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-D0092R
    7-Ethoxy-4-methylcoumarin (Standard)
    7-Ethoxy-4-methylcoumarin (Standard) is the analytical standard of 7-Ethoxy-4-methylcoumarin. This product is intended for research and analytical applications. 7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6.
    7-Ethoxy-4-methylcoumarin (Standard)
  • HY-N4205R
    Tetrahydropiperine (Standard)
    Inhibitor
    Tetrahydropiperine (Standard) is the analytical standard of Tetrahydropiperine. This product is intended for research and analytical applications. Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum. Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM).
    Tetrahydropiperine (Standard)
  • HY-W739700
    (R)-(+)-Aminoglutethimide L-Tartrate
    Inhibitor
    (R)-(+)-Aminoglutethimide (L-Tartrate) is an inhibitor of aromatase. (R)-(+)-Aminoglutethimide inhibits androstenedione with a Ki value of 0.3 μM.
    (R)-(+)-Aminoglutethimide L-Tartrate
  • HY-B1717
    Oxolamine
    Inhibitor
    Oxolamine (SKF-9976) is an orally active antitussive. Oxolamine can inhibit CYP2B1/2. Oxolamine has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine can be used in respiratory disease research.
    Oxolamine
  • HY-137931
    Testololactone
    Inhibitor
    Testololactone is an aromatase inhibitor. Testololactone can be used for research of breast carcinoma.
    Testololactone
  • HY-168210
    Antifungal agent 122
    Inhibitor
    Antifungal agent 122 (compound 201) is a potent and broad-spectrum antifungal agent. Antifungal agent 122 prevents fungal phase transition and the formation of fungal biofilm. Antifungal agent 122 inhibits CYP3A4-M and CYP3A4-T enzyme activity with IC50 values of 2.11, 4.53 µM. Antifungal agent 122 shows no cytotoxicity.
    Antifungal agent 122
  • HY-D0092
    7-Ethoxy-4-methylcoumarin
    99.44%
    7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6.
    7-Ethoxy-4-methylcoumarin
  • HY-B1812S
    Veratrole-d4
    Substrate
    Veratrole-d4 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.
    Veratrole-d<sub>4</sub>
  • HY-172808
    BNS808
    Inhibitor
    BNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding.
    BNS808
  • HY-N2194R
    Bergamottin (Standard)
    Inhibitor
    Bergamottin (Standard) is the analytical standard of Bergamottin. This product is intended for research and analytical applications. Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
    Bergamottin (Standard)
  • HY-170928
    DA-0157
    Inhibitor
    DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models.
    DA-0157
  • 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-E70468
    Human CYP1A1,High-Reductase
    Human CYP1A1, High-Reductase, a recombinant CYP1A1, is one of the most important cytochrome P450 (CYP) enzymes. Human CYP1A1, High-Reductase is involved in the metabolism of several genotoxic/carcinogenic environmental xenobiotics.
    Human CYP1A1,High-Reductase
  • HY-B1812S1
    Veratrole-d2
    Substrate
    Veratrole-d2 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.
    Veratrole-d<sub>2</sub>
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity

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