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-13632S
    Exemestane-d2
    		Inhibitor
    Exemestane-d2 is the deuterium labeled Exemestane. 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-d<sub>2</sub>
  • HY-N7128R
    Flavanone (Standard)
    		Inhibitor
    Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). lavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
    Flavanone (Standard)
  • HY-B1462S1
    Chlorzoxazone-13C
    Chlorzoxazone-13C is the 13C labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort.
    Chlorzoxazone-<sup>13</sup>C
  • HY-W699866
    Gemfibrozil 1-O-β-glucuronide-d6
    Gemfibrozil 1-O-β-glucuronide-d6 is the deuterium labeled Gemfibrozil 1-O-β-glucuronide (HY-129993). Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM.
    Gemfibrozil 1-O-β-glucuronide-d<sub>6</sub>
  • HY-W713284
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). 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.
    2-Ethylhexyl (E)-3-(4-(methoxy-d<sub>3</sub>)phenyl)acrylate
  • HY-178786
    RET-IN-31
    		Inhibitor
    RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RETWT, RETV804L, RETV804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers.
    RET-IN-31
  • HY-103392S
    Stiripentol-d9
    		Inhibitor
    Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Kis of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
    Stiripentol-d<sub>9</sub>
  • HY-156151
    CYP51/PD-L1-IN-3
    		Inhibitor
    CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death.
    CYP51/PD-L1-IN-3
  • HY-174332
    Cholesterol 24-hydroxylase-IN-3
    		Inhibitor
    Cholesterol 24-hydroxylase-IN-3 is an orally active, selective, and blood-brain barrier-penetrant CH24H inhibitor (IC50 = 23 nM) belonging to 1,3-oxazole derivatives. Cholesterol 24-hydroxylase-IN-3 competitively inhibits CH24H enzyme activity by using the 1,3-oxazole nitrogen atom to coordinate the heme iron and the cyclopropyl group occupying the hydrophobic pocket. Cholesterol 24-hydroxylase-IN-3 can be used for research on epilepsy and other neurological diseases.
    Cholesterol 24-hydroxylase-IN-3
  • HY-B1311R
    Proadifen hydrochloride (Standard)
    		Inhibitor
    Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases[4].
    Proadifen hydrochloride (Standard)
  • HY-N12443
    Antioxidant agent-18
    Antioxidant agent-18 (compound 5) is a flavonol glycoside with antioxidant activity isolated from Ginkgo biloba. Antioxidant agent-18 scavenges DPPH radicals (IC50: 15.8 μM) and reduces cytochrome c (IC50: 14.7 μM).
    Antioxidant agent-18
  • HY-N9434
    5,7,2',6'-Tetrahydroxyflavone
    		Inhibitor
    5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that inhibits hepatic testosterone 6β-hydroxylation (CYP3A4) activity with an IC50 of 7.8 μM.
    5,7,2',6'-Tetrahydroxyflavone
  • HY-172897
    EGFR/DHFR-IN-2
    		Inhibitor
    EGFR/DHFR-IN-2 (9b) is a dual h-DHFR/EGFRTK inhibitor, with IC50 values of 0.192 μM and 0.109 μM for h-DHFR and EGFR, respectively. EGFR/DHFR-IN-2 (9b) halts the cell cycle at the G1/S phase and induces apoptosis. EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. EGFR/DHFR-IN-2 (9b) can be used in the cancer research.
    EGFR/DHFR-IN-2
  • HY-162370
    CYP51-IN-16
    		Inhibitor
    CYP51-IN-16 (compound C6) is a phenylpyrimidine CYP51 inhibitor, and shows antifungal activity in in vitro. CYP51-IN-16 inhibits tumor cell growth.
    CYP51-IN-16
  • HY-N0153R
    Naringin (Standard)
    		Inhibitor
    Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1).
    Naringin (Standard)
  • HY-168188
    CYP51-IN-21
    		Inhibitor
    CYP51-IN-21 (Compound A33) is a potent CYP51 inhibitor. CYP51-IN-21 shows excellent antifungal activities against pathogenic fungi and drug-resistant strains. CYP51-IN-21 inhibits the formation of fungal biofilm.
    CYP51-IN-21
  • HY-17570R
    Desoximetasone (Standard)
    		Substrate
    Desoximetasone (Standard) is the analytical standard of Desoximetasone (HY-17570). This product is intended for research and analytical applications. Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.
    Desoximetasone (Standard)
  • HY-N6972R
    Cepharanthine (Standard)
    		Inhibitor
    Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM. Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model. Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects.
    Cepharanthine (Standard)
  • HY-B1812R
    Veratrole (Standard)
    		Substrate
    Veratrole (Standard) is the analytical standard of Veratrole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N10344
    Glucoarabin
    Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity.
    Glucoarabin
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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