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-N0921
    Dihydromethysticin
    Activator 99.94%
    Dihydromethysticin is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23.
    Dihydromethysticin
  • HY-133091
    7-Ethoxycoumarin
    99.84%
    7-Ethoxycoumarin is a substrate for cytochrome P450(CYP450) and has been used in the functional characterization of various CYPs[1].
    7-Ethoxycoumarin
  • HY-14405A
    Casopitant mesylate
    Inhibitor 99.84%
    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-N0762
    Isobavachin
    Inhibitor 99.84%
    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-117026
    LKY-047
    Inhibitor 99.94%
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
    LKY-047
  • 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-N0779
    Isosilybin
    Inhibitor 99.95%
    Isosilybin (Isosilybinin) is a flavonoid from Silybum marianum; inhibits CYP3A4 induction with an IC50 of 74 μM.
    Isosilybin
  • HY-112619
    TES-991
    Inhibitor 99.65%
    TES-991 is a potent and selective human α?Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
    TES-991
  • HY-15565
    APD668
    Inhibitor 99.10%
    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-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-N7266
    Obtusifoliol
    Inhibitor 99.86%
    Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 μM and 1.4 μM for Trypanosoma brucei (TB) and human CYP51, respectively.
    Obtusifoliol
  • HY-N2625A
    Harmalol hydrochloride
    99.72%
    Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties.
    Harmalol hydrochloride
  • HY-B0822
    Fipronil
    Activator 98.98%
    Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
    Fipronil
  • HY-147277
    Lorundrostat
    Inhibitor 99.37%
    Lorundrostat (MT-4129) is an orally active aldosterone synthase inhibitor. Lorundrostat can be used in studies of high blood pressure.
    Lorundrostat
  • 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/KDR/Flk-1/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-N2071
    Cedrol
    Inhibitor ≥98.0%
    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-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-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-101527
    20-HEDE
    Antagonist ≥98.0%
    20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).
    20-HEDE
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