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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Human CYP1A1, Reductase+b5
0 ImagesCat. No.: HY-E72103Human CYP1A1, Reductase+b5 refers to a near-physiological recombinant microsomal system co-expressed in insect cells, consisting of human cytochrome P450 1A1, NADPH-P450 oxidoreductase (CPR) and cytochrome b5. Human CYP1A1 is a human cytochrome P450 subtype belonging to the CYP1 family, as well as a major metabolic enzyme. Its expression is concentrated in tissues such as lung, breast, placenta and endometrium, and it can metabolize polycyclic aromatic hydrocarbons and estrogens into carcinogenic intermediates with DNA-damaging activity.
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CYP1B1-IN-15
0 ImagesCat. No.: HY-187206CYP1B1-IN-15 is a CYP1B1 inhibitor with an IC50 of 1.47 nM, and it exhibits high selectivity against six major CYP subtypes. CYP1B1-IN-15 exerts competitive inhibitory effects by competing with substrates for binding to the active site of CYP1B1. CYP1B1-IN-15 enhances the inhibitory effect of Paclitaxel (HY-B0015) on the proliferation of paclitaxel-resistant cancer cells, and inhibits the migration and invasion of paclitaxel-resistant cancer cells. CYP1B1-IN-15 can be used in studies related to paclitaxel-resistant non-small cell lung cancer.
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AhR/PDE4 modulator-1
0 ImagesCat. No.: HY-189218AhR/PDE4 modulator-1 is a AhR/PDE4D dual-target modulator, with an AhR agonistic EC50 of 0.11 μM and a PDE4D inhibitory IC50 of 2.12 μM. AhR/PDE4 modulator-1 activates the AhR-CYP1A1 signaling pathway, promotes AhR nuclear translocation, and upregulates downstream CYP1A1; it inhibits PDE4D activity, elevates intracellular cAMP levels, and activates the downstream cAMP-PKA-CREB signaling pathway. Topical administration of AhR/PDE4 modulator-1 exerts anti-inflammatory effects in the Imiquimod (HY-B0180)-induced psoriasis-like mouse model, alleviates epidermal hyperplasia and inflammatory infiltration, and suppresses the expression of IL-17A/F. AhR/PDE4 modulator-1 can be used in research related to psoriasis.
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Human CYP1A2, Reductase+b5
0 ImagesCat. No.: HY-E72094Human CYP1A2, Reductase+b5 refers to a near-physiological recombinant microsomal system co-expressed in insect cells, consisting of human cytochrome P450 1A2, NADPH-P450 oxidoreductase (CPR) and cytochrome b5. Human CYP1A2 is a human cytochrome P450 subtype belonging to the CYP1 family, as well as a major metabolic enzyme. Its expression is centered in the human liver, and it can activate procarcinogens including aromatic heterocyclic amines and polycyclic aromatic hydrocarbons.
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17(S)-HETE
0 ImagesCat. No.: HY-116050CAS No.: 183509-25-317S-HETE is arachidonic acid metabolite through cytochrome P-450 pathways. 17S-HETE serves as allosteric activator of the cytochrome P450 1B1 and inhibitor of ATPase, induces cardic hypertrophy.
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Methysticin
0 ImagesCat. No.: HY-N0922CAS No.: 20697-20-5Synonyms: DL-Methysticin; (±)-MethysticiMethysticin is a major kavalactone in kava extract to induce CYP1A1.
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2,6-Dimethylnaphthalene
0 Images2,6-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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CYP1A1-IN-1
0 ImagesCat. No.: HY-174333CAS No.: 3065926-17-9CYP1A1-IN-1 (Compound 47) is a small-molecule cytochrome P4501A1 (CYP1A1) inhibitor. CYP1A1-IN-1 reduces the bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii by enhancing macrophage phagocytosis. CYP1A1-IN-1 is promising for research of sepsis caused by multidrug-resistant (MDR) bacteria.
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meso-Zeaxanthin
0 ImagesCat. No.: HY-167632CAS No.: 31272-50-1Synonyms: (3R,3′S)-Zeaxanthinmeso-Zeaxanthin ((3R,3′S)-Zeaxanthin) is an orally active xanthophyll carotenoid. meso-Zeaxanthin inhibits CYP1A1, CYP1A2, CYP2B1/2, COX-2, TNF-α and iNOS, and enhances the activities of Uridine diphosphate glucuronosyltransferase and Glutathione-S-transferase. meso-Zeaxanthin quenches oxygen free radicals. meso-Zeaxanthin filters short-wavelength blue light, alleviates oxidative damage and visual abnormalities. meso-Zeaxanthin reduces tumor incidence, prolongs tumor latency and survival rate of tumor-bearing mice, and inhibits paw edema. meso-Zeaxanthin can be used in research related to sarcoma and age-related macular degeneration.
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3-Bromocarbazole-d7
0 Images3-Bromocarbazole-d7 is the d7-labeled 3-Bromocarbazole (HY-33798). 3-Bromocarbazole is an inhibitor of the aryl hydrocarbon receptor (AHR). 3-Bromocarbazole induces the mRNA expression of CYP1A1 and CYP1B1, with EC50 values of 2500 nM and 1100 nM, respectively. 3-Bromocarbazole inhibits motor neuron axon length by downregulating the mRNA transcription levels of α1-tubulin, Gap43, Syn2a and shha in zebrafish larvae. 3-Bromocarbazole reduces central nervous system neurogenesis by downregulating the mRNA transcription levels of elavl3, nrd, mbp and gfap in zebrafish larvae. 3-Bromocarbazole induces developmental neurotoxicity and decreases body length in zebrafish larvae or embryos; at high concentrations, it also reduces hatching rate, and increases mortality and malformation rate. 3-Bromocarbazole can be used in studies related to developmental neurotoxicity and breast cancer.
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Sudan IV-d6
0 ImagesCat. No.: HY-D0932SCAS No.: 1014689-18-9Synonyms: Solvent Red 24-d6; C.I. 26105-d6Sudan IV-d6 (Solvent Red 24-d6) is the deuterium labeled Sudan IV(HY-D0932). 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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Versicolorin A
0 ImagesVersicolorin A is a biosynthetic precursor of Aflatoxin B1 (HY-N6615). Versicolorin A induces phosphorylation of p53. Versicolorin A activates the aryl hydrocarbon receptor AhR and significantly induces the expression of CYP1A1. Versicolorin A exerts genotoxic and cytotoxic effects. Versicolorin A enhances the genotoxicity of aflatoxin B1 in cells by promoting CYP450-mediated bioactivation of aflatoxin B1. Versicolorin A can be used in research related to colorectal cancer and hepatocellular carcinoma.
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Aceanthrenequinone
0 ImagesAceanthrenequinone is a polycyclic aromatic hydrocarbon quinone organic compound that belongs to the category of free radical photoinitiators. Aceanthrenequinone serves as an intermediate for dyes and pigments, and also acts as a substrate for organic synthesis and polymer materials. Aceanthrenequinone activates the Aryl Hydrocarbon Receptor pathway, induces the expression of CYP1A protein in the vascular system of zebrafish embryos, and causes the death of embryos at 120 hpf. Aceanthrenequinone is applicable to research related to industrial or biomedical applications.
