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-N2071
    Cedrol
    Inhibitor 99.76%
    Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
    Cedrol
  • 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-N0926A
    Columbamine chloride
    Inhibitor 98.63%
    Columbamine (Columbamin; Dehydroisocorypalmine) chloride is an organic heterotetracyclic alkaloid extracted from plants. Columbamine chloride is a metabolite of Berberine (HY-N0716). Columbamine chloride inhibits the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 30.6 µM). Columbamine chloride induces apoptosis in cancer cells. Columbamine chloride can be used for antioxidant, anti-inflammatory, antitumor, antifungal, antiparasite, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic study.
    Columbamine chloride
  • HY-N0779
    Isosilybin
    Inhibitor 99.95%
    Isosilybin (Isosilybinin) is a flavonoid from Silybum marianum; inhibits CYP3A4 induction with an IC50 of 74 μM.
    Isosilybin
  • HY-132845
    Utreloxastat
    Inhibitor 99.69%
    Utreloxastat (PTC857) is an orally active and blood-brain barrier-permeable 15-lipooxygenase inhibitor. Utreloxastat is a weak inhibitor of CYP1A2 and 2B6 with an IC50 of >5.3 μM. Utreloxastat reduces oxidative stress and inhibits the consumption of reduced glutathione and ferroptosis. Utreloxastat can be used in the study of neurodegenerative diseases characterized by high levels of oxidative stress and mitochondrial pathology, such as amyotrophic lateral sclerosisc.
    Utreloxastat
  • HY-N0094
    Ipriflavone
    Inhibitor 99.89%
    Ipriflavone is a synthetic isoflavone derivative used to suppress bone resorption.
    Ipriflavone
  • HY-101527
    20-HEDE
    Antagonist ≥98.0%
    20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
    20-HEDE
  • HY-137258
    (±)-N-3-Benzylnirvanol
    Inhibitor 99.86%
    (±)-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-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-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-14405A
    Casopitant mesylate
    Inhibitor 99.83%
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant mesylate
  • HY-41404
    Piperonylic acid
    Inhibitor 99.91%
    Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase. Piperonylic acid has anticancer, antioxidant and antibacterial activities.
    Piperonylic acid
  • HY-B1234
    Octinoxate
    Inhibitor 99.84%
    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-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-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-N6677
    β-​Apo-​8'-​carotenal
    Activator
    β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables.
    β-​Apo-​8'-​carotenal
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