Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Nampt Inhibitor
Nampt-IN-5 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), a crucial enzyme in the NAD+ biosynthesis pathway. It demonstrates significant biological activity with cellular IC50 values of 0.7 nM against A2780 cells and 3.9 nM against COR-L23 cells, indicating strong efficacy in targeting cancer metabolism. In addition, Nampt-IN-5 inhibits CYP3A4 activity, making it relevant for studies on drug metabolism and potential interactions. Research applications include cancer cell metabolism and the investigation of therapeutic strategies targeting NAD+ pathways. -
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. -
FXR Agonist
BMS-986339 is a potent agonist of the farnesoid X receptor (FXR), demonstrating oral bioactivity. This compound interacts with key residues, including His298 and Asn287, to exert its biological effects. BMS-986339 is utilized in research focusing on primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), making it valuable for studies related to anti-fibrotic pathways. -
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. -
CYP Inhibitor
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. -
CYP1A Inhibitor
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. -
Endogenous metabolite
11,12-DiHETE is an endogenous metabolite formed through cytochrome P450-mediated epoxide formation followed by epoxide hydrolase activity. This compound plays a critical role in various biological processes and has been implicated in inflammatory responses. Its research applications include studies on metabolic pathways, cardiovascular function, and the physiological effects of eicosanoids. -
Endogenous Metabolite
17(R)-HETE is an endogenous metabolite derived from arachidonic acid via cytochrome P-450 pathways. This compound is known for its role in promoting cardiac hypertrophy, although it demonstrates lower efficacy compared to its isomer, 17(S)-HETE. It serves as a valuable tool for studying cardiovascular biology and the mechanisms of cardiac muscle remodeling. -
CYP-17A1 Llyase Inhibitor
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 Inhibitor
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. -
CYP1A1 Inhibitor
(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 Inhibitor
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. -
CYP2B6 Inhibitor
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. -
Fasn/Cyp2e1/Cyp4a32 Binder
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. -
CYP1A2 Inhibitor
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. -
IDO1 Inhibitor
IDO1-IN-30 is a selective and potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), demonstrating an IC50 of 4.8 nM in SKOV3 cells. This compound exhibits minimal cytotoxicity in HepG2 cells at concentrations up to 25 µM and does not significantly inhibit CYP450 enzymes, including 3A4, 2C9, and 2D6. IDO1-IN-30 is suitable for studies focused on cancer immunotherapy and the modulation of inflammatory responses. -
CYP2C9 Inhibitor
Bifeprofen is a selective inhibitor of cytochrome P450 2C9 (CYP2C9), exhibiting dose-dependent inhibition with an IC50 value of 75 µM. This compound is utilized in pharmacological research to study drug metabolism and interactions mediated by CYP2C9. Its application may extend to understanding the implications of CYP2C9 inhibition in clinical settings, providing insights into personalized medicine and therapy optimization. -
CYP1A2 Inhibitor
3-Methylquinoline is a selective inhibitor of cytochrome P450 1A2 (CYP1A2) with an IC50 value of 13 μM. This compound is known to decrease the metabolic clearance of substrates processed by CYP1A2, thereby enhancing the pharmacological effects of these drugs. Additionally, 3-Methylquinoline is capable of inhibiting the activation of certain carcinogenic precursors, making it a valuable tool in cancer research and drug metabolism studies. -
CYP3A4 Inhibitor
5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that functions as a selective inhibitor of CYP3A4, impacting the hepatic metabolism of steroids. It demonstrates significant biological activity with an IC50 value of 7.8 μM, making it a valuable tool for research on testosterone metabolism and drug interactions. This compound is particularly useful for studies investigating the modulation of cytochrome P450 enzymes in pharmacological and toxicological contexts.
