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

Cytochrome P450

CYPs

Cytochrome P450

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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.

Cytochrome P450 Isoform Specific Products:

Cytochrome P450 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-100238
    Antihistamine-1
    		Inhibitor 99.45%
    Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
    Antihistamine-1
  • 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-152118
    CYP1B1-IN-4
    		Inhibitor 99.09%
    CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes.
    CYP1B1-IN-4
  • 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-N1407
    Polygalaxanthone III
    		Inhibitor 99.76%
    Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
    Polygalaxanthone III
  • HY-151239
    ONT-993
    		Inhibitor 99.85%
    ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM).
    ONT-993
  • HY-W027773
    7-Methoxy-4-(trifluoromethyl)coumarin
    		≥98.0%
    7-Methoxy-4-(trifluoromethyl)coumarin (MFC) is a fluorescent substrate for cytochrome P450 and can quantify CYP activity.
    7-Methoxy-4-(trifluoromethyl)coumarin
  • 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-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-B0876A
    Fomepizole hydrochloride
    		Inhibitor 99.85%
    Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning.
    Fomepizole hydrochloride
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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