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-75054S
    Abiraterone acetate-d4
    		Inhibitor
    Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. 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-d<sub>4</sub>
  • HY-159585
    CYP51-IN-20
    		Inhibitor
    CYP51-IN-20 (compound 5b) is an inhibitor of CYP51 and has antifungal activity. CYP51-IN-20 has a significant inhibitory effect on Candida albicans ATCC 10231, downregulates ERG11 (Cyp51) gene expression, and significantly reduces the yeast-to-hyphae morphological transition. CYP51-IN-20 can synergize with Voriconazole (HY-76200) to occupy the entire CYP51 binding site and exert a synergistic inhibitory effect in the Glechoma moth model.
    CYP51-IN-20
  • HY-105114
    Imitrodast
    		Inhibitor
    Imitrodast is an inhibitor of thromboxane synthase. Imitrodast can be used in the research of bronchoconstriction.
    Imitrodast
  • HY-E70493
    Human CYP3A5,High-Reductase +b5
    Human CYP3A5, High-Reductase +b5, a recombinant CYP3A5, is a member of the CYP enzyme family. CYP3A5 is mainly expressed in the prostate and the liver.
    Human CYP3A5,High-Reductase +b5
  • HY-149977
    Anticancer agent 111
    		Inhibitor
    Anticancer agent 111 (compound 11) is a potent cytochrome P450 inhibitor with an IC50 value of 3 μM for CYP3A4. Anticancer agent 111 has anticancer activity. Anticancer agent 111 can be used in research of cancer.
    Anticancer agent 111
  • HY-130139
    11,12-DiHETE
    11,12-DiHETE is an orally active metabolite produced by cytochrome p450 mediated epoxide formation and subsequent epoxide hydrolase production.
    11,12-DiHETE
  • HY-116050A
    17(R)-HETE
    17R-HETE is an arachidonic acid metabolite through cytochrome P-450 pathways. 17R-HETE exhibits efficacy in inducing cardic hypertrophy with less efficiency with compared to 17S-HETE.
    17(R)-HETE
  • HY-161403
    CYP1B1-IN-8
    		Inhibitor
    CYP1B1-IN-8 (Compound 14b) is a CYP1B1 inhibitor (IC50: 4.14 × 10–5 nM). CYP1B1-IN-8 reduces the resistance in A549 cells to Paclitaxel (HY-B0015), and inhibits cell migration and invasion.
    CYP1B1-IN-8
  • HY-B0725R
    Doxepin (Hydrochloride) (Standard)
    		Inhibitor
    Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
    . Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system.
    . Doxepin has also been proposed as a protective factor against oxidative stress.
    .
    Doxepin (Hydrochloride) (Standard)
  • HY-10672
    Urotensin-II receptor antagonist-1
    		Inhibitor
    Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM).
    Urotensin-II receptor antagonist-1
  • HY-B1751E
    Quinidine polygalacturonate
    		Inhibitor
    Quinidine polygalacturonate is an antiarrhythmic agent. Quinidine polygalacturonate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine polygalacturonate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine polygalacturonate can be used for malaria research.
    Quinidine polygalacturonate
  • HY-G0024A
    Vildagliptin carboxylic acid metabolite TFA
    		Inhibitor
    Vildagliptin carboxylic acid metabolite (M20.7) TFA is a potent P450 enzyme activity inhibitor.
    Vildagliptin carboxylic acid metabolite TFA
  • HY-162738
    JMV6944
    		Inducer
    JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC50 of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704).
    JMV6944
  • HY-14225
    BMS-764459
    		Inducer
    BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer.
    BMS-764459
  • HY-E70510
    Human CYP46A1,Low-Reductase
    Human CYP46A1, Low-Reductase, a recombinant CYP46A1, is a member of the CYP enzyme family. CYP46A1 is expressed mainly in brain neurons and is responsible for brain cholesterol homeostasis by regulating the cholesterol efflux.
    Human CYP46A1,Low-Reductase
  • HY-164457
    ASN-001
    		Inhibitor
    ASN-001 is an orally active CYP-17A1 lyase inhibitor that selectively inhibits testosterone synthesis. ASN-001 has anticancer activity and can be used for research in the field of prostate cancer.
    ASN-001
  • HY-E70475
    Human CYP2C18,Low-Reductase
    Human CYP2C18, Low-Reductase, a recombinant CYP2C18, is a member of the CYP enzyme family and is involved in the metabolism of xenobiotics in the body.
    Human CYP2C18,Low-Reductase
  • HY-E70489
    Human CYP4A11,High-Reductase+b5
    Human CYP4A11, High-Reductase+b5, a recombinant CYP4A11, is a member of the CYP4 enzyme family and is involved in the metabolism of medium- and long-chain fatty acids. Human CYP4A11, High-Reductase+b5 primarily metabolizes endobiotics and catalyzes the ω-hydroxylation of fatty acids in human liver and kidney tissues.
    Human CYP4A11,High-Reductase+b5
  • HY-172783
    Aromatase-IN-5
    		Inhibitor
    Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. Aromatase-IN-5 effectively blocks estrogen production. Aromatase-IN-5 inhibits the proliferation of breast cancer cell lines like MCF-7, arrests the cell cycle at the G1 phase, and induces apoptosis. Aromatase-IN-5 is promising for research of breast cancer.
    Aromatase-IN-5
  • HY-163571
    CYP51-IN-17
    		Inhibitor
    CYP51-IN-17 (compound 7a) is a potent CYP51 inhibitor with an IC50 of 0.377 μg/mL. CYP51-IN-17 shows significant fungicidal activity against B. cinerea with an EC50 of 0.326 μg/mL.
    CYP51-IN-17
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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