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Cytochrome P450 (CYP) inhibitors act on heme enzymes that oxidize drugs, steroids and other lipophilic compounds. The name comes from the 450 nm absorption peak of a carbon monoxide-bound pigment, described in liver microsomes in 1964. Hepatic enzymes such as CYP3A4, CYP2C9 and CYP1A2 metabolize a large share of drugs and many environmental chemicals. Other members synthesize steroid hormones, among them CYP17A1, which is required for androgen production. The P450 system can also convert chemicals into toxic or carcinogenic metabolites, which links it closely to toxicology. Abiraterone inhibits CYP17A1, while clarithromycin and itraconazole serve as CYP3A4 inhibitors in drug-interaction studies. Alizarin is listed for its inhibition of enzymes in the CYP1 family.
CYP3A4-IN-2 is a selective inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting an IC50 value of 0.055 μM. As a ritonavir analogue, it possesses enhanced hydrophobicity in the R2 side group, resulting in a more potent inhibitory effect than ritonavir. This reagent is applicable in research focused on antiviral therapies and immunosuppressive mechanisms.
(-)-Vorozole is a selective inhibitor of cytochrome P450, specifically targeting aromatase. This non-steroidal compound exhibits significant antitumor activity in vivo and is primarily utilized in breast cancer research. Its potent inhibitory properties make it a valuable tool for investigating estrogen synthesis and its implications in various malignancies.
CYP1A1-IN-2 is a competitive inhibitor of CYP1A1 with a Ki value of 1.4 μM. This compound demonstrates significant antimitotic activity by effectively arresting cells in the G2/M phase of the cell cycle. Furthermore, CYP1A1-IN-2 disrupts microtubule integrity and the cytoskeletal structure in breast cancer cells that express CYP1A1, making it a valuable tool for studies on cancer biology and therapeutic resistance.
CYP11A1-IN-2 is a selective inhibitor of the cholesterol side-chain cleavage enzyme CYP11A1. This compound effectively inhibits steroid biosynthesis, making it a valuable tool for investigating steroid hormone-dependent cancers, including prostate cancer. Its application in research enables the exploration of novel therapeutic strategies targeting steroid pathways.
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CYP4Z1-IN-1 is a potent inhibitor of the cytochrome P450 enzyme CYP4Z1, exhibiting an IC50 of 41.8 nM. This compound effectively reduces the expression of cancer stem cell (CSC) markers associated with breast cancer, as well as inhibiting spheroid formation, metastatic potential, and tumor initiation capabilities in both in vitro and in vivo models. Its application in cancer research enhances understanding of CSC biology and potential therapeutic avenues targeting CYP4Z1.
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Synonyms: G297X
GW273297X is a selective inhibitor of CYP27A1, a key enzyme involved in cholesterol metabolism. This compound effectively reduces the concentration of 27-hydroxycholesterol (27HC) in E0771 tumor models in APOE3 mice. GW273297X serves as a valuable tool for investigating the role of CYP27A1 in breast cancer research and its potential impact on tumor progression and metabolism.
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Proadifen is a selective inhibitor of cytochrome P450 enzymes, impacting the metabolic activity of various substrates. Its inhibitory action can modulate the excitability of catecholamine-secreting neurons, potentially leading to differential effects across distinct brain regions. Proadifen is utilized in research to investigate the role of cytochrome P450 in neurotransmitter regulation and neuropharmacology.
3-Phenylthiophene is a selective inhibitor of CYP2A6 with a Ki value of 3.3 μM. It demonstrates minimal inhibition of other cytochrome P450 enzymes, including CYP2E1 (Ki 9.7 μM), CYP2B6 (Ki 14 μM), CYP2C9 (Ki 112 μM), and CYP2C19 (Ki 107 μM), while showing no significant activity against CYP3A4 and CYP2D6. This compound is valuable for research applications aimed at understanding smoking cessation mechanisms and the metabolism of nicotine.
CYP3A4-IN-3 is a potent and selective inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting an IC50 value of 0.075 μM. This compound, a modified analogue of ritonavir, demonstrates significantly enhanced inhibitory efficacy compared to its predecessor. CYP3A4-IN-3 is primarily utilized in antiviral research and immunosuppression studies, serving as a valuable tool for investigating drug metabolism and therapeutic interventions.
CYP1B1-IN-2 is a highly potent and selective inhibitor of cytochrome P450 1B1 (CYP1B1), exhibiting an IC50 of 0.52 nM. This compound is valuable for research exploring the role of CYP1B1 in various biological processes, including cancer metabolism and drug metabolism. Its specificity makes it a useful tool for studying CYP1B1-related pathways and potential therapeutic applications.
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Kushenol M is a flavonoid derived from Sophora flavescens, functioning primarily as a cytochrome P450 (CYP) inhibitor. It exhibits potent inhibitory activity, with an IC50 value of 1.29 μM specifically for CYP3A4 in human liver microsomes. This compound is valuable for research involving drug metabolism and pharmacokinetics, as well as studies assessing the interactions and regulation of CYP enzymes.
CYP1B1-IN-5 is a highly potent and selective inhibitor of cytochrome P450 1B1 (CYP1B1), exhibiting an IC50 of 4.7 nM. This compound is valuable for research applications aimed at understanding the role of CYP1B1 in various biological processes, including cancer metabolism and toxicity. Its specificity and efficacy make it an important tool for exploring CYP1B1's contributions to disease mechanisms and potential therapeutic interventions.
Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) with an IC50 value of 5.4 nM. This compound serves as a valuable tool for studying cholesterol metabolism and is particularly useful in imaging studies involving CH24H in mammalian systems. Its ability to selectively inhibit CH24H facilitates research on neurodegenerative diseases and related metabolic pathways.
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Ganolucidic acid B is a triterpenoid compound that acts as an inducer of CYP3A4 via activation of human PXR (hPXR). This compound is significant in the study of metabolic pathways and drug metabolism, making it a valuable reagent for research into the regulation of cytochrome P450 enzymes. Ganolucidic acid B is useful for investigating the effects of metabolic inducers on pharmacokinetics and drug-drug interactions.
CYP19A1-IN-1 is a selective inhibitor of CYP19A1, exhibiting an IC50 of 271 nM. By binding to CYP19A1, it effectively inhibits the conversion of androgens to estrogens. This reagent is valuable for research applications focused on estrogen-dependent diseases, including breast cancer, enabling studies on hormone regulation and potential therapeutic interventions.
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Antiproliferative agent-53-d3 is a selective inhibitor of cytochrome P450 enzymes CYP2C19 and CYP2C9, exhibiting IC50 values of 0.77 µM and 3.1 µM, respectively. This compound effectively inhibits theta-mediated end joining (TMEJ) in HEK293 cells, with an IC50 of 0.14 µM, and demonstrates significant antiproliferative effects on DNA repair-compromised BRCA2-/- DLD-1 cells, showing an IC50 of 8.1 µM. In addition, antiproliferative agent-53-d3 displays favorable pharmacokinetic properties in CD-1 mice, making it a valuable reagent for studies in cancer research and drug metabolism.
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Erysolin is a selective CYP1A inhibitor known for its antitumor properties. It effectively reduces benzo(a)pyrene-induced genotoxicity, making it valuable for research into the mechanisms of chemical carcinogenesis. Erysolin's ability to modulate CYP1A activity may provide insights into the metabolic pathways involved in drug metabolism and toxicity.
Synonyms: Vildagliptin carboxy acid metabolite TFA
Vildagliptin carboxylic acid metabolite TFA is a potent inhibitor of the cytochrome P450 enzyme system. This compound plays a crucial role in understanding the pharmacokinetics of vildagliptin and its metabolic pathways. Researchers can utilize it for studying drug-drug interactions and metabolic inhibition in various biological systems.
ASN-001 is an orally active CYP-17A1 lyase inhibitor that selectively targets testosterone synthesis. This compound exhibits notable anticancer activity, particularly in the context of prostate cancer research. Its specific mechanism of action makes ASN-001 a valuable tool for studying androgen-dependent malignancies and developing treatment strategies.
CYP3A4-IN-1 is a potent inhibitor of cytochrome P450 3A4 (CYP3A4), demonstrating an inhibition constant (IC50) of 0.085 µM. This compound is essential for studies involving drug metabolism and pharmacokinetics, particularly in the context of identifying potential drug-drug interactions. Its use can facilitate research in pharmacology and toxicology by evaluating the effects of CYP3A4 inhibition on various therapeutic agents.
Synonyms: (R)-6′,7′-DHB
(R)-6',7'-Dihydroxybergamottin is a competitive inhibitor of cytochrome P450 1A1 (CYP1A1) with inhibition constants (Kis) of 55 μM for human CYP1A1 and 1.72 μM for rat CYP1A1. This compound is primarily utilized in cancer research, offering insights into CYP1A1's role in cancer biology and pharmacology. Its inhibitory properties make it a valuable tool for studying CYP1A1-related pathways and cancer metabolism.
CYP1B1-IN-3 is a selective inhibitor of CYP1B1, exhibiting an IC50 of 6.6 nM for this target while demonstrating minimal activity against CYP1A1 and CYP1A2 with IC50 values of 347.3 nM and >10000 nM, respectively. This compound effectively inhibits cell migration and invasion, along with modulation of critical signaling pathways, including P-glycoprotein, AKT/ERK, FAK/SRC, and epithelial-mesenchymal transition (EMT). CYP1B1-IN-3 serves as a valuable tool for research applications focusing on cancer metastasis and the underlying mechanisms of CYP1B1 activity in various biological systems.
Synonyms: γ-Oenantholacton
Gamma-heptalactone is a selective inhibitor of cytochrome P450 2B6 (CYP2B6), exhibiting an IC50 of 2400 μM. This compound is valuable for studies investigating the metabolism of drugs by CYP2B6 and can aid in understanding the pharmacokinetics of various therapeutic agents. Its inhibitory properties make it a useful tool for exploring drug-drug interactions and metabolic pathways involved in the biotransformation of xenobiotics.
Floramanoside F is a flavonol glycoside that targets Fasn, Cyp2e1, and Cyp4a32, key enzymes associated with type 1 diabetic nephropathy. This compound exhibits a moderate free radical scavenging effect with an SC₅₀ of 25.1 μM and demonstrates weak inhibition of aldose reductase (IC₅₀ > 100 μM). By binding to these critical enzymes, Floramanoside F effectively inhibits lipid accumulation and oxidative stress, contributing to the reduction of renal inflammation and fibrosis. This reagent is valuable for research into mechanisms of type 1 diabetic nephropathy and related diabetic complications.
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1,2-Dimethylnaphthalene is identified as a potent inhibitor of CYP1A2, exhibiting an IC₅₀ of 5.5 μM and a corresponding pIC₅₀ of 5.26. This compound plays a significant role in studies focused on drug metabolism and enzyme inhibition. It is valuable for understanding the modulation of CYP450 enzymes in various physiological and pathological conditions.
