Catalog No.
Product Name
Application
Product Information
Citations
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CYP2E1 Inhibitor
Fomepizole hydrochloride is a potent inhibitor of cytochrome P450 enzyme CYP2E1. It functions as a competitive inhibitor of alcohol dehydrogenase, effectively preventing the metabolic conversion of methanol and ethylene glycol into harmful metabolites. This compound is primarily used in clinical settings as an antidote for poisoning due to methanol or ethylene glycol exposure, showcasing its significant biological activity in toxicology research. -
CYP2C19 Inhibitor
(±)-N-3-Benzylnirvanol acts as an inhibitor of the cytochrome P450 enzyme CYP2C19. This racemic mixture, comprised of both (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol, exhibits potent inhibitory activity with Ki values of 0.25 μM and 5.3 μM, respectively, for the respective enantiomers. It is valuable in pharmacological research aimed at understanding drug metabolism and potential drug-drug interactions involving CYP2C19. -
CYP2B6 Inhibitor
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible inhibitor of the human cytochrome P450 enzyme CYP2B6, displaying an IC50 value of 5.1 μM and a Ki of 5.6. In addition to its primary activity, this compound also moderately inhibits CYP2D6 and CYP3A, with IC50 values of 74 μM and 200 μM, respectively. This reagent is pertinent for research into drug metabolism and interactions involving CYP2B6 and other related P450 enzymes. -
CYP1B1 Inhibitor
CYP1B1-IN-4 is a selective CYP1B1 inhibitor, demonstrating a potent inhibitory activity with an IC50 value of 0.2 nM. This compound exhibits low cytotoxicity and maintains high stability in both human and rat liver microsomes, making it suitable for pharmacological studies. Its selectivity and stability position CYP1B1-IN-4 as a valuable tool for research into CYP1B1-related biological pathways and diseases. -
CYP4A11/CYP4F2 Inhibitor
TP0472993 is a potent and orally active dual inhibitor of cytochrome P450 enzymes CYP4A11 and CYP4F2, exhibiting IC50 values of 140 nM and 40 nM, respectively. This compound is valuable for investigating the role of these enzymes in renal diseases, contributing to a deeper understanding of their biological functions and potential therapeutic implications. Its selective inhibition profile makes TP0472993 a useful tool for studying the pharmacological effects related to cytochrome P450-mediated pathways. -
CYP2D6 Inhibitor
ONT-993 is a hydroxylated metabolite that primarily inhibits the cytochrome P450 enzyme CYP2D6, with an IC50 value of 7.9 µM. Additionally, ONT-993 induces metabolism-dependent inactivation of CYP3A, characterized by a KI of 1.6 µM. This compound is useful in research applications focused on drug metabolism and pharmacokinetics, particularly regarding interactions involving CYP450 enzymes. -
CYP11A1 Inhibitor
CYP11A1-IN-1 is an inhibitor of cytochrome P450 11A1 (CYP11A1), exhibiting an IC50 range of 201-2000 nM. This compound is valuable for research focusing on steroid hormone synthesis and the role of androgens in diseases such as prostate cancer. It offers potential applications in studies related to androgen receptor-dependent pathways and their therapeutic implications. -
hCYP3A4 Fluorogenic Substrate
hCYP3A4 Fluorogenic Substrate 1 is a potent substrate designed for human cytochrome P450 3A4 (hCYP3A4), exhibiting a Km value of 0.36 μM. This substrate is valuable for investigating hCYP3A4-mediated biotransformation processes and can be utilized in both cellular and in vivo imaging studies to monitor enzyme activity. Its fluorogenic properties facilitate real-time observation of metabolic activity, aiding in drug metabolism and pharmacokinetic research. -
CYP3A Biomarker
1β-Hydroxydeoxycholic acid (1β-OH-DCA) is a secondary bile acid and a recognized biomarker for the CYP3A enzyme family. It is primarily generated through the metabolism of deoxycholic acid via CYP3A4 and CYP3A7 employing recombinant human CYP450 enzymes. This compound serves as an important tool in pharmacokinetic studies and the evaluation of drug metabolism, facilitating research in drug interactions and personalized medicine involving CYP3A activity. -
CYP1A2 Inhibitor
2,6-Dimethylquinoline is a selective inhibitor of CYP1A2, exhibiting an IC50 of 3.3 µM. Additionally, it shows inhibitory activity towards CYP2B6 with an IC50 of 480 µM. This compound, derived from the roots of Peucedanum praeruptorum, serves as a valuable tool for research into drug metabolism and pharmacokinetics, particularly in studies exploring cytochrome P450 enzyme modulation. -
CYP17/CYP11B2 Inhibitor
Lapiteronel is a nonsteroidal, orally active inhibitor of CYP17 and CYP11B2, functioning as a reversible dual inhibitor. This compound exhibits significant biological activity in the modulation of steroid hormone synthesis, making it a valuable tool for research in metastatic castration-resistant prostate cancer. Its role in inhibiting critical enzymatic pathways positions Lapiteronel as a potential therapeutic agent in advancing cancer treatment studies. -
CYP2E1 Inhibitor
1-(Isothiazol-3-yl)ethan-1-one is a selective inhibitor of CYP2E1, an enzyme involved in the metabolism of various xenobiotics and endogenous compounds. This compound has demonstrated potential in modulating pathways relevant to oxidative stress and inflammation. Its applications extend to research on conditions such as rheumatoid arthritis and sepsis, providing insights into therapeutic strategies targeting these diseases. -
CYP17 Lyase Inhibitor
Seviteronel (R enantiomer) is a potent inhibitor of CYP17 lyase, with an h-Lyase IC50 value of 69 nM. This compound specifically targets the cytochrome P450 17A1 enzyme, crucial in steroidogenesis, and has applications in research focused on hormone-dependent cancers. Its efficacy in inhibiting steroid biosynthesis makes it a valuable reagent for studies investigating hormonal modulation and therapeutic interventions. -
CYP1B1 Inhibitor
CYP1B1 ligand 3 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1, exhibiting an IC50 of 11.9 nM. This compound is significant for research involving the modulation of CYP1B1 activity and serves as a valuable tool in the development of PROTAC CYP1B1 degrader-2. Its inhibitory properties make it suitable for studies related to drug metabolism and potential therapeutic applications. -
CYP1A1 Control Ligand
2-Hydroxybenzimidazole is a structural analog targeting CYP1A1, primarily utilized as a control ligand in structure-activity relationship studies of benzimidazole derivatives. This compound is inactive in terms of CYP1A1 induction, distinguishing it from other derivatives with thiol or amino substitutions. Its purpose is to serve as a baseline reference to better understand the biological activities of more active compounds in research applications. -
CYP2A6 Inhibitor
Chalepensin is a furanocoumarin that acts as a competitive inhibitor of the cytochrome P450 enzyme CYP2A6. In addition to its primary inhibitory effects on CYP2A6, Chalepensin has been shown to inhibit several other CYP enzymes, including CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4, albeit to varying degrees. This compound is valuable for research into drug metabolism and enzyme regulation, as well as for studies on the pharmacokinetics of therapeutic agents that undergo cytochrome P450-mediated biotransformation. -
PROTAC CYP1B1 Degrader
PROTAC CYP1B1 Degrader-1 is a targeted degrader designed to selectively eliminate cytochrome P450 1B1 (CYP1B1), utilizing a α-naphthoflavone chimera derivative. This compound exhibits IC50 values of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2, demonstrating its specificity in degrading CYP1B1. It serves as a valuable tool for investigating the role of CYP1B1 in prostate cancer and may aid in overcoming CYP1B1-mediated drug resistance in therapeutic applications. -
CYP1A2 Inhibitor
2,7-Dimethylnaphthalene is a selective inhibitor of the cytochrome P450 1A2 (CYP1A2) enzyme, exhibiting an IC50 of 65 μM. This compound is important for investigating metabolic diseases and understanding the role of CYP1A2 in drug metabolism and toxicity. Its application in research can provide insights into enzyme regulation and the pharmacokinetics of various substrates. -
CYP4A11/CYP4F2 Inhibitor
CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 enzymes CYP4A11 and CYP4F2, exhibiting IC50 values of 19 nM and 17 nM, respectively. This compound is valuable for studying the role of these enzymes in renal diseases and can aid in the development of targeted therapies. Its high specificity and effectiveness make it a crucial tool for researchers investigating cytochrome P450-mediated pathways. -
Aromatase/CYP19 Inhibitor
7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19), displaying an IC50 of 65 μM. This compound is known for its diverse biological activities, including anticarcinogenic and antioxidant properties, as well as exerting both estrogenic and anti-estrogenic effects. It is valuable for research applications focused on cancer biology, hormone regulation, and oxidative stress. -
CYP1B1 inhibitor
CYP1B1-IN-7 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1, exhibiting an IC50 value of 75 nM. This compound effectively reverses drug resistance in cancer cells, demonstrating an IC50 of 29 µM in the CYP1B1-overexpressing MCF-7 cell line resistant to Docetaxel. Its ability to induce cytotoxicity in resistant cell lines makes it a valuable tool for research on pharmacoresistance and the development of targeted cancer therapies. -
CYP3A4 Inhibitor
Thermopsoside is a flavone derivative that functions as a specific inhibitor of CYP3A4. Demonstrating inhibitory effects on various CYP450 isozymes, it exhibits IC50 values of 6.0 μM for CYP3A4, alongside inhibitory activities against CYP2C19, CYP2D6, and CYP2C9 at concentrations of 9.5 μM, 12.0 μM, and 32.0 μM, respectively. This compound is valuable for research focused on drug metabolism and pharmacokinetics, particularly in studies exploring drug interactions mediated by CYP450 enzymes. -
CYP17A1 Inhibitor
SU 10603 is a specific inhibitor of cytochrome P45017A1 (CYP17A1). It effectively blocks the enzymatic activity responsible for the conversion of pregnenolone and progesterone into androgens, thereby regulating steroidogenesis. This compound is utilized in research applications related to hormone-driven conditions such as prostate cancer and adrenal hyperplasia, facilitating studies on the modulation of androgen levels. -
CYP3A4 Inhibitor
Dasatinib analog-1 is a potent inhibitor of CYP3A4, achieving a Ki value of 5.4 μM. This compound effectively blocks the formation of glutathione adducts, making it valuable for studying drug metabolism and interactions. Its ability to modulate CYP3A4 activity positions it as a useful tool in pharmacological research and toxicology studies. -
CYP3A7 Substrate
N-Desmethyl diltiazem hydrochloride is a substrate for the enzyme CYP3A7, which is predominantly expressed during fetal development and has minimal expression in adult tissues. This compound is utilized in pharmacokinetic studies to investigate drug metabolism pathways in neonatal and fetal contexts. Its involvement in CYP3A7 activity makes it an important reagent for researchers examining developmental pharmacology and drug interactions. -
CYP2A6 Inhibitor
3-Methylbenzofuran is a specific inhibitor of the cytochrome P450 enzyme CYP2A6, exhibiting an IC50 of 7.35 μM. This compound is particularly relevant for studies investigating tobacco-related carcinogenesis, providing insights into metabolic pathways involved in the activation of tobacco-derived carcinogens. Its role in modulating CYP2A6 activity makes it a valuable tool in chemical research focused on cancer biology and pharmacology. -
CYP11B2 Inhibitor
CYP11B2-IN-1 is a potent inhibitor of CYP11B2, exhibiting an IC50 of 2.3 nM. Additionally, it demonstrates inhibitory activity against CYP11B1 with an IC50 of 142 nM. This compound is primarily utilized in research focused on steroidogenesis, hypertension, and cardiovascular diseases. Its selective inhibition properties make it a valuable tool for studying adrenal enzymatic pathways and developing therapeutic strategies. -
CYP2C8 Inhibitor
Clopidogrel-β-D-glucuronide is an inhibitor of the CYP2C8 enzyme. As a metabolite of Clopidogrel, it selectively binds to CYP2C8, resulting in significant inhibition of this liver enzyme's activity. This compound plays a crucial role in understanding drug metabolism and interactions, making it valuable for research applications in pharmacology and toxicology. -
CYP3A4 Inhibitor
Tabimorelin is a potent inhibitor of the CYP3A4 enzyme. This compound is recognized for its ability to act as an orally active growth hormone (GH) secretagogue, stimulating the release of GH in a physiological context. Its dual role as a CYP3A4 inhibitor has implications in drug metabolism studies and in understanding pharmacokinetic interactions. Tabimorelin is utilized in research related to endocrine function and therapeutic applications in conditions characterized by GH deficiency. -
CYP4A Hydroxylase Inhibitor
CAY 10462 dihydrochloride is a potent inhibitor of CYP4A hydroxylase. This compound enhances the contractile response to angiotensin II, demonstrating a maximal contractile response (Emax) at 6764 mg. CAY 10462 dihydrochloride is valuable for research focused on cardiovascular physiology and metabolic pathways involving cytochrome P450 enzymes. -
CYP1A2 Inhibitor
4,5-Dimethoxycanthin-6-one is a potent uncompetitive inhibitor of CYP1A2, exhibiting an IC50 value of 1.7 μM and a Ki value of 2.6 μM in phenacetin O-deethylation assays. This alkaloid, derived from the wood of Picrasma quassioides BENNET (Simaroubaceae), serves as a valuable tool for studying CYP1A2-mediated drug metabolism and interactions. Its inhibitory properties make it suitable for research applications in pharmacology and toxicology. -
CYP3A4 Substrate
Senkirkin is a pyrrolizidine alkaloid that serves as a substrate for the cytochrome P450 enzyme CYP3A4. It has been shown to induce chromosomal damage in lymphocytes, highlighting its potential utility in toxicological studies. This compound can be leveraged in research applications involving drug metabolism and the assessment of genotoxicity. -
CYP3A Inhibitor
Keto-itraconazole, a potent inhibitor of CYP3A, is a metabolite of Itraconazole. It demonstrates a significant unbound IC50 value of 4.6 nM when assessed using human liver microsomes in conjunction with midazolam. This compound is valuable for research focused on drug metabolism and interactions involving CYP3A-mediated pathways. -
CYP2A13 Inhibitor
Octahydrocoumarin is a potent inhibitor of the cytochrome P450 enzyme CYP2A13, exhibiting an IC50 value of 6.6 μM. This compound's inhibition of CYP2A13 makes it a valuable tool for investigating drug metabolism and potential interactions in chemical research. It is particularly relevant for studies related to the metabolism of various xenobiotics and therapeutic agents. -
CYP2A6 Inhibitor
CYP2A6-IN-2 is a selective inhibitor of the cytochrome P450 isoform CYP2A6. This compound is primarily utilized in research focused on elucidating the mechanisms underlying nicotine dependence and metabolism. Its inhibition of CYP2A6 may provide valuable insights into the pharmacological profiles of nicotine and other substrates metabolized by this enzyme, facilitating the development of therapeutic strategies for addiction and related disorders. -
CYP1A2 Inhibitor
γ-Dodecanolactone acts as an inhibitor of the cytochrome P450 enzyme CYP1A2, demonstrating an IC50 value of 58 µM and a pIC50 value of 4.24. This γ-lactone compound is suitable for studies investigating the biological implications of CYP1A2 inhibition, particularly in the context of diseases associated with this enzyme. Researchers can utilize γ-Dodecanolactone to explore metabolic pathways and drug interactions involving CYP1A2. -
CYP4A11/4F2 Inhibitor
CYP4A11/CYP4F2-IN-2 is a selective inhibitor of CYP4A11 and CYP4F2, exhibiting IC50 values of 120 nM and 220 nM, respectively. This compound effectively inhibits the production of 20-HETE in rat kidney models, demonstrating potential in research related to diabetic nephropathy and autosomal dominant polycystic kidney disease. Its oral bioavailability makes it a valuable tool for exploring the therapeutic effects of CYP4A11 and CYP4F2 inhibition in relevant biological conditions. -
CYP3A4 Inhibitor
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. -
CYP1A1 Inhibitor
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 Inhibitor
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. -
CYP4Z1 Inhibitor
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. -
CYP27A1 Inhibitor
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. -
CYP2A6 Inhibitor
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 Inhibitor
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 Inhibitor
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. -
CYP Inhibitor
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 Inhibitor
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. -
CH24H/CYP46A1 Inhibitor
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. -
CYP3A4 Inducer
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 Inhibitor
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.
