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-170929
    EMT inhibitor-3
    Activator
    EMT inhibitor-3 (compound 11i) is a epithelial-mesenchymal transition (EMT) inhibitor. EMT inhibitor-3 inhibits neuroblastoma SK-N-SH cells with an IC50 of 2.5 μM. EMT inhibitor-3 inhibits SK-N-SH cell proliferation, migration, and invasion. EMT inhibitor-3 increases the Bax/Bcl-2 protein expression ratio, promotes Cytochrome C ( HY-125857) release from mitochondria, and activates caspases 9 and caspases 3, inducing mitochondria-mediated endogenous tumor cell Apoptosis. EMT inhibitor-3 is potential for cancer research.
    EMT inhibitor-3
  • HY-121213
    Erysolin
    Inhibitor
    Erysolin is a CYP1A inhibitor with antigenic toxicity. Erysolin reduces benzo(a)pyrene-induced genotoxicity.
    Erysolin
  • HY-B0940S
    Ethylvanillin-d5
    Ethylvanillin-d5 is a deuterium labeled Ethylvanillin (HY-B0940).
    Ethylvanillin-d<sub>5</sub>
  • HY-B1751A
    Quinidine sulfate
    Inhibitor
    Quinidine Monosulfate is an antiarrhythmic agent. Quinidine Monosulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine Monosulfate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine Monosulfate can be used for malaria research.
    Quinidine sulfate
  • HY-161700
    BMS-737
    BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels.
    BMS-737
  • HY-B0859S
    MCPA-13C8
    Activator
    MCPA-13C8 is the 13C-labeled MCPA (HY-B0859). MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds.
    MCPA-<sup>13</sup>C<sub>8</sub>
  • HY-N2372R
    Fraxinol (Standard)
    Inhibitor
    Fraxinol (Standard) is the analytical standard of Fraxinol. This product is intended for research and analytical applications. Fraxinol is isolated from Lobelia chinensis.
    Fraxinol (Standard)
  • HY-17367S4
    Atazanavir-d6
    Inhibitor 99.28%
    Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir-d<sub>6</sub>
  • HY-159143
    BChE-IN-33
    Inhibitor
    BChE-IN-33 (compound 4r), an arylaminonaphthol derivative, is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 14.78 µM. BChE-IN-33 also inhibits CYP2C19, CYP2C9, CYP2D6. BChE-IN-33 shows potent antioxidant activity with IC50 values of 150.48 μM, 2.56 μM and 4.61 μM by DPPH, ABTS, Ferric-phenanthroline assay, respectively. BChE-IN-33 has the potential for Alzheimer research.
    BChE-IN-33
  • HY-75054S
    Abiraterone acetate-d4
    Inhibitor
    Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. 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-d<sub>4</sub>
  • HY-159585
    CYP51-IN-20
    Inhibitor
    CYP51-IN-20 (compound 5b) is an inhibitor of CYP51 and has antifungal activity. CYP51-IN-20 has a significant inhibitory effect on Candida albicans ATCC 10231, downregulates ERG11 (Cyp51) gene expression, and significantly reduces the yeast-to-hyphae morphological transition. CYP51-IN-20 can synergize with Voriconazole (HY-76200) to occupy the entire CYP51 binding site and exert a synergistic inhibitory effect in the Glechoma moth model.
    CYP51-IN-20
  • HY-149977
    Anticancer agent 111
    Inhibitor
    Anticancer agent 111 (compound 11) is a potent cytochrome P450 inhibitor with an IC50 value of 3 μM for CYP3A4. Anticancer agent 111 has anticancer activity. Anticancer agent 111 can be used in research of cancer.
    Anticancer agent 111
  • HY-130139
    11,12-DiHETE
    11,12-DiHETE is an orally active metabolite produced by cytochrome p450 mediated epoxide formation and subsequent epoxide hydrolase production.
    11,12-DiHETE
  • HY-116050A
    17(R)-HETE
    17R-HETE is an arachidonic acid metabolite through cytochrome P-450 pathways. 17R-HETE exhibits efficacy in inducing cardic hypertrophy with less efficiency with compared to 17S-HETE.
    17(R)-HETE
  • HY-W777749
    Methoxsalen-13C,d3
    Methoxsalen-13C,d3 (8-Methoxypsoralen-13C,d3) is the deuterium and 13C-labeled Methoxsalen (HY-30151). Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.
    Methoxsalen-<sup>13</sup>C,d<sub>3</sub>
  • HY-161403
    CYP1B1-IN-8
    Inhibitor
    CYP1B1-IN-8 (Compound 14b) is a CYP1B1 inhibitor (IC50: 4.14 × 10–5 nM). CYP1B1-IN-8 reduces the resistance in A549 cells to Paclitaxel (HY-B0015), and inhibits cell migration and invasion.
    CYP1B1-IN-8
  • HY-B0725R
    Doxepin Hydrochloride (Standard)
    Inhibitor
    Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
    . Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system.
    . Doxepin has also been proposed as a protective factor against oxidative stress.
    .
    Doxepin Hydrochloride (Standard)
  • HY-W008364S1
    Olivetol-d9
    Olivetol-d9 is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activities.
    Olivetol-d<sub>9</sub>
  • HY-10672
    Urotensin-II receptor antagonist-1
    Inhibitor
    Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM).
    Urotensin-II receptor antagonist-1
  • HY-B1751E
    Quinidine polygalacturonate
    Inhibitor
    Quinidine polygalacturonate is an antiarrhythmic agent. Quinidine polygalacturonate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine polygalacturonate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine polygalacturonate can be used for malaria research.
    Quinidine polygalacturonate
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