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-Y1155S
    Hexamethylphosphoramide-d18
    Hexamethylphosphoramide-d18 is the deuterium labeled Hexamethylphosphoramide (HY-Y1155). Hexamethylphosphoramide is an orally active polar aprotic solvent, flame retardant additive, and carcinogen. Hexamethylphosphoramide undergoes cytochrome P-450-mediated N-demethylation to Formaldehyde. Hexamethylphosphoramide induces DNA-protein crosslinks. Hexamethylphosphoramide has been linked to nasal tumors (squamous cell carcinoma, adenoid squamous cell carcinoma), squamous metaplasia, rhinitis, tracheitis, and reversible and irreversible infertility.
    Hexamethylphosphoramide-d<sub>18</sub>
  • HY-14405
    Casopitant
    		Inhibitor
    Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant
  • HY-162105
    Aromatase-IN-3
    		Inhibitor
    Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research.
    Aromatase-IN-3
  • HY-N10421
    Dihydrocubebin
    		Inhibitor
    Dihydrocubebin is a compound isolated from Piper cubeba as potent and selective inhibitors against cytochrome P450 3A4 (CYP3A4).
    Dihydrocubebin
  • HY-N12196
    Terretonin
    Terretonin is a fungal terpenoid isolated from Aspergillus terreus. The complete biosynthetic pathway of terretonin includes: cytochrome P450 Trt6 catalyzes the oxidation of terrenoid to obtain an unstable intermediate; then it is catalyzed by isomerase Trt14 and processed by non-heme iron-dependent dioxygenase Trt7 to complete the biosynthesis of terretonin.
    Terretonin
  • HY-10575
    MK-5596
    		Inhibitor
    MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.
    MK-5596
  • HY-179011
    CYP3A4-IN-6
    		Inhibitor
    CYP3A4-IN-6 (Compound 8a) is a CYP3A4 inhibitor with tissue-selective metabolism. CYP3A4-IN-6 remains stable in the intestinal S9 component but is rapidly metabolized in the liver S9 component, forming a less active metabolite. CYP3A4-IN-6 can be used for intestinal selectivity studies.
    CYP3A4-IN-6
  • HY-19377
    SS-750
    		Ligand
    SS-750 is an orally active Triazole derivative and antifungal agent. SS-750 binds to fungal cytochrome P450. SS-750 shows antifungal activities against Candida species and C. neoformans strains tested. SS750 shows MIC90 values of 0.25, 1, and 2 μg/mL against Candida parapsilosis, C. krusei, and C. glabrata, respectively. SS-750 improves systemic and pulmonary candidiasis caused by C. albicans.
    SS-750
  • HY-W008003R
    2-Hydroxybenzimidazole (Standard)
    		Control
    2-Hydroxybenzimidazole (Standard) is the analytical standard of 2-Hydroxybenzimidazole. This product is intended for research and analytical applications. 2-Hydroxybenzimidazole is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    2-Hydroxybenzimidazole (Standard)
  • HY-N16478
    Echihumiline
    		Substrate
    Echihumiline is an alkaloid targeting hepatic cytochrome P450 enzymes (CYP450). Echihumiline induces DNA cross-linking and oxidative stress in hepatocytes, leading to liver necrosis and fibrosis. Echihumiline is promising for research of liver diseases.
    Echihumiline
  • HY-182284
    Anticancer agent 310
    		Modulator
    Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP+ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric cancer.
    Anticancer agent 310
  • HY-158328A
    CA IX/VEGFR-2-IN-2
    		Activator
    CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) .
    CA IX/VEGFR-2-IN-2
  • HY-N6748S
    Roquefortine C-13C22
    Roquefortine C-13C22 is the 13C-labeled Roquefortine C (HY-N6748). Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of P-gp and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity.
    Roquefortine C-<sup>13</sup>C<sub>22</sub>
  • HY-N18161
    Isopsoralidin
    		Inhibitor
    Isopsoralidin is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential hepatotoxicity and CYP2D6 inhibitory activity.
    Isopsoralidin
  • HY-12946A
    BI 653048 phosphate
    		Inhibitor
    BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate 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 phosphate
  • HY-155061
    hCYP1B1-IN-1
    		Inhibitor
    hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM)，as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells.
    hCYP1B1-IN-1
  • HY-116444
    16(S)-HETE
    		Activator
    16(S)-HETE is an endogenous inhibitor of neutrophil activity and can be used in the study of acute ischemic brain injury.
    16(S)-HETE
  • HY-174377
    PeS-9
    		Activator

    PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.
    PeS-9
  • HY-13600S1
    Clobetasol propionate-d5
    		Inhibitor
    Clobetasol propionate-d5 is a deuterium substitute of Clobetasol propionate. Clobetasol propionate is a potent, selective CYP3A5 inhibitor with a IC50 of 0.206 μM and has potential for use in the study of psoriasis and other skin diseases.
    Clobetasol propionate-d<sub>5</sub>
  • HY-13762
    Tesmilifene
    		Modulator
    Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance.
    Tesmilifene
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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