Catalog No.
Product Name
Application
Product Information
Citations
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CYP450 Inhibitor
11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) serves as an activator for cytochrome P450 enzymes. This compound is known to upregulate the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, leading to significant biological effects such as cell hypertrophy in RL-14 cells. Due to its modulatory role in cytochrome P450 activity, 11-HETE holds potential applications in the study of cardiovascular diseases. -
CYP1A1 Inducer
Methysticin is a kavalactone derived from kava extract, primarily acting as an inducer of CYP1A1. This compound is relevant in studies investigating metabolic enzyme modulation and its impact on drug metabolism. Additionally, it has potential implications in understanding the biochemical pathways associated with liver function and detoxification processes. -
CYP17A1 Lyase Inhibitor
BMS-351 is a potent, orally active nonsteroidal inhibitor of CYP17A1 lyase, demonstrating IC50 values of 19 nM for human CYP17A1 and 4 nM for cynomolgus monkey CYP17A1. This compound is primarily utilized in research focused on castration-resistant prostate cancer, providing insights into hormonal regulation and potential therapeutic interventions in this challenging malignancy. -
CYP1B1 Inhibitor
(E/Z)-DMU2105 is a selective inhibitor of CYP1B1, demonstrating potent inhibition with an IC50 value of 10 nM in yeast-derived microsomes and 63.65 nM in live recombinant yeast and human HEK293 kidney cells. This compound is valuable for research focused on cancer, glaucoma, ischemia, and obesity, offering insights into the role of CYP1B1 in various biological processes. Its specificity and potency make it a suitable tool for elucidating the function of this key enzyme in disease contexts. -
CYP11B2 Inhibitor
CYP11B2-IN-2 is a potent inhibitor of the aldosterone synthase enzyme CYP11B2, exhibiting an IC50 value of 0.3 nM. This compound is labeled with 18F, enabling its application as a positron emission tomography (PET) tracer for the diagnosis of primary aldosteronism. Its high specificity and efficacy make it a valuable tool for research in endocrine disorders and adrenal function. -
CYP2C9/VKOR Inhibitor
10-Hydroxywarfarin is a potent inhibitor of CYP2C9 and vitamin K epoxide reductase complex 1 (VKOR), exhibiting IC50 values of 1.6 µM and 80 ng/mL, respectively. This compound serves as a valuable tool in pharmacological research, particularly in studies related to anticoagulation therapies and vitamin K metabolism. Its role in influencing coagulation pathways makes it relevant for investigations into therapeutic strategies for thrombosis and related disorders. -
CYP1B1 Inhibitor
(E/Z)-DMU2139 is a potent and selective inhibitor of CYP1B1, exhibiting an IC50 value of 4 nM. This compound serves as a valuable tool for investigating the role of CYP1B1 in various biological processes and disease models. Its specificity and efficacy make it suitable for research aimed at understanding the mechanisms underlying CYP1B1-related pathways and the development of targeted therapies. -
CYP2C9 Inhibitor
Cloperidone is an inhibitor of cytochrome P450 2C9 (CYP2C9), demonstrating an IC50 of 17.7 μM. This compound has shown cytotoxic effects in HepG2 cells expressing CYP2C9, with a survival rate of 60% at a concentration of 10 μM. Cloperidone is valuable for studies investigating CYP2C9-related metabolic pathways and the effects of its inhibition in cellular models. -
CYP2B4/CYP2E1 Inhibitor
4-Phenyl-1,2,3-thiadiazole is an inhibitor of cytochrome P450 enzymes CYP2B4 and CYP2E1. This compound effectively obstructs the oxidation of 1-phenylethanol to acetophenone, making it valuable for studies related to drug metabolism and enzymatic activity. Its ability to selectively inhibit these enzymes positions it as a significant tool for research in pharmacology and toxicology. -
CYP4Z1 Inhibitor
CYP4Z1-IN-2 is a reversible inhibitor of the enzyme CYP4Z1, displaying a Ki value of 2.2 μM. This compound effectively reduces the production of 14,15-EET in breast cancer cells and demonstrates an IC50 of 5.9 μM in inhibiting the CYP4Z1-mediated Luc-BE O-debenzylation reaction. CYP4Z1-IN-2 serves as a valuable tool for research focused on the role of CYP4Z1 in cancer biology and associated signaling pathways. -
CYP11A1 Inhibitor
Opevesostat is a selective inhibitor of CYP11A1, designed for oral administration. This compound demonstrates significant potential in the study of metastatic castration-resistant prostate cancer (mCRPC), supporting research into therapeutic approaches targeting steroidogenesis. Its specificity for CYP11A1 makes it a valuable tool in understanding the biochemical pathways involved in androgen synthesis and cancer progression. -
CYP3A4 Inhibtior
Curcumenol is a potent inhibitor of CYP3A4, exhibiting an IC50 value of 12.6 μM. This bioactive compound, derived from Curcuma zedoaria, demonstrates neuroprotective, anti-inflammatory, anti-tumor, and hepatoprotective activities. In studies, Curcumenol suppresses Akt-mediated NF-κB activation and inhibits the p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells, making it a valuable tool for research in neuroinflammation and cancer therapy. -
CYP2C19 Inhibitor
(S)-(+)-N-3-Benzylnirvanol is a selective and competitive inhibitor of the cytochrome P450 isoform CYP2C19, exhibiting a Ki value of 250 nM. This compound displays low inhibition against other CYP isoforms, including CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4. It is primarily utilized in pharmacological research to study drug metabolism and drug-drug interactions involving CYP2C19. -
CYP2J2 Inhibitor
LKY-047 is a selective reversible inhibitor of cytochrome P450 2J2 (CYP2J2), exhibiting an IC50 of 1.7 μM. This compound demonstrates high specificity, remaining inactive against other human cytochrome P450 isoforms, including CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A. LKY-047 is utilized in research applications focused on understanding the role of CYP2J2 in drug metabolism and cardiovascular diseases. -
CYP3A4 Inhibitor
6',7'-Dihydroxybergamottin (6′,7′-DHB) is a furanocoumarin that acts as a potent inhibitor of the cytochrome P450 enzyme CYP3A4. This compound is instrumental in studying drug metabolism and interactions, making it valuable for research in pharmacokinetics and toxicology. Its ability to modulate CYP3A4 activity has implications for understanding the effects of herbal supplements and dietary compounds on drug efficacy and safety. -
CYP Epoxygenase Inhibitor
MS-PPOH is a selective inhibitor of cytochrome P450 epoxygenases, primarily targeting CYP2C8 and CYP2C9 with IC50 values of 15 μM and 11 μM, respectively. This compound demonstrates key biological activity through the modulation of enzymatic metabolism pathways, making it valuable for research in pharmacology and toxicology. Additionally, MS-PPOH features an alkyne group, enabling its application in click chemistry via copper-catalyzed azide-alkyne cycloaddition (CuAAc) for tagging and labeling in various biochemical assays. -
CYP11B2 Inhibitor
Lorundrostat is a selective inhibitor of CYP11B2, targeting aldosterone synthase. This compound exhibits significant antihypertensive activity and is primarily utilized in research focused on the management of high blood pressure and related cardiovascular conditions. Its ability to modulate aldosterone levels makes it a valuable tool in studying endocrine and cardiovascular function. -
CYP3Aa Inhibitor
Azamulin is an irreversible, highly selective inhibitor of human CYP3A4, effectively targeting this crucial cytochrome P450 enzyme. With IC50 values ranging from 0.03 to 0.24 μM, Azamulin exhibits potent CYP3A inhibition, making it a valuable tool in the study of drug metabolism and pharmacokinetics. Additionally, it holds potential for research in anti-infection therapies, providing insights into therapeutic strategies against infectious agents. -
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.
