Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Herbicide
MCPA sodium is a phenoxyacetic acid herbicide that primarily targets plant cell metabolism. It disrupts membrane integrity, reduces ATP levels, and impairs redox balance, leading to effective control of broadleaf weeds. MCPA sodium also enhances hepatic cytochrome P-450 levels and increases the activities of aniline hydroxylase and 7-ethoxycoumarin O-deethylase, making it a valuable tool in agricultural research and development. -
CYP51 Inhibitor
CYP51-IN-21 is a potent inhibitor of cytochrome P450 51 (CYP51), demonstrating significant antifungal activity against various pathogenic fungi, including drug-resistant strains. By targeting CYP51, CYP51-IN-21 disrupts the biosynthesis of essential sterols, impairing fungal growth and viability. Additionally, CYP51-IN-21 effectively inhibits the formation of fungal biofilms, making it a valuable candidate for research in antifungal therapeutics and biofilm-related studies. -
CYP1A2 Inducer
Imiprothrin is a potent inducer of CYP1A2, known for its significant effects on metallothionein 1a expression. This compound exhibits genotoxic and cytotoxic properties, evident through the initiation of detoxification responses in rat hepatocytes and the induction of chromosomal aberrations and micronucleus formation in bone marrow cells. Additionally, Imiprothrin prompts oxidative stress, resulting in lipid peroxidation and reactive oxygen species production, which can adversely affect liver and kidney functions. Though it inhibits weight gain and can lead to high mortality in female mice at elevated doses, it has not shown carcinogenicity in rat studies, with sensitive toxicity biomarkers including aspartate aminotransferase and total protein. -
CYP3A4 Inhibitor
Dihydrocubebin is a selective inhibitor of cytochrome P450 3A4 (CYP3A4), a key enzyme involved in drug metabolism. Isolated from Piper cubeba, it demonstrates potent inhibitory effects, making it a valuable tool for studying CYP3A4-related metabolic processes. Its role in research applications includes evaluating drug interactions and understanding the metabolic pathways of pharmaceutical compounds. -
Aromatase (CYP19) Inhibitor
2-Methoxy-5-acetoxyfuranogermacr-1(10)-en-6-one is a potent aromatase (CYP19) inhibitor, exhibiting an IC50 value of 0.21 μM against human targets. This compound is particularly relevant for research in breast cancer, providing insights into estrogen synthesis regulation and its implications in cancer progression. Its use in preclinical studies may advance the understanding of therapeutic strategies targeting estrogen-dependent tumors. -
CYP1B1 Inhibitor
CYP1B1-IN-9 is a highly selective competitive inhibitor of CYP1B1, demonstrating an IC50 of 1.48 nM. It effectively inhibits the migration and invasion of A549/T cells and has been shown to resensitize cells resistant to Paclitaxel. Notable for its favorable pharmacokinetic properties, metabolic stability, and safety profile, CYP1B1-IN-9 serves as a valuable tool for investigating tumor-drug resistance mechanisms in cancer research. -
CYP2A6/MAO Inhibitor
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate functions as an irreversible inhibitor of CYP2A6, exhibiting IC50 values of 8.64 μM and 22.3 μM under pre-incubation and co-incubation conditions, respectively. Additionally, this compound demonstrates inhibitory activity against monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B), with IC50 values of 60.2 μM and 38.6 μM, respectively. It serves as a valuable tool for research involving drug metabolism, neurochemistry, and the study of pharmacological responses influenced by these metabolic pathways. -
CYP2C9/CYP3A4 Inhibitor
GW694481 is a selective inhibitor of CYP2C9 and CYP3A4, exhibiting IC50 values of 2.1 μM and 17.0 μM, respectively. This compound functions as an ApoA1 upregulator, enhancing the expression of ApoA1 in human hepatic cells. GW694481 is valuable for research focused on atherosclerosis and related metabolic disorders, providing insights into lipid metabolism and cardiovascular health. -
RARβ/RARα Antagonist
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts. -
11β-HSD1 Inhibitor
11β-HSD1-IN-24 is a potent and selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with an IC50 of 0.5 nM. This compound effectively inhibits the conversion of inactive cortisone to active cortisol, making it a valuable tool for research in metabolic diseases, particularly type 2 diabetes. Its high selectivity and potency position it as an important reagent for studying the physiological roles of glucocorticoids in metabolic pathways. -
17β-HSD2 Inhibitor
11β-HSD2-IN-2 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2), demonstrating an IC50 of 300 nM. This compound plays a crucial role in modulating steroid metabolism and is valuable for research applications investigating hormonal regulation and related disorders. Its specificity makes it a useful tool for exploring the biological effects of 17β-HSD2 inhibition in various physiological contexts. -
11β-HSD1 Inhibitor
SKI2852 is a selective, orally active inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), exhibiting IC50 values of 1.6 nM for mouse HSD1 and 2.9 nM for human HSD1. This compound plays a critical role in the modulation of local glucocorticoid metabolism, making it valuable for research focused on metabolic diseases, obesity, and related disorders. Its potent inhibitory activity positions SKI2852 as a significant tool for investigating the physiological and therapeutic implications of 11β-HSD1 modulation. -
11β-HSD Inhibitor
Tetrahydro-11-dehydrocorticosterone is an inhibitor of the 11β-hydroxysteroid dehydrogenase (11β-HSD) enzyme, which plays a critical role in the metabolism of corticosteroids. This compound is utilized in research to study the regulation of glucocorticoid action and its implications in metabolic disorders, stress response, and inflammation. By modulating 11β-HSD activity, it serves as a valuable tool for investigating the therapeutic potential of targeted interventions in hormone-related diseases. -
11β-HSD1 Inhibitor
BMS-770767 is an inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), which is implicated in the pathophysiology of type 2 diabetes. By selectively targeting 11β-HSD1, this compound modulates cortisol availability, influencing metabolic processes in liver and adipose tissue. BMS-770767 is utilized in research focused on obesity, metabolic syndrome, and diabetes-related conditions.
