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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
CYP11B1/CYP11B2 Inhibitor
Osilodrostat phosphate is a selective inhibitor of 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2), demonstrating an IC50 of 35 nM and 0.7 nM, respectively, for human enzymes. This compound effectively inhibits the synthesis of aldosterone and corticosterone, contributing to its role in blood pressure regulation. Osilodrostat phosphate is particularly valuable for research investigating Cushing syndrome and related disorders involving dysregulated steroidogenesis. -
CYP2D6 Inhibitor
Guanfu base A is a potent noncompetitive inhibitor of CYP2D6, with a Ki value of 1.20 μM in human liver microsomes and 0.37 μM for the recombinant form. This antiarrhythmic alkaloid, derived from Aconitum coreanum, also exhibits competitive inhibition of CYP2D in monkey and dog microsomes, with Ki values of 0.38 μM and 2.4 μM, respectively. In addition to its CYP2D6 inhibitory activity, Guanfu base A demonstrates the ability to inhibit HERG channel current, making it relevant for studies in drug metabolism and cardiac electrophysiology. -
CYP2D6 Inhibitor
Guanfu base A hydrochloride is a selective inhibitor of the CYP2D6 enzyme, demonstrating significant potential in the management of arrhythmia-related disorders. This alkaloid exhibits inhibitory effects across various species, including humans, primates, and canines. Its ability to modulate CYP2D6 activity may provide valuable insights and therapeutic applications in pharmacology and toxicology research. -
CypD Inhibitor
CypD-IN-5 is a selective inhibitor of cyclophilin D (CypD), a key regulator of mitochondrial permeability transition. This compound demonstrates significant potential in modulating mitochondrial function and may be particularly useful in studying neurodegenerative diseases such as Alzheimer's disease. Its application in research focuses on understanding the role of CypD in cellular stress responses and the underlying mechanisms of neurodegeneration. -
AR Degrader/CYP17A1 Inhibitor
YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context. -
CYP1A Inhibitor
Dibenzothiophene is a noncompetitive inhibitor of cytochrome P450 1A (CYP1A), effectively inhibiting CYP1A-mediated ethoxyresorufin O-deethylation (EROD) activity with a Km value of 0.592 μM. This compound interacts with the aryl hydrocarbon receptor (AHR) pathway and has been shown to enhance the embryotoxicity of β-naphthoflavone. Its acute toxicity in animal models underscores its relevance in research. Dibenzothiophene is primarily utilized in studies investigating the mechanisms of developmental toxicity in various organisms. -
Aromatase/CYP19 Inhibitor
(±) Homoeriodictyol is a potent inhibitor of aromatase (CYP19), an enzyme critical in estrogen biosynthesis. This compound is primarily utilized in breast cancer research to investigate estrogen-mediated pathways and their role in tumor growth. Its inhibitory activity makes it a valuable tool for studying therapeutic strategies targeting aromatase in hormone-related cancers.
