CYP1
Cytochrome P450 CYP1 enzymes comprise the CYP1A1, CYP1A2, and CYP1B1 isoforms, which function as heme-containing monooxygenases that catalyze the oxidation of endogenous molecules and xenobiotics during phase I metabolism[1][2]. Mechanistically, CYP1 enzymes are induced through aryl hydrocarbon receptor (AhR) signaling and participate in the metabolism of polycyclic aromatic hydrocarbons, aromatic amines, steroid hormones, eicosanoids, and numerous therapeutic compounds[1]. Through these reactions, CYP1 family members contribute to both detoxification and the bioactivation of procarcinogens, thereby influencing chemical toxicity, mutagenesis, and carcinogenesis[1][3]. In disease contexts, altered CYP1 activity has been linked to cancer susceptibility, drug response variability, and other pathological processes associated with endogenous signaling molecules and environmental exposures[1][3]. Compared with related isoforms, CYP1A1, CYP1A2, and CYP1B1 share substantial sequence similarity and overlapping substrate selectivity, yet they exhibit distinct functional properties, protein-protein interactions, tissue distribution patterns, and catalytic behaviors[2][4]. CYP1A2 is constitutively expressed in the liver and plays a major role in xenobiotic metabolism, whereas CYP1A1 and CYP1B1 are more strongly associated with extrahepatic metabolism and procarcinogen activation[1][2]. For experimental applications, selective CYP1 inhibitors and isoform-specific probes are widely used to dissect CYP1-dependent metabolic pathways, evaluate enzyme selectivity, and investigate mechanisms of drug efficacy, toxicity, and cancer biology[1][5].
References:
- [1]. Kwon YJ, et al. Biological roles of cytochrome P450 1A1, 1A2, and 1B1 enzymes. Arch Pharm Res. 2021 Jan;44(1):63-83. [Content Brief]
- [2]. Deguchi S, et al. Modeling of Hepatic Drug Metabolism and Responses in CYP2C19 Poor Metabolizer Using Genetically Manipulated Human iPS cells. Drug Metab Dispos. 2019 Jun;47(6):632-638. [Content Brief]
- [3]. Nebert DW, et al. The role of cytochrome P450 enzymes in endogenous signalling pathways and environmental carcinogenesis. Nat Rev Cancer. 2006 Dec;6(12):947-60. [Content Brief]
- [4]. Valenzuela B, et al. Isolation and Characterization of Thermus thermophilus Strain ET-1: An Extremely Thermophilic Bacterium with Extracellular Thermostable Proteolytic Activity Isolated from El Tatio Geothermal Field, Antofagasta, Chile. Int J Mol Sci. 2023 Sep 25;24(19):14512. [Content Brief]
- [5]. Dutour R, et al. Inhibitors of cytochrome P450 (CYP) 1B1. Eur J Med Chem. 2017 Jul 28;135:296-306. [Content Brief]
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CYP1 Related Products (93)
Related Products (93)
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Antibodies (1)
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DMU2139
0 ImagesDMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
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Polyphyllin H
0 ImagesPolyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 μM, competitive), CYP2D6 (IC50 = 13.88 μM, competitive) and CYP3A4 (IC50 = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel.
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Quinestrol
0 ImagesQuinestrol (W-3566) is an orally effective synthetic estrogen compound that acts on CYP3A4, CYP1A2, and GnRH. Quinestrol interferes with GnRH release and disrupts the hypothalamic-pituitary-ovarian axis. Quinestrol downregulates the gene expression of follicle-stimulating hormone β and luteinizing hormone β, induces oxidative stress, damages reproductive organs, reduces sperm density and motility, increases sperm malformation rate, and alters the levels of sex hormones such as testosterone, luteinizing hormone, estradiol, and progesterone. Quinestrol can be used in studies related to reproductive function regulation.
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CYP1B1-IN-4
0 ImagesCYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes.
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Dibenzothiophene
0 ImagesDibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with a 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.
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ε-Viniferin
0 ImagesSynonyms: epsilon-Viniferinε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.
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PY109
0 ImagesPY109 is an orally active and highly selective aryl hydrocarbon receptor (AHR) agonist. PY109's EC50 values in human-derived HepG2 and mouse Hepa-1c1c7 cells are 1.2 nM and 1.4 nM respectively. PY109 significantly upregulates the expression of CYP1A1 and IL-22, and inhibits the expression of IL-17A. PY109 significantly improves colitis in mice. PY109 can be used for research on colitis.
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Gemfibrozil (Standard)
0 ImagesSynonyms: CI-719 (Standard)Gemfibrozil (Standard) is the analytical standard of Gemfibrozil. This product is intended for research and analytical applications. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
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BI 653048
0 ImagesBI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
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CYP1B1 ligand 3
0 ImagesCYP1B1 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).
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DMU2105
0 ImagesDMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
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Phortress
0 ImagesSynonyms: NSC 710305Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.
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17-HETE
0 ImagesCat. No.: HY-116196CAS No.: 128914-47-617-HETE is arachidonic acid metabolite through cytochrome P-450 pathways, which consists of 17R-HETE and 17S-HETE enantiomers. 17-HETE serves as allosteric activator of the cytochrome P450 1B1 and inhibitor of ATPase, induces cardic hypertrophy.
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Chalepensin
0 ImagesChalepensin is a nematicide and CYP inhibitor. Chalepensin inhibits CYP2A6, CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees, with IC50 values of 82.3 μM, 2.86 μM, 3.01 μM, 0.21 μM, 6.58 μM, 1.67 μM, 61.1 μM, and 61.7 μM, respectively. Chalepensin potently and selectively kills third-stage infective larvae of Strongyloides venezuelensis.
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7-Epi-docetaxel
0 ImagesSynonyms: 4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere7-Epi-docetaxel (4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere) is the major C7 epimeric impurity/in vivo metabolite of Docetaxel (HY-B0011). 7-Epi-docetaxel acts as a potent allosteric activator of rhCYP1B1. 7-Epi-docetaxel exhibits certain cell line-specific anti-migratory activity. 7-Epi-docetaxel can be used in research related to melanoma and lung adenocarcinoma.
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2,6-Dimethylnaphthalene-d12
0 Images2,6-Dimethylnaphthalene-d12 is the deuterated-labeled 2,6-Dimethylnaphthalene (HY-W017280). 2,6-Dimethylnaphthalene is a cytochrome P450 1A2 (CYP1A2) inhibitor, with an IC50 of 52 μM and a pIC50 of 4.28 against human targets. 2,6-Dimethylnaphthalene inhibits the 7-ethoxyresorufin O-dealkylation activity catalyzed by CYP1A2.
