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-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-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-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-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
  • 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-N16471
    Escholtzine
    Inhibitor
    Escholtzine is an alkaloid found in Eschscholzia californica. Escholtzine can inhibit [3H]8-OH-DPAT Binding to the 5-HT1A receptor with an EC50 of 11 μM and a Ki of 6 μM. Escholtzine can inhibit CYP3A4 with an IC50 of 13.4 μg/mL. Escholtzine can be used for the research of neurological disease, such as anxiety.
    Escholtzine
  • 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
  • HY-W779191
    MeIQx-13C
    MeIQx-13C (2-Amino-3,8-dimethylimidazo[4,5-f]quinoxaline-2-13C) is the 13C-labeled MeIQx (HY-W355129). MeIQx, a dietary aromatic amine, is mutagenic compound could be isolated from present in fried beef and beef extracts. MeIQx binds covalently to hemoglobin. MeIQx induces liver tumors.
    MeIQx-<sup>13</sup>C
  • HY-116214S
    Cyprodinil-d5
    Inducer
    Cyprodinil-d5(CGA-219417-d5) is the deuterium labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil-d<sub>5</sub>
  • HY-W014566R
    4-Nitro-3-(trifluoromethyl)phenol (Standard)
    Inhibitor
    Moxifloxacin (hydrochloride monohydrate) (Standard) is the analytical standard of Moxifloxacin (hydrochloride monohydrate). This product is intended for research and analytical applications. Moxifloxacin (BAY 12-8039) hydrochloride monohydrate is an orally active bacterial inhibitor that is effective against Streptococcus pneumoniae. Moxifloxacin hydrochloride monohydrate can be used in tuberculosis research.
    4-Nitro-3-(trifluoromethyl)phenol (Standard)
  • HY-120067
    YM116
    Inhibitor
    YM116 is an orally active and competitive CYP17A1 (17,20-lyase) inhibitor (Ki: 0.38 nM). YM116 reduces the synthesis of adrenal androgens by preferentially inhibiting C17-20 lyase activity. YM116 decreases the serum testosterone concentration, reduces dehydroepiandrosterone sulfate levels and decreases prostatic weights.
    YM116
Cat. No. Product Name / Synonyms Application Reactivity

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