Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
CYP17A1 Substrate
11-Ketoprogesterone (11KP4) serves as a substrate for the enzymes CYP17A1 and 11β-HSD2, facilitating the conversion to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF), both of which exhibit glucocorticoid activity. This compound is pivotal for studies examining steroidogenesis and adrenal hormone metabolism. It is utilized in research applications focusing on hormonal regulation and related disorders, providing insights into steroid hormone biosynthesis pathways. -
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-4 is a potent and selective inhibitor of cyclophilin D (CypD), exhibiting high affinity with an IC50 of 0.057 μM. This compound is valuable in researching various conditions related to oxidative stress, neurodegenerative diseases, liver dysfunction, aging processes, autophagy, and diabetes. CypD-IN-4 facilitates the exploration of CypD's role in these pathologies, providing insights into potential therapeutic strategies. -
CypD Inhibitor
CypD-IN-3 is a potent and selective inhibitor of cyclophilin D (CypD), demonstrating high affinity with an IC50 value of 0.01 μM. This compound is valuable for studying a range of biological processes and diseases, including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes. Its specificity towards CypD makes it an important tool for elucidating the role of this target in various cellular functions and pathological conditions. -
CypE Inhibitor
CypE-IN-1 is a highly potent and selective inhibitor of cyclophilin E (CypE), exhibiting an IC50 of 0.013 μM and a Ki value of 0.072 μM. This compound is valuable for investigating the role of CypE in various pathological conditions, including oxidative stress, neurodegenerative diseases, liver disorders, aging processes, autophagy, and diabetes. Researchers can utilize CypE-IN-1 to explore therapeutic strategies targeting CypE-related pathways. -
CYP450 Interactor
7-Methoxyindole is a potent interactor of cytochrome P450 enzymes. This compound is utilized in research focused on drug metabolism and toxicity, as it plays a critical role in the modulation of enzymatic activity. Its pharmacological properties make it suitable for studies investigating the metabolic pathways of various xenobiotics and endogenous compounds. -
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. -
CYP2E1 Biomarker
2-Piperidone is an endogenous metabolite that serves as a biomarker for the activity of the cytochrome P450 enzyme CYP2E1. This compound is utilized in research applications aimed at understanding drug metabolism, toxicology, and the biochemical pathways involving liver function. Its relevance in pharmacokinetic studies makes it an important reagent for investigating the metabolic effects of various compounds. -
CYP17A1 Inhibitor
YM116 is a potent and orally active competitive inhibitor of CYP17A1, with a reported Ki of 0.38 nM. By specifically inhibiting the C17-20 lyase activity, YM116 effectively reduces the synthesis of adrenal androgens, leading to decreased serum testosterone levels and lower dehydroepiandrosterone sulfate concentrations. This compound is valuable for research applications involving androgen-related disorders and prostate health. -
CYP1B1 Degrader
PROTAC CYP1B1 degrader-2 is a VHL E3 ligase-based degrader targeting CYP1B1, exhibiting a DC50 of 1.0 nM in A549/Taxol cells after 24 hours. This compound effectively inhibits the growth, migration, and invasion of cancer cells, making it a valuable tool for research into the therapeutic potential of targeting CYP1B1 in cancer treatment. Its unique mechanism of action offers insights into the modulation of protein levels in various biological contexts. -
hCYP3A4 Inhibitor
hCYP3A4-IN-1 is a potent inhibitor of human cytochrome P450 3A4 (hCYP3A4) with notable activity in both human liver microsomes and CHO-3A4 stable cell lines, exhibiting IC50 values of 43.93 nM and 153.00 nM, respectively. This inhibitor effectively blocks CYP3A4-mediated hydroxylation of N-ethyl-1,8-naphthalimide (NEN) in a competitive manner, with a Ki of 30.00 nM. hCYP3A4-IN-1 is valuable for research applications focused on drug metabolism and interactions involving CYP3A4. -
CYP3A4 Inhibitor
Tabimorelin hemifumarate is a potent inhibitor of the cytochrome P450 enzyme CYP3A4. This compound functions as a growth hormone secretagogue, promoting the secretion of growth hormone in the body. Its key biological activities make it valuable for research applications in endocrine signaling and pharmacokinetics, particularly in studies assessing drug metabolism and interactions involving CYP3A4. -
CYP4A Hydroxylase Inhibitor
CAY 10434 is a potent inhibitor of CYP4A hydroxylase, demonstrating significant effects on vascular smooth muscle contractility. This compound enhances the contractile response to angiotensin II, achieving a maximal contractile response (Emax) of 6764 mg. CAY 10434 is valuable for research into cardiovascular physiology and the regulatory mechanisms underlying vascular reactivity. -
CYP11B2 Inhibitor
CYP11B2-IN-3 is a selective inhibitor of CYP11B2, demonstrating an IC50 value of 12.92 nM for CYP11B2 and 2341 nM for CYP11B1. This compound is orally active, making it suitable for in vivo studies. CYP11B2-IN-3 is primarily applicable in research related to hypertension, providing a valuable tool for investigating the role of CYP11B2 in adrenal steroidogenesis and blood pressure regulation. -
CYP1A2/CYP2D6/CYP3A4 Inhibitor
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM, while functioning as a competitive inhibitor of CYP1A2 and CYP2D6, with Ki values of 3.39 μM and 6.77 μM, respectively. This compound plays a significant role in pharmacological research by modulating drug metabolism pathways. Its ability to inhibit key cytochrome P450 enzymes makes it a valuable tool for studies examining drug interactions and metabolic regulation. -
CYP3A4 Inhibitor
Licopyranocoumarin is an isoflavonoid known for its inhibitory action on the cytochrome P450 enzyme CYP3A4, exhibiting an IC50 of 32 μM. This compound also demonstrates significant neuroprotective properties, making it a valuable reagent for studies focused on drug metabolism and neurodegenerative disorders. Researchers may utilize Licopyranocoumarin to explore its effects on enzyme activity and potential therapeutic applications in neurological research. -
CYP1B1 Inhibitor
CYP1B1-IN-1 is a selective inhibitor of cytochrome P450 1B1 (CYP1B1) with an IC50 value of 0.49 nM. This compound is valuable for studying the role of CYP1B1 in various biological processes, including the metabolism of xenobiotics and the activation of pro-carcinogens. CYP1B1-IN-1 is suitable for research applications focused on cancer biology and toxicology, providing insights into the pharmacological modulation of CYP1B1 activity. -
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. -
CYP2D6/AChE Inhibitor
Rhodiosin is a dual inhibitor of CYP2D6 and acetylcholinesterase (AChE), extracted from the root of Rhodiola rosea. It exhibits an IC50 value of 0.761 μM for CYP2D6 and a Ki of 0.769 μM. This compound demonstrates notable antioxidant and neuroprotective properties, contributing to the regulation of the HIF-1α signaling pathway, which is vital for central nervous system protection. Rhodiosin serves as a valuable tool for research in neuropharmacology and metabolic studies. -
Cypermethrin Isomer
(1R,2S,1'R)-Cypermethrin is a specific isomer of the pyrethroid pesticide Cypermethrin, classified as Class II due to its moderate toxicity. This compound exhibits significant neurotoxic activity by interacting with voltage-gated sodium channels, leading to prolonged neuronal depolarization. (1R,2S,1'R)-Cypermethrin is primarily employed in research focusing on its effects on nervous system function and insecticidal action. Its ability to cross the blood-brain barrier allows for studies on its impact on both invertebrate and vertebrate models.
