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-112690A
    Pradefovir mesylate
    99.89%
    Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
    Pradefovir mesylate
  • 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 99.45%
    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-13632R
    Exemestane (Standard)
    Inhibitor 99.63%
    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-N8382
    Chalepensin
    Inhibitor ≥98.0%
    Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents.
    Chalepensin
  • HY-75054R
    Abiraterone acetate (Standard)
    Inhibitor 99.85%
    Abiraterone acetate (Standard) is the analytical standard of Abiraterone acetate. This product is intended for research and analytical applications. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
    Abiraterone acetate (Standard)
  • HY-B0105S1
    Ketoconazole-d4
    Inhibitor ≥98.0%
    Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole-d<sub>4</sub>
  • HY-117161
    ZINC05626394
    Inhibitor 99.8%
    ZINC05626394 is a cytochrome b5 reductase 3 inhibitor with activity by increasing nitric oxide bioavailability. ZINC05626394 may have potential applications in anti-cancer suppression, especially in combination with antibody drug conjugates (ADCs) and immune checkpoint inhibitors. The efficacy of ZINC05626394 may be limited by different mechanisms, including antigen-related resistance and failure of endocytosis.
    ZINC05626394
  • HY-N2262
    8-Geranyloxypsoralen
    Inhibitor 99.93%
    8-Geranyloxypsoralen is a furanocoumarin isolated from grapefruit, acts as a potent inhibitor of P450 3A4 (CYP3A4) with an IC50 of 3.93 μM.
    8-Geranyloxypsoralen
  • HY-108938
    SDZ285428
    Inhibitor 98.00%
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
    SDZ285428
  • HY-155493
    CYP19A1/CYP11B2-IN-1
    Inhibitor 99.85%
    CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer.
    CYP19A1/CYP11B2-IN-1
  • HY-17508S1
    Clarithromycin-d3
    Inhibitor 99.90%
    Clarithromycin-d3 is the deuterium labeled Clarithromycin (HY-17508). Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
    Clarithromycin-d<sub>3</sub>
  • HY-16718A
    Dagrocorat hydrochloride
    Inhibitor 99.85%
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis.
    Dagrocorat hydrochloride
  • HY-W006230
    Anthraflavic acid
    Inhibitor 99.51%
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
    Anthraflavic acid
  • HY-B0892R
    Benzyl alcohol (Standard)
    Inhibitor
    Benzyl alcohol (Standard) is the analytical standard of Benzyl alcohol. This product is intended for research and analytical applications. Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor.
    Benzyl alcohol (Standard)
  • HY-118474
    GW 610
    Activator 99.78%
    GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines.
    GW 610
  • HY-122277S
    1'-Hydroxy bufuralol-d9
    99.00%
    1'-Hydroxy bufuralol-d9 is a deuterium labeled 1'-Hydroxy bufuralol (HY-122277). 1'-Hydroxy bufuralol, the main metabolite of bufuralol, can reflect CYP2D activity.
    1'-Hydroxy bufuralol-d<sub>9</sub>
  • HY-N0453R
    Hypericin (Standard)
    Inhibitor
    Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.
    Hypericin (Standard)
  • HY-W014075S
    1-Hydroxypyrene-d9
    Activator 99.95%
    1-Hydroxypyrene-d9 is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 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-d<sub>9</sub>
  • HY-N2233
    Rhapontigenin 3'-O-glucoside
    Inhibitor 99.94%
    Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent.
    Rhapontigenin 3'-O-glucoside
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