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-N1457
    Chrysosplenetin
    Inhibitor 99.68%
    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-17356R
    Fenofibrate (Standard)
    Inhibitor 99.91%
    Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate (Standard)
  • HY-116568
    Prothioconazole
    Inhibitor 99.52%
    Prothioconazole is a triazolinthione fungicide. Prothioconazole is a CYP51 inhibitor.
    Prothioconazole
  • HY-W010195
    2,6-Dimethylquinoline
    Inhibitor 99.95%
    2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM.
    2,6-Dimethylquinoline
  • 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-135334
    ACP-5862
    Inhibitor 98.41%
    ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
    ACP-5862
  • HY-101284
    DMU2105
    Inhibitor 99.54%
    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
    DMU2105
  • 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-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-B1184S1
    Mephenytoin-d5
    98.72%
    Mephenytoin-d5 is the deuterium labeled Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].
    Mephenytoin-d<sub>5</sub>
  • HY-103223
    Phortress
    Inducer 99.25%
    Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.
    Phortress
  • HY-70013S
    Abiraterone-d4
    Inhibitor ≥98.0%
    Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
    Abiraterone-d<sub>4</sub>
  • HY-127112
    Oleic acid alkyne
    99.96%
    Oleic acid alkyne is oleic acid with an acetylene group. The terminal alkyne group can be used for click chemical ligation reactions. Oleic acid can be hydroxylated by a microsomal cytochrome P-450-dependent system (ω-OAH). Through click chemistry reactions, fluorescent or biotin-labeled oleic acid can be introduced to analyze its metabolism and biological activity.
    Oleic acid alkyne
  • 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
  • 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-17508S
    Clarithromycin-13C,d3
    ≥99.0%
    Clarithromycin-13C,d3 is the deuterium and 13C labeled Clarithromycin[1].
    Clarithromycin-<sup>13</sup>C,d<sub>3</sub>
  • HY-17514S1
    Itraconazole-d3
    99.62%
    Itraconazole-d3 is the deuterium labeled Itraconazole (HY-17514)[1].
    Itraconazole-d<sub>3</sub>
  • HY-N3680
    Danshenxinkun A
    99.95%
    Danshenxinkun A is a natural compound that could be isolated from Tanshen and is used in the study for heart diseases.
    Danshenxinkun A
  • 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
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