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

Cytochrome P450

CYPs

Cytochrome P450

Related Products

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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-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-B2169
    Melperone
    		Inhibitor 99.24%
    Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone
  • 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-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-101217
    BI 689648
    		Inhibitor 99.20%
    BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
    BI 689648
  • 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
  • HY-B0258S
    Gemfibrozil-d6
    		Inhibitor 98.00%
    Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
    Gemfibrozil-d<sub>6</sub>
  • 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-156883
    Dasatinib analog-1
    		Inhibitor 98.08%
    Dasatinib analog-1 (compound 5826) inhibits CYP3A4 viability with a Ki value of 5.4 μM. Dasatinib analog-1 blocks the formation of glutathione adducts.
    Dasatinib analog-1
  • 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-13632R
    Exemestane (Standard)
    		Inhibitor 99.63%
    Exemestane (Standard) is the analytical standard of Exemestane. This product is intended for research and analytical applications. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
    Exemestane (Standard)
  • HY-75054R
    Abiraterone acetate (Standard)
    		Inhibitor 99.85%
    Abiraterone acetate (Standard) is the analytical standard of Abiraterone acetate. This product is intended for research and analytical applications. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
    Abiraterone acetate (Standard)
  • HY-B0105S1
    Ketoconazole-d4
    		Inhibitor ≥98.0%
    Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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