CYP2
Cytochrome P450 CYP2 comprises a major branch of the human cytochrome P450 superfamily and catalyzes Phase I oxidative metabolism of endogenous compounds and xenobiotics, thereby contributing substantially to drug clearance and chemical detoxification processes[1][2]. Mechanistically, CYP2 enzymes function as heme-dependent monooxygenases that convert lipophilic substrates into more hydrophilic metabolites, a key biochemical step that facilitates downstream elimination pathways and influences pharmacokinetic behavior[1]. Within drug-metabolizing pathways, CYP2 subfamily members, including CYP2C9, CYP2C19, and CYP2D6, participate in the metabolism of a large proportion of clinically used therapeutics and are major determinants of interindividual variability in drug response[1][2][3]. In disease-relevant and translational research models, genetic variation in CYP2 genes is closely associated with altered metabolic phenotypes, affecting drug efficacy, toxicity, and susceptibility to clinically significant drug-drug interactions[3][4]. Compared with related cytochrome P450 isoforms, CYP2 enzymes are distinguished by extensive genetic polymorphism and substrate selectivity, features that make them central targets in pharmacogenomics and precision medicine investigations[3][4]. For experimental applications, selective inhibitors and substrates are widely used to define CYP2-mediated metabolic pathways, characterize enzyme activity, and evaluate metabolism-dependent pharmacological or toxicological outcomes during drug discovery and development[1][4].
References:
- [1]. Zhao M, et al. Cytochrome P450 Enzymes and Drug Metabolism in Humans. Int J Mol Sci. 2021 Nov 26;22(23):12808. [Content Brief]
- [2]. Zanger UM, et al. Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation. Pharmacol Ther. 2013 Apr;138(1):103-41. [Content Brief]
- [3]. Zhou SF, et al. Polymorphism of human cytochrome P450 enzymes and its clinical impact. Drug Metab Rev. 2009;41(2):89-295. [Content Brief]
- [4]. Peter EK, et al. A Hybrid Hamiltonian for the Accelerated Sampling along Experimental Restraints. Int J Mol Sci. 2019 Jan 16;20(2):370. [Content Brief]
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CYP2 Related Products (144)
Related Products (144)
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Antibodies (1)
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Ginsenoside C-K (Standard)
0 ImagesCat. No.: HY-N0904RCAS No.: 39262-14-1Synonyms: Ginsenoside compound K(Standard); Ginsenoside K (Standard)Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
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FGFR-IN-10
0 ImagesCat. No.: HY-148597CAS No.: 2847092-41-3FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively.
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Ginsenoside Rd (Standard)
0 ImagesSynonyms: Gypenoside VIII (Standard)Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
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Antiproliferative agent-53-d3
0 ImagesCat. No.: HY-163816CAS No.: 2923508-77-2Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2-/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice.
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Oxolamine hydrochloride
0 ImagesOxolamine hydrochloride (SKF-9976 hydrochloride) is an orally active antitussive. Oxolamine hydrochloride can inhibit CYP2B1/2. Oxolamine hydrochloride has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine hydrochloride increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine hydrochloride can be used in respiratory disease research.
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Human CYP2C9, Reductase+b5
0 ImagesCat. No.: HY-E72098Human CYP2C9, Reductase+b5 refers to a near-physiological recombinant microsomal system co-expressed in insect cells, which consists of human cytochrome P450 2C9, NADPH-P450 oxidoreductase (CPR) and cytochrome b5. Human CYP2C9 is a human cytochrome P450 subtype belonging to the CYP2 family, and also a major metabolic enzyme. It is predominantly expressed in human liver and can metabolize a variety of active compounds.
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HIV-1 inhibitor-40
0 ImagesCat. No.: HY-147807CAS No.: 2789676-44-2HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity.
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Human CYP2C8, Reductase+b5
0 ImagesCat. No.: HY-E72097Human CYP2C8, Reductase+b5 refers to a near-physiological recombinant microsomal system co-expressed in insect cells, which consists of human cytochrome P450 2C8, NADPH-P450 oxidoreductase (CPR) and cytochrome b5. Human CYP2C8 is a human cytochrome P450 subtype belonging to the CYP2 family, and also serves as a major metabolic enzyme. It is predominantly expressed in human liver and is capable of metabolizing a variety of active compounds.
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BChE-IN-33
0 ImagesCat. No.: HY-159143BChE-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.
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(S)-Nornicotine (Standard)
0 ImagesCat. No.: HY-W040430RCAS No.: 494-97-3(S)-Nornicotine (Standard) is the analytical standard of (S)-Nornicotine (HY-W040430). This product is intended for research and analytical applications. (S)-Nornicotine is a nicotine metabolite that crosses the blood-brain barrier. (S)-Nornicotine weakly inhibits human CYP2A6 with a Ki >300 μM. (S)-Nornicotine promotes dopamine release in rat striatal and nucleus accumbens slices and increases endogenous DOPAC overflow through a calcium-dependent nAChR pathway that is sensitive to Mecamylamine (HY-B1395A). (S)-Nornicotine reduces behavioral responses maintained by nicotine or sucrose, exerts analgesic effects in persistent inflammatory pain and neuropathic pain models, and enhances the analgesic effect of morphine. (S)-Nornicotine is useful for research on tobacco dependence and pain.
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Paroxetine-d2
0 ImagesCat. No.: HY-111124CAS No.: 923932-43-8Synonyms: BRL29060-d2Paroxetine-d2 (BRL29060-d2) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.
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Gamma-heptalactone
0 ImagesSynonyms: γ-OenantholactonGamma-heptalactone (γ-Oenantholacton) is a selective cytochrome P450 2B6 (CYP2B6) inhibitor with an IC50 of 2400 μM.
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N,N-Diethylacetamide
0 ImagesCat. No.: HY-W008829CAS No.: 685-91-6N,N-Diethylacetamide is a polar solvent widely used in film and fiber manufacturing, as well as in laboratories as a carrier for water-insoluble chemicals. N,N-Diethylacetamide exerts potent anti-inflammatory effects by inhibiting the NF-κB pathway, suppressing the expression of NO and iNOS, and downregulating key inflammatory cytokines such as TNF-α and IL-6, without affecting the MAPK pathway. N,N-Diethylacetamide can be used to study inflammatory preterm birth.
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DL-Acetylshikonin
0 ImagesCat. No.: HY-N2181ACAS No.: 54984-93-9DL-Acetylshikonin is a non-selective, reversible cytochrome P450 inhibitor with IC50 values of 1.4-4.0 μM. DL-Acetylshikonin has anti-cancer and anti-inflammatory activities.
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RET-IN-31
0 ImagesCat. No.: HY-178786CAS No.: 2491726-04-4RET-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.
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(2E,6E,10E)-12-Hydroxyfarnesol
0 ImagesCat. No.: HY-N20617CAS No.: 69809-46-7(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.
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Polθ-IN-10
0 ImagesCat. No.: HY-181611CAS No.: 3068829-46-6Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers.
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Oxolamine
0 ImagesOxolamine (SKF-9976) is an orally active antitussive. Oxolamine can inhibit CYP2B1/2. Oxolamine has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine can be used in respiratory disease research.
