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-N0094
    Ipriflavone
    Inhibitor 99.89%
    Ipriflavone is a synthetic isoflavone derivative used to suppress bone resorption.
    Ipriflavone
  • HY-N0563
    Alizarin
    99.17%
    Alizarin is a natural dye. Alizarin can be extracted from the roots of madder plant. Alizarin activates AMPK and VEGFR2/eNOS pathway. Alizarin regulates PI3K/Akt and inhibits NF-κB pathway. Alizarin enhances CYP1A1 enzyme activity. Alizarin has protective effects on hypertension and vascular endothelial dysfunction. Alizarin has anti-tumor activity against multiple cancers including pancreatic cancer, breast cancer, osteosarcoma and liver cancer. Alizarin has been widely used as a pigment in textile fabrics and paintings.
    Alizarin
  • HY-15565
    APD668
    Inhibitor 99.73%
    APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.
    APD668
  • HY-137258
    (±)-N-3-Benzylnirvanol
    Inhibitor 99.88%
    (±)-N-3-Benzylnirvanol is a racemic mixture of (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol. (+)-N-3-Benzylnirvanol and (–)-N-3-Benzylnirvanol are potent and selective cytochrome P450 inhibitors with Ki values of 0.25 and 5.3 μM for CYP2C19, respectively.
    (±)-N-3-Benzylnirvanol
  • HY-14247A
    Fadrozole
    Inhibitor 99.78%
    Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
    Fadrozole
  • HY-W014075
    1-Hydroxypyrene
    Activator 99.84%
    1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.
    1-Hydroxypyrene
  • HY-W040030
    Hematin
    98.09%
    Hematin, an iron-containing porphyrin, inhibits the activity of clotting factors and also fibrin clot lysis through the mechanism of binding to and inactivation of hemostatic proteins. Hematin can be used for the research of acute porphyrias and cancer.
    Hematin
  • HY-101527
    20-HEDE
    Antagonist ≥98.0%
    20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
    20-HEDE
  • HY-160972
    MM0299
    Inhibitor 98.51%
    MM0299 is an inhibitor for lanosterol synthase (LSS) with an IC50 of 2.2 μM. MM0299 inhibits cell proliferation of Mut6 with an IC50 of 0.0182 μM, through generation of 24(S),25-epoxycholesterol (EPC) and the depletion of cellular cholesterol.
    MM0299
  • HY-B1234
    Octinoxate
    Inhibitor 99.89%
    Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate
  • HY-N0598
    Ginsenoside F1
    Inhibitor ≥99.0%
    Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1
  • HY-N9608
    6-Ketocholestanol
    98.68%
    6-Ketocholestanol is a recoupler for mitochondria, chromatophores and cytochrome oxidase proteoliposomes. 6-Ketocholestanol increases the membrane dipole potential.
    6-Ketocholestanol
  • HY-B0854
    Mancozeb
    Modulator
    Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.
    Mancozeb
  • HY-B1324
    Oxiconazole nitrate
    Activator ≥98.0%
    Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest.
    Oxiconazole nitrate
  • HY-N2260
    Cephaeline dihydrochloride
    Inhibitor 99.84%
    Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
    Cephaeline dihydrochloride
  • HY-N8354
    6',7'-Dihydroxybergamottin
    Inhibitor ≥99.0%
    6',7'-Dihydroxybergamottin (6′,7′-DHB), a furanocoumarin, is a potent CYP3A4 inhibitor.
    6',7'-Dihydroxybergamottin
  • HY-135331
    N-Desmethyl-Apalutamide
    Modulator 99.68%
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.
    N-Desmethyl-Apalutamide
  • HY-148825
    NP10679
    Inhibitor 99.42%
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
    NP10679
  • HY-106019
    Liarozole
    Inhibitor 98.83%
    Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.
    Liarozole
  • HY-17570
    Desoximetasone
    Substrate 99.31%
    Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.
    Desoximetasone
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