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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hCYP1B1-IN-2
0 ImagesCat. No.: HY-161649CAS No.: 3043683-33-3hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM.
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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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CYP1B1-IN-14 TFA
0 ImagesCat. No.: HY-181550ACYP1B1-IN-14 TFA is a metabolically stable hCYP1B1 competitive inhibitor with an IC50 of 1.32 nM and a Ki of 0.72 μM. CYP1B1-IN-14 TFA reverses the resistance of cancer cells to Paclitaxel (HY-B0015). CYP1B1-IN-14 TFA acts synergistically with Paclitaxel (HY-B0015) to inhibit tumor growth in xenograft models without obvious toxicity. CYP1B1-IN-14 TFA can be used for the research of cancers such as paclitaxel-resistant lung cancer.
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PAIB-SOs-12
0 ImagesCat. No.: HY-187120CAS No.: 1422528-30-0PAIB-SOs-12 is a CYP1A1-activated antimitotic prodrug with affinity for human CYP1A1, with a Ki value of 1.2 μM. PAIB-SOs-12 exhibits nanomolar antiproliferative activity in cancer cells expressing CYP1A1, with a selectivity ratio of over 100 against cancer cells that do not express CYP1A1. PAIB-SOs-12 undergoes CYP1A1-mediated N-dealkylation to form the active metabolite PIB-SO, which induces G2/M cell cycle arrest and microtubule disruption, and shows significantly improved stability in rodent liver microsomes compared to its n-butyl analog. PAIB-SOs-12 can be used in breast cancer-related research.
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CYP1B1-IN-3
0 ImagesCat. No.: HY-152079CAS No.: 2872575-51-2CYP1B1-IN-3 is a potent and selective CYP1B1 inhibitor with IC50 values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways.
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Antitumor agent-87
0 ImagesCat. No.: HY-148592CAS No.: 1422527-88-5Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity.
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1,2-Dimethylnaphthalene
0 ImagesCat. No.: HY-W142473CAS No.: 573-98-81,2-Dimethylnaphthalene is a CYP1A2 inhibitor with an IC50 of 5.5 μM and a pIC50 of 5.26.
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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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Imiprothrin
0 ImagesCat. No.: HY-119578CAS No.: 72963-72-5Imiprothrin is an inducer that induces CYP1A2 and metallothionein 1a, with significant genotoxicity and cytotoxicity. In rat hepatocytes, Imiprothrin initiates detoxification responses by triggering the overexpression of these two genes. Imiprothrin induces chromosomal aberrations and micronucleus formation in rat bone marrow cells, and causes DNA damage in hepatocytes. Imiprothrin triggers oxidative stress in rats, leading to lipid peroxidation, excessive reactive oxygen species production and redox imbalance, which in turn impairs liver and kidney functions and causes tissue damage. Imiprothrin inhibits weight gain in mice, and even causes high mortality in female mice at high doses. However, it shows no carcinogenicity in rat experiments; among relevant indicators, aspartate aminotransferase and total protein are identified as sensitive toxicity biomarkers.
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ZSTK3341
0 ImagesCat. No.: HY-188098ZSTK3341 is an aryl hydrocarbon receptor (AhR) and cytochrome P450 1A1 (CYP1A1) dependent cell growth inhibitor. ZSTK3341 exhibits growth inhibitory activity against cancer cells. ZSTK3341 can be used in the research of triple-negative breast cancer.
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BNS808
0 ImagesBNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding.
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BI 653048 phosphate
0 ImagesCat. No.: HY-12946ACAS No.: 1198784-97-2BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
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Galangin (Standard)
0 ImagesSynonyms: Norizalpinin (Standard); 3,5,7-Trihydroxyflavone (Standard)Galangin (Standard) is the analytical standard of Galangin. This product is intended for research and analytical applications. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
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CYP1B1-IN-9
0 ImagesCat. No.: HY-174425CAS No.: 3077254-39-5CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance.
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1,2,3,6,7,8-Hexachlorodibenzofuran
0 ImagesCat. No.: HY-W762015CAS No.: 57117-44-9Synonyms: 1,2,3,6,7,8-HxCDF1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 1,2,3,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC50s = 1.47 and 1.24 nM, respectively). 1,2,3,6,7,8-Hexachlorodibenzofuran reduces weight, induces thymic atrophy, and induces the expression of genes encoding the cytochrome P450 (CYP) isoform CYP1A1 and 4-chlorobiphenyl hydroxylase in rats (EC50s = 3.2, 0.9, 0.35, and 0.21 µmol/kg, respectively).
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Phortress free base
0 ImagesCat. No.: HY-128920CAS No.: 741241-36-1Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
