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-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 98.74%
    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-175064
    3,4-Methylenedioxyphenmetrazine hydrochloride
    Inhibitor
    3,4-Methylenedioxyphenmetrazine (3,4-MDPM) hydrochloride is a psychoactive substance. 3,4-Methylenedioxyphenmetrazine exhibits strong CYP2D6 inhibition and moderate inhibition of CYP3A4 and CYP1A2.
    3,4-Methylenedioxyphenmetrazine hydrochloride
  • 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-B0859A
    MCPA sodium
    Activator
    MCPA sodium is an orally active phenoxyacetic acid herbicide. MCPA sodium interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA sodium increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA sodium can be used to control broadleaf weeds.
    MCPA sodium
  • 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-182728
    CD564
    Inhibitor
    CD564 (Compound 11b) is a cytochrome P450 CYP26A1 and CYP26B1 inhibitor, with IC50 values of 1.63 μM and 0.52 μM, respectively. Cytochrome P450 CYP26 enzymes clear all-trans retinoic acid (atRA).
    CD564
  • 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-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-N20617
    (2E,6E,10E)-12-Hydroxyfarnesol
    (2E,6E,10E)-12-Hydroxyfarnesol is a metabolite of Farnesol (HY-Y0248A). (2E,6E,10E)-12-Hydroxyfarnesol forms via CYP2E1- and CYP2C19-mediated ω-hydroxylation of Farnesol in mammalian systems, and via CYP2E1-catalyzed selective hydroxylation of Farnesol in mammalian cells. (2E,6E,10E)-12-Hydroxyfarnesol is produced by the endophytic fungus Aspergillus sp. AST0006. When cholesterol synthesis is blocked, (2E,6E,10E)-12-Hydroxyfarnesol acts as a precursor for the formation of α,β-dicarboxylic acid.
    (2E,6E,10E)-12-Hydroxyfarnesol
  • 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-W707554
    Ticlopidine hydrochloride-d6
    Ticlopidine hydrochloride-d6 is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
    Ticlopidine hydrochloride-d<sub>6</sub>
  • 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-W778179
    Benoxaprofen-13C,d3
    Inhibitor
    Benoxaprofen-13C, d3 is the 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms.
    Benoxaprofen-<sup>13</sup>C,d<sub>3</sub>
  • 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
  • HY-N10755A
    (±)-ε-Viniferin
    Inhibitor
    (±)-ε-Viniferin is a racemate of ε-Viniferin (HY-N3841). (±)-ε-Viniferin exhibits P450 inhibitory antioxidants, as well as hepato-protective and antimicrobial activities. (±)-ε-Viniferin has antibacterial and antibiofilm activity against Gram-positive bacteria Streptococcus pneumoniae with a MIC of 20 μM.
    (±)-ε-Viniferin
Cat. No. Product Name / Synonyms Application Reactivity

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