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 (96)
Related Products (96)
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Antibodies (1)
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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.
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TRPV1 antagonist 10
0 ImagesTRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.
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3-Methylquinoline
0 Images3-Methylquinoline is a selective cytochrome P450 (CYP1A2) inhibitor with an IC50 of 13 μM. 3-Methylquinoline can reduce the metabolic clearance of CYP1A2 substrate drugs. 3-Methylquinoline can inhibit the activation of carcinogenic precursors.
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Resorufin methyl ether
0 ImagesResorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate. Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents.
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Dimethocaine
0 ImagesDimethocaine (Larocaine) is a cocaine derivative and ester-type local anesthetic. Dimethocaine is metabolized by hP450 1A2, 2C19, 2D6, and 3A4 in vitro. Dimethocaine exhibits locomotor-promoting, reinforcing, and anxiogenic effects.
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4,5-Dimethoxycanthin-6-one
0 Images4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae).
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Sudan IV (Standard)
0 ImagesSudan IV (Standard) (Solvent Red 24 (Standard)) is the analytical standard of Sudan IV (HY-D0932). This product is intended for research and analytical applications. Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.
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γ-Dodecanolactone
0 ImagesCat. No.: HY-W275481CAS No.: 2305-05-7
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Aurofusarin
0 ImagesCat. No.: HY-120805CAS No.: 13191-64-5Aurofusarin is a secondary metabolite. Aurofusarin catalytically inhibits topoisomerase II alpha, induces CYP1A1, p53, oxidative stress, DNA damage, and glutathione redox shift, intercalates into DNA, and causes S phase reduction accompanied by cytoskeletal/nuclear condensation. Aurofusarin disrupts intestinal epithelial barrier integrity, acts additively with deoxynivalenol, reduces mitochondrial activity, is cytotoxic to colon cells, and inhibits probiotic Gram-positive bacteria through outer membrane penetration without affecting Gram-negative bacteria. Aurofusarin can be used in research on colon cancer and bacterial infections.
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ML252 hydrochloride
0 ImagesCat. No.: HY-18063ACAS No.: 2309887-61-2ML252 hydrochloride is a selective inhibitor of KCNQ2 (Kv7.2) channel with IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 hydrochloride also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 hydrochloride shows highly brain penetrant.
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Saccharolactone
0 ImagesSaccharolactone is a potent orally active β-glucuronidase inhibitor. Saccharolactone markedly lowers biliary endogenous β-glucuronidase activity in the rat bile. Saccharolactone can stabilize glucuronide metabolites in vitro. Saccharolactone is also a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms (IC50 < 4 mM).
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CYP11B1-IN-2
0 ImagesCat. No.: HY-151140CAS No.: 3031098-46-8CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol.
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CYP1A1-IN-2
0 ImagesCat. No.: HY-148595CAS No.: 1422527-87-4CYP1A1-IN-2 (Compound 14) is a competitive inhibitor of CYP1A1 (Ki: 1.4 μM). CYP1A1-IN-2 exhibits potent antimitotic activity and arrests cell in the G2/M phase. CYP1A1-IN-2 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells.
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CYP1B1-IN-12
0 ImagesCat. No.: HY-175836CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC).
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Anticancer agent 318
0 ImagesCat. No.: HY-183304CAS No.: 2482789-24-0Anticancer agent 318 (Compound 8 (6)) is a selective anticancer agent. Anticancer agent 318 can be metabolized by CYP1A1, CYP1A2 and CYP1B1. After bioactivation, Anticancer agent 318 exerts antiproliferative activity in breast cancer cells expressing CYP1. Anticancer agent 318 can be used in the research of breast cancer.
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1,4-Dihydroxy-2-naphthoic acid (Standard)
0 Images1,4-Dihydroxy-2-naphthoic acid (Standard) is the analytical standard for 1,4-Dihydroxy-2-naphthoic acid (HY-W014701). 1,4-Dihydroxy-2-naphthoic acid is an orally active aryl hydrocarbon receptor (AhR) agonist and a bifidogenic growth stimulator. 1,4-Dihydroxy-2-naphthoic acid can improve the motor dysfunction in parkinson's disease (PD) model through AhR-dependent and -independent pathways. 1,4-Dihydroxy-2-naphthoic acid exerts anti-inflammatory effects by regulating the gut microbiota (such as promoting the proliferation of Bifidobacterium) and directly regulating the host immune system. 1,4-Dihydroxy-2-naphthoic acid induces apoptosis through G0/G1 cell cycle arrest in human keratinocyte to inhibit psoriasis.
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CYP1B1-IN-11
0 ImagesCat. No.: HY-175760CYP1B1-IN-11 (Compound M2) is a selective CYP1B1 inhibitor with an IC50 of 0.00605 pM. CYP1B1-IN-11 effectively reverses DMBA (HY-W011845)-induced Paclitaxel (HY-B0015) resistance and CYP1B1-IN-11 suppresses tumor cells invasion and migration. CYP1B1-IN-11 can be used for tumor drug resistance research.
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CYP1B1-IN-2
0 ImagesCat. No.: HY-150558CAS No.: 727730-24-7CYP1B1-IN-2 (compound 9j) is a potent and selective CYP1B1 (cytochrome P450 1B1) inhibitor, with an IC50 of 0.52 nM.
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CYP1B1-IN-5
0 ImagesCYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM.
