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-169119
    Antifungal agent 114
    Inhibitor
    Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes.
    Antifungal agent 114
  • HY-B1184S
    Mephenytoin-d3
    (Rac)-Mephenytoin-d3 is a labelled racemic Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.
    Mephenytoin-d<sub>3</sub>
  • HY-122932
    Neoquassin
    Neoquassin is found in Picrasma quassioides.
    Neoquassin
  • HY-133091R
    7-Ethoxycoumarin (Standard)
    7-Ethoxycoumarin (Standard) is the analytical standard of 7-Ethoxycoumarin. This product is intended for research and analytical applications. 7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573).
    7-Ethoxycoumarin (Standard)
  • HY-B0973R
    Dibenzothiophene (Standard)
    Inhibitor
    Dibenzothiophene (Standard) is the analytical standard of Dibenzothiophene (HY-B0973). This product is intended for research and analytical applications. Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with Km of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms.
    Dibenzothiophene (Standard)
  • HY-W777979
    Frutinone A
    Inhibitor
    Frutinone A is a CYP1A2 inhibitor, possesses a chromonocoumarin structural scaffold. Frutinone A shows various biological activities, including antibacterial and antioxidant.
    Frutinone A
  • HY-N2689
    (R)-6',7'-Dihydroxybergamottin
    Inhibitor
    (R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research.
    (R)-6',7'-Dihydroxybergamottin
  • HY-117219
    SKF 104976
    Inhibitor
    SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin.
    SKF 104976
  • HY-114763
    LP8
    Inhibitor
    LP8 is a Pyridinyl-type CYP51 inhibitor and can be used for study of chagas disease and American trypanosomiasis.
    LP8
  • HY-B0859R
    MCPA (Standard)
    Activator
    MCPA (Standard) is the analytical standard of MCPA (HY-B0859). This product is intended for research and analytical applications. 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 (Standard)
  • HY-W422288
    (Rac)-Ketoconazole
    Inhibitor
    (Rac)-Ketoconazole ((Rac)-R 41400) is an antifungal imidazole compound with oral activity. (Rac)-Ketoconazole interferes with ergosterol synthesis by inhibiting cytochrome P450-dependent 14α-sterol demethylase (CYP51), a key enzyme on the fungal cell membrane, leading to membrane dysfunction and ultimately inhibition of fungal growth and reproduction. (Rac)-Ketoconazole is indicated for studies of fungal infections.
    (Rac)-Ketoconazole
  • HY-B1324R
    Oxiconazole nitrate (Standard)
    Activator
    Oxiconazole nitrate (Standard) is the analytical standard of Oxiconazole nitrate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-122481
    Thaspine acetate
    Inducer
    Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri.
    Thaspine acetate
  • HY-13762S
    Tesmilifene-d4
    Modulator
    Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance.
    Tesmilifene-d<sub>4</sub>
  • HY-30151R
    Methoxsalen (Standard)
    Inhibitor
    Methoxsalen (Standard) is the analytical standard of Methoxsalen. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N3758
    Dihydrosesamin
    Dihydrosesamin is a Lignans product that can be isolated from the young shoots of Chamaecyparis obtusa cv. Breviramea..
    Dihydrosesamin
  • HY-B1307R
    Zoxazolamine (Standard)
    Zoxazolamine (Standard) is the analytical standard of Zoxazolamine. This product is intended for research and analytical applications. Zoxazolamine is widely used for a pharmacologic test that serves as a convenient indicator of changes in cytochrome P-450 activity in rodents.
    Zoxazolamine (Standard)
  • HY-111052R
    AZD7325 (Standard)
    Activator
    AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
    AZD7325 (Standard)
  • HY-B1812S4
    Veratrole-d2-1
    Substrate
    Veratrole-d2-1 is the deuterium labeled Veratrole (HY-B1812). Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.
    Veratrole-d<sub>2</sub>-1
  • HY-130318
    Quinidine N-oxide
    Control
    Quinidine N-oxide is a pharmacologically inactive metabolite of Quinidine (HY-B1751H). Quinidine is an active probe of CYP3A4.
    Quinidine N-oxide
Cat. No. Product Name / Synonyms Application Reactivity

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