2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome P450

Related Products

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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.

Cytochrome P450 Isoform Specific Products:

Cytochrome P450 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-117789
    Keto-itraconazole
    		Inhibitor
    Keto-itraconazole (keto-ITZ) is a metabolism of Itraconazole (HY-17514) with a potent inhibitor activity of CYP3A. Keto-itraconazole shows unbound IC50 value of 4.6 nM when coincubated with human liver microsomes and midazolam.
    Keto-itraconazole
  • HY-B0035B
    Sulfamethazine 100 µg/mL in acetonitrile
    		Activator
    Sulfamethazine 100 μg/mL in acetonitrile (Sulfadimidine 100 μg/mL in acetonitrile) is an antimicrobial agent that induces CYP3A4 expression and is acetylated by N-acetyltransferase. It exhibits sex-dependent pharmacokinetics and is metabolized by CYP2C11 in males.
    Sulfamethazine 100 µg/mL in acetonitrile
  • HY-159006
    CYP1B1 ligand 3
    		Inhibitor
    CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429).
    CYP1B1 ligand 3
  • HY-126308
    (E/Z)-DMU2139
    		Inhibitor
    (E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM).
    (E/Z)-DMU2139
  • HY-128706
    (+)-Menthofuran
    		Inhibitor
    (+)-Menthofuran (compound 1) is a furan terpenoid that can be found in mint oils.
    (+)-Menthofuran
  • HY-W008364R
    Olivetol (Standard)
    		Inhibitor
    Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. 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. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
    Olivetol (Standard)
  • HY-157170
    CYP450-IN-1
    		Inhibitor
    CYP450-IN-1 (compound 2e) is a potent inhibitor of CYP450.
    CYP450-IN-1
  • HY-W014566
    4-Nitro-3-(trifluoromethyl)phenol
    		Inhibitor 99.91%
    4-Nitro-3-(trifluoromethyl)phenol (TFM) is a piscicide that is toxic to lampreys (P. marinus) (LC50 values ??are 1.97-2.11 for cysts, 2.05-2.21 for fry, 1.6-2.45 for juveniles, and 1.6-1.63 for adults, respectively). 4-Nitro-3-(trifluoromethyl)phenol is also toxic to juvenile lake sturgeons (A. fulvescens) less than 100 mm, but is nontoxic to a variety of other fish species. 4-Nitro-3-(trifluoromethyl)phenol (50 μM) dissociates oxidative phosphorylation by 22% and 28% in isolated livers of lampreys and rainbow trout (O. mykiss), respectively. 4-Nitro-3-(trifluoromethyl)phenol can be used to control lamprey larval populations.
    4-Nitro-3-(trifluoromethyl)phenol
  • HY-13832R
    Atovaquone (Standard)
    		Inhibitor
    Atovaquone (Standard) is the analytical standard of Atovaquone. This product is intended for research and analytical applications. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and  P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia.
    Atovaquone (Standard)
  • HY-B1234S
    Octinoxate-13C,d3
    		Inhibitor
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). 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-<sup>13</sup>C,d<sub>3</sub>
  • 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-122932
    Neoquassin
    Neoquassin is found in Picrasma quassioides.
    Neoquassin
  • 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-119536
    Norsufentanil
    Sufentanil is a potent synthetic opioid analgesic. Norsufentanil, a metabolite of sufentanil, is produced by the oxidative N-dealkylation of the liver cytochrome P450 isomer. Norsufentanil has analgesic activity.
    Norsufentanil
  • 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-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)
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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