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-135281
    CYP11B2-IN-1
    Inhibitor 99.83%
    CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM.
    CYP11B2-IN-1
  • HY-13600R
    Clobetasol propionate (Standard)
    Inhibitor
    Clobetasol propionate (Standard) is the analytical standard of Clobetasol propionate. This product is intended for research and analytical applications. Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research.
    Clobetasol propionate (Standard)
  • HY-U00373
    Revexepride
    Activator 99.84%
    Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.
    Revexepride
  • HY-119647
    PPOH
    Inhibitor 99.87%
    PPOH, a fatty acid derivative, is a selective cyclooxygenase (COX) inhibitor that inhibits arachidonic acid cyclooxygenase activity in renal cortical microsomes. In addition, PPOH acts on CYP4A2 and CYP4A3 with the IC50 values of 22 μM and 6.5 μM, respectively. PPOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PPOH
  • HY-175266
    MI1013
    Inhibitor
    MI1013 is a PROTAC PXR degrader (DC50 = 89 nM, Dmax = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67). (Pink: PXR ligand 3: HY-175267, Blue: Pomalidomide-propargyl ligand: HY-W410002, Pink + Black: PXR ligand-Linker Conjugate 1: HY-175268).
    MI1013
  • HY-141530
    Clopidogrel-β-D-glucuronide
    Inhibitor
    Clopidogrel-β-D-glucuronide is a metabolite of Clopidogrel (HY-15283). Clopidogrel-β-D-glucuronide directly interacts with CYP2C8 enzyme and strongly inhibits the liver enzyme CYP2C8.
    Clopidogrel-β-D-glucuronide
  • HY-U00048
    Bucolome
    Inhibitor 98.93%
    Bucolome is a CYP2C9 inhibitor, used as an uricosuric agent or anti-inflammatory agent.
    Bucolome
  • HY-N2233
    Rhapontigenin 3'-O-glucoside
    Inhibitor 99.94%
    Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent.
    Rhapontigenin 3'-O-glucoside
  • HY-17514S2
    Itraconazole-d9
    Itraconazole-d9 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
    Itraconazole-d<sub>9</sub>
  • HY-130419
    (±)13(14)-EpDPA
    (±)13(14)-EpDPA (13,14-EpDPE) is the product of the reaction of cytochrome P-450 epoxygenase with Docosahexaenoic Acid (DHA).(±)13(14)-EpDPA has antihyperalgesic and vasorelaxative activities.
    (±)13(14)-EpDPA
  • HY-112734
    4'-Methylchrysoeriol
    Inhibitor 99.17%
    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
    4'-Methylchrysoeriol
  • HY-121580
    Tabimorelin
    Inhibitor 98.11%
    Tabimorelin (NN703) is an orally active growth hormone (GH) secretagogue. Tabimorelin is also a potent inhibitor of CYP3A4 activity.
    Tabimorelin
  • HY-D0144
    Resorufin methyl ether
    99.75%
    Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate. Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents.
    Resorufin methyl ether
  • HY-B0859S1
    MCPA-d3
    Activator 98.0%
    MCPA-d3 is the deuterium labeled MCPA (HY-B0859). MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds.
    MCPA-d<sub>3</sub>
  • HY-111202
    Pyributicarb
    Activator 99.80%
    Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
    Pyributicarb
  • HY-120648A
    CAY 10462 dihydrochloride
    Inhibitor 98.02%
    CAY 10434 dihydrochloride is a potent CYP4A hydroxylase inhibitor. CAY 10434 dihydrochloride improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg.
    CAY 10462 dihydrochloride
  • HY-B0852R
    Tebuconazole (Standard)
    Inhibitor
    Tebuconazole (Standard) is the analytical standard of Tebuconazole. This product is intended for research and analytical applications. Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.
    Tebuconazole (Standard)
  • HY-N1882
    4,5-Dimethoxycanthin-6-one
    Inhibitor 98.68%
    4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae).
    4,5-Dimethoxycanthin-6-one
  • HY-W587878
    Thujopsene
    Inhibitor
    Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation.
    Thujopsene
  • HY-14248R
    Letrozole (Standard)
    Inhibitor
    Letrozole (Standard) is the analytical standard of Letrozole. This product is intended for research and analytical applications. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
    Letrozole (Standard)
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