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-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-113031
    16a-Hydroxydehydroisoandrosterone
    98.54%
    16a-Hydroxydehydroisoandrosterone (16α-Hydroxy-DHEA) is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.
    16a-Hydroxydehydroisoandrosterone
  • HY-41268
    3-Methoxyphenylethylamine
    Substrate 99.39%
    3-Methoxyphenylethylamine is an organic compound that is used as an intermediate for pharmaceuticals, dyestuffs, and liquid crystal materials.
    3-Methoxyphenylethylamine
  • HY-W196803
    Dipropyl disulfide
    99.54%
    Dipropyl disulfide is oxidized to dipropyl thiosulfinate (DPDSO) by rat microsomes. Both flavincontaining monooxygenases (FMO) and cytochrome P450 enzymes (CYPs) are involved in dipropyl disulfide oxidation. Dipropyl disulfide forms two metabolites: propylglutathione sulfide conjugate and propylthiol.
    Dipropyl disulfide
  • HY-W010195
    2,6-Dimethylquinoline
    Inhibitor 99.95%
    2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM.
    2,6-Dimethylquinoline
  • HY-B0113S
    Omeprazole-d3
    98.99%
    Omeprazole-d3 (H 16868-d3) is deuterium labeled Omeprazole. Omeprazole (H 16868) is an orally active H+,K+-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.
    Omeprazole-d<sub>3</sub>
  • HY-101284
    DMU2105
    Inhibitor 99.31%
    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
    DMU2105
  • HY-12946
    BI 653048
    Inhibitor 99.84%
    BI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
    BI 653048
  • HY-12035
    AMG-208
    Inhibitor 99.86%
    AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity.
    AMG-208
  • HY-B1462S
    Chlorzoxazone-d3
    Modulator 99.88%
    Chlorzoxazone-d3 is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.
    Chlorzoxazone-d<sub>3</sub>
  • HY-155002
    hCYP3A4 Fluorogenic substrate 1
    99.07%
    hCYP3A4 Fluorogenic substrate 1 is a potrnt hCYP3A4 fluorogenic substrate with an Km value of 0.36 μM. hCYP3A4 Fluorogenic substrate 1 can be used for cell and in vivo imaging.
    hCYP3A4 Fluorogenic substrate 1
  • HY-156883
    Dasatinib analog-1
    Inhibitor 98.08%
    Dasatinib analog-1 (compound 5826) inhibits CYP3A4 viability with a Ki value of 5.4 μM. Dasatinib analog-1 blocks the formation of glutathione adducts.
    Dasatinib analog-1
  • HY-100238
    Antihistamine-1
    Inhibitor 99.08%
    Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
    Antihistamine-1
  • HY-151810
    TP0472993
    Inhibitor 98.22%
    CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases.
    TP0472993
  • HY-N5011R
    5,7-Dimethoxyflavone (Standard)
    Inhibitor
    5,7-Dimethoxyflavone (Standard) is the analytical standard of 5,7-Dimethoxyflavone. This product is intended for research and analytical applications. 5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
    5,7-Dimethoxyflavone (Standard)
  • HY-13632R
    Exemestane (Standard)
    Inhibitor
    Exemestane (Standard) is the analytical standard of Exemestane. This product is intended for research and analytical applications. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
    Exemestane (Standard)
  • HY-116780A
    Prothipendyl hydrochloride
    Substrate 99.94%
    Prothipendyl hydrochloride is a tricyclic azaphenothiazine neuroleptic agent. Prothipendyl hydrochloride is a substrate of the CYP isozymes CYP1A2, CYP2D6, CYP2C19 and CYP3A4. Prothipendyl hydrochloride has sedating and psychomotorically damping effects. Prothipendyl hydrochloride can be used for psychomotoric agitation, sleep disorder and anxiety research .
    Prothipendyl hydrochloride
  • HY-B0113S3
    Omeprazole-13C,d3
    98.00%
    Omeprazole-13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868) is an orally active H+,K+-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.
    Omeprazole-<sup>13</sup>C,d<sub>3</sub>
  • HY-N3680
    Danshenxinkun A
    99.84%
    Danshenxinkun A is a natural compound that could be isolated from Tanshen and is used in the study for heart diseases.
    Danshenxinkun A
  • HY-B0822R
    Fipronil (Standard)
    Activator
    Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. 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 (Standard)
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