  • HY-N2372
    Fraxinol
    Inhibitor 99.83%
    Fraxinol is isolated from Lobelia chinensis.
    Fraxinol
  • HY-N1993
    5-Methyl-7-methoxyisoflavone
    Inhibitor 99.78%
    5-Methyl-7-methoxyisoflavone is an orally active anti-oxidant with remyelinating activity. 5-Methyl-7-methoxyisoflavone inhibits the enzyme aromatase, interfering with the normal metabolic pathways of testosterone. 5-Methyl-7-methoxyisoflavone is a non-steroidal anabolic isoflavone, used as a anabolic agent. 5-Methyl-7-methoxyisoflavone shows better potency increasing muscle mass and endurance than Ipriflavone (HY-N0094). 5-Methyl-7-methoxyisoflavone can be used for fat loss besides the maintenance of low cholesterol level and strengthen bones.
    5-Methyl-7-methoxyisoflavone
  • HY-164793
    TGFBR1-IN-2
    Modulator
    TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.
    TGFBR1-IN-2
  • 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-10505
    Orteronel
    Inhibitor 99.70%
    Orteronel (TAK-700) is a highly selective?inhibitor of human?17,20-lyase (CYP17) with?IC50?of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4.
    Orteronel
  • HY-12946
    BI 653048
    Inhibitor 99.84%
    BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
    BI 653048
  • HY-101285
    DMU2139
    Inhibitor ≥98.0%
    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
    DMU2139
  • HY-130606
    Nampt-IN-5
    Inhibitor 98.02%
    Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
    Nampt-IN-5
  • HY-128859
    EMT inhibitor-2
    Inhibitor 99.55%
    EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
    EMT inhibitor-2
  • HY-B1751B
    Quinine sulfate
    Inhibitor
    Quinidine sulfate is an antiarrhythmic agent. Quinidine sulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine sulfate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine sulfate can be used for malaria research.
    Quinine sulfate
  • HY-156530
    CYP11A1-IN-1
    Inhibitor 99.64%
    CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1, with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.
    CYP11A1-IN-1
  • HY-112690A
    Pradefovir mesylate
    99.89%
    Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
    Pradefovir mesylate
  • 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 99.9%
    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
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