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-76316
    Bergaptol
    Inhibitor 99.44%
    Bergaptol is an inhibitor of debenzylation of the CYP3A4 enzyme with an IC50 of 24.92 μM. Recent studies have shown that it has anti-proliferative and anti-cancer properties.
    Bergaptol
  • HY-18719E
    Endoxifen
    Inhibitor 99.42%
    Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
    Endoxifen
  • HY-N2534
    Karanjin
    Inhibitor 99.89%
    Karanjin is an orally active furanoflavonoid which can be isolated from several Leguminosae. Karanjin exhibits evident anti-diabetic, anti-cancer, anti-inflammatory, antioxidant, anticolitis, anti-ulcer, anti-Alzheimer properties and multiple insect repellent/insecticidal, acaricide properties, suggesting the potential of Karanjin to be applied to relevant research.
    Karanjin
  • HY-B0852
    Tebuconazole
    Inhibitor 99.63%
    Tebuconazole is an 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
  • HY-100590
    FPH1
    Activator 99.89%
    FPH1(BRD-6125) increases the number and activity of primary human hepatocytes in vitro and promotes the differentiation of iPS cells towards a hepatic lineage.
    FPH1
  • HY-W013268
    (S)-(+)-N-3-Benzylnirvanol
    Inhibitor 99.82%
    (S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.
    (S)-(+)-N-3-Benzylnirvanol
  • HY-100386
    Ticlopidine
    Inhibitor 99.74%
    Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
    Ticlopidine
  • HY-21065
    Tienilic acid
    99.69%
    Tienilic acid (Ticrynafen; ANP 3624) acts as a diuretic hypotensive agent. However, Tienilic acid induces hepatotoxicity. Tienilic acid is converted into electrophilic metabolites by cytochrome P450 (CYP) in vitro.
    Tienilic acid
  • HY-129105
    Clomethiazole
    Inhibitor 98.65%
    Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Clomethiazole
  • HY-N0920
    Dihydrokavain
    Inhibitor 99.94%
    Dihydrokavain (7,8-Dihydrokawain) is a natural kavalactone compound. Dihydrokavain inhibits COX-1, COX-2, CYP2C9 (IC50 = 130.95 μM), CYP2C19 (IC50 = 10.05 μM) and CYP3A4 (IC50 = 78.59 μM). Dihydrokavain reduces TNFα secretion. Dihydrokavain shows analgesic and anxiolytic effects.
    Dihydrokavain
  • HY-B1311
    Proadifen hydrochloride
    Inhibitor 99.95%
    Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases.
    Proadifen hydrochloride
  • HY-70006
    Galeterone
    Inhibitor 99.87%
    Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
    Galeterone
  • HY-B0105B
    (-)-Ketoconazole
    Inhibitor 99.39%
    (-)-Ketoconazole ((-)-R 41400) is one of the enantiomers of ketoconazole (HY-B0105). Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole). Ketoconazole is an antifungal agent and a cytochrome P450 inhibitor.
    (-)-Ketoconazole
  • HY-17367A
    Atazanavir sulfate
    Inhibitor 99.68%
    Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir sulfate
  • HY-14247
    Fadrozole hydrochloride
    Inhibitor 99.91%
    Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
    Fadrozole hydrochloride
  • HY-B0885
    Econazole
    Inhibitor 99.93%
    Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage.
    Econazole
  • HY-18642
    CYP3cide
    Inhibitor 99.92%
    CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism.
    CYP3cide
  • HY-160186
    20-SOLA
    Antagonist 98.76%
    20-SOLA is an orally active 20-HETE antagonist. 20-SOLA greatly ameliorates changes in blood pressure and renal injury associated with a Streptozotocin (STZ) (HY-13753)-diabetic mouse model. 20-SOLA facilitates the restoration of coronary collateral growth (CCG) after ischemic injury. 20-SOLA can be studied for research in cardiovascular diseases and diabetes.
    20-SOLA
  • HY-N0762
    Isobavachin
    Inhibitor 99.88%
    Isobavachin, an antioxidant isaolated from Psoralea corylifolia with a prenyl group at position 8 of ring A, promotes neuronal differentiation and the potential role of its protein prenylation.
    Isobavachin
  • HY-B1184
    Mephenytoin
    99.96%
    Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.
    Mephenytoin
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