Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HMG-CoA Reductase (HMGCR) Inhibitor
SKF 104976 is a selective inhibitor of HMG-CoA reductase (HMGCR), demonstrating significant inhibitory activity in biochemical assays. It effectively reduces cholesterol synthesis in Hep G2 cells by inhibiting the incorporation of [14C]acetate at concentrations as low as 2 nM, leading to the accumulation of lanosterol and a substantial decrease in HMGR activity by 40-70%. Importantly, SKF 104976 does not influence low-density lipoprotein uptake or degradation, indicating a distinct regulatory mechanism for HMGR and low-density lipoprotein receptors. This compound serves as a valuable tool for studying cholesterol metabolism and the regulation of sterol synthesis pathways in cellular models. -
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. -
Endogenous Metabolite
N-Methylnicotinamide is an endogenous metabolite primarily involved in thrombotic regulation through its antithrombotic properties. It functions by promoting the production and release of prostacyclin, which inhibits the development of arterial thrombosis. This compound is synthesized via the N-methylation of nicotinamide, catalyzed by N-methyltransferase, and plays a crucial role in the nicotinate and nicotinamide metabolic pathways, making it relevant for research in cardiovascular health and metabolic processes. -
Endogenous Metabolite
4-Hydroxyestradiol is an endogenous metabolite of estradiol that acts as a potent estrogen receptor antagonist. This compound exhibits carcinogenic properties and demonstrates mutagenic activity in breast epithelial cells, indicating its role in cellular transformation processes. Its competitive inhibition of estradiol binding to the estrogen receptor, with a Ki value of 0.48 nM, makes it a valuable tool for studying estrogen-related pathways and breast cancer biology. -
Endogenous Metabolite
Diclofenac acyl glucuronide (D-1-O-G) is an endogenous metabolite that results from the conjugation of diclofenac. This compound plays a significant role in the pharmacokinetics of non-steroidal anti-inflammatory drugs (NSAIDs) and is implicated in gastrointestinal toxicity, particularly small intestinal ulceration in rat models. It serves as a valuable tool for studying drug metabolism and the effects of NSAIDs on the digestive system in research applications. -
Levofloxacin Minor Metabolite
Levofloxacin N-oxide is a minor metabolite of the fluoroquinolone antibiotic Levofloxacin, primarily functioning as an antibacterial agent targeting DNA gyrase and topoisomerase IV. It demonstrates minimal genotoxic risks, which may provide insights into the safety profile of Levofloxacin. This compound is valuable for research applications focused on antibiotic metabolism and the mechanistic studies of bacterial resistance. -
Metabolin
5-Hydroxyomeprazole is the primary metabolite of Omeprazole, functioning as a proton pump inhibitor. It inhibits gastric acid secretion by targeting the proton pump in gastric parietal cells, thereby reducing acidity. This compound is valuable in research related to gastrointestinal physiology and pharmacokinetics, as well as in studies examining the effects of acid suppression on various physiological processes. -
Fungal Metabolites
O-Methylsterigmatocystin is a mycotoxin derived from the fungi Aspergillus flavus and Aspergillus parasiticus. It primarily acts by inhibiting protein synthesis, which can lead to cytotoxic effects in various biological systems. This compound is commonly used in research to study fungal metabolites, mycotoxin biosynthesis, and their impact on human health and the environment. -
Drug Metabolite
4-Desmethoxy Omeprazole is an active metabolite of the proton pump inhibitor Omeprazole, primarily targeting acid-related gastrointestinal disorders. This compound exhibits competitive inhibition of CYP2C19, with a Ki value ranging from 2 to 6 μM, influencing drug metabolism. Additionally, 4-Desmethoxy Omeprazole demonstrates antimicrobial activity by inhibiting the growth of both Gram-positive and Gram-negative bacteria, making it relevant for various pharmacological and microbiological research applications. -
HMG-CoA Inhibitor
tert-Butyl Pitavastatin is a potent inhibitor of HMG-CoA reductase, a key enzyme in the cholesterol biosynthesis pathway. As a metabolite of Pitavastatin, it demonstrates significant biological activity in lowering lipid levels and managing hyperlipidemia. This compound is primarily utilized in pharmacological studies to explore cholesterol regulation and the therapeutic effects of statins in cardiovascular disease research. -
Naloxegol Metabolite
N-Dealkylated-mPEG7-Naloxol is a metabolite of Naloxegol, functioning primarily as an opioid receptor antagonist. This compound is relevant for research involving opioid receptor modulation and can aid in investigating the pharmacokinetics and pharmacodynamics of Naloxegol. Its unique structural features make it suitable for applications in drug metabolism studies and the exploration of opioid receptor interactions. -
Stable Isotope
Omeprazole sulfone (methoxy-d3) is a deuterium-labeled metabolite of Omeprazole, a well-known proton pump inhibitor. This stable isotope is utilized to study metabolic pathways and pharmacokinetics of Omeprazole in various biological systems. Its unique labeling provides enhanced sensitivity and specificity in analytical applications, making it a valuable tool for researchers investigating drug metabolism and interactions. -
Stable Isotope
4-Desmethoxy Omeprazole-d3 is a deuterium-labeled form of 4-Desmethoxy Omeprazole, the active metabolite of the proton pump inhibitor Omeprazole. This compound primarily targets the CYP2C19 enzyme, exhibiting competitive inhibition with an inhibition constant (Ki) ranging from 2 to 6 μM. It has significant biological activity, including the suppression of gastric acid secretion and the inhibition of growth in both Gram-positive and Gram-negative bacteria. This reagent is valuable for studies involving drug metabolism, pharmacokinetics, and antimicrobial activity. -
Aldicarb Metabolite
Aldicarb sulfoxide is a metabolite of aldicarb that primarily interacts with glutathione-linked enzymes in CHO-K1 cells. This compound exhibits inhibitory activity against cholinesterase (ChE) and carboxylesterase (CaE), with an IC50 of 10 μM in zebrafish models. Its mechanism of action and biological activity make it a valuable tool for research on neurotoxicology and enzymatic regulation. -
Raloxifene Oxidative Ddegradation
Raloxifene N-Oxide is an oxidative degradation product of Raloxifene, functioning primarily as a selective estrogen receptor modulator (SERM). This compound is of particular interest in research related to estrogen signaling pathways, as it may provide insights into the metabolism and pharmacokinetics of Raloxifene. Its biological activity allows for the exploration of estrogen receptor interactions and implications in conditions such as osteoporosis and breast cancer. -
Raloxifene Metabolite
Raloxifene Bismethyl Ether hydrochloride is a metabolic derivative of Raloxifene, characterized by the absence of both hydroxyl groups, rendering it inactive at the estrogen receptor. This compound serves as a valuable tool for studying the pharmacokinetics and metabolic pathways of Raloxifene in various biological systems. It is particularly useful in research focused on estrogen receptor signaling and related physiological processes. -
Raloxifene Metabolite
Raloxifene 6,4'-Bis-β-D-glucuronide is a metabolite of Raloxifene, functioning primarily as a selective estrogen receptor antagonist. This compound is significant in research related to osteoporosis prevention and estrogen receptor modulation. It serves as an important tool for studying the pharmacokinetics and biological effects of Raloxifene in various cellular contexts. -
Fungal Metabolite
(3S,5S)-Octahydrocurcumin, a fungal metabolite derived from Curcuma longa, functions as a potent antioxidant. This compound exhibits significant biological activity, particularly in modulating oxidative stress pathways. Its unique properties make it a valuable tool in research focused on inflammation, neuroprotection, and the therapeutic potential of curcumin derivatives. -
Oxidative/Nitrosative Stress Biomarker
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal recognized as a biomarker for oxidative and nitrosative stress. It acts as both a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2) and can modulate various signaling pathways by forming covalent adducts with nucleophilic sites on proteins, nucleic acids, and membrane lipids. This compound is implicated in cancer biology, particularly through its influence on mitochondrial function, making it a valuable tool for research in cellular stress responses and oncogenesis. -
ALDH Inhibitor
4-Diethylaminobenzaldehyde is a reversible inhibitor of aldehyde dehydrogenases (ALDHs), exhibiting a Ki value of 4 nM specifically for ALDH1. This compound has demonstrated significant anti-androgenic activity with an IC50 of 1.71 μM. Its inhibitory effects on ALDH activities make it a valuable tool in biological research, particularly in studies focused on metabolic processes and hormonal regulation. -
ALDH1 Inhibitor
ABD-3001 is a selective inhibitor of aldehyde dehydrogenase 1 (ALDH1). It has demonstrated potential in the study of refractory or relapsed acute myeloid leukemia and high-risk myelodysplastic syndrome. This compound may serve as a valuable tool for elucidating the role of ALDH1 in hematological malignancies and developing targeted therapies. -
Acohol use disorder
Lefelsiran sodium is a small interfering RNA (siRNA) that targets aldehyde dehydrogenase 2 (ALDH2). It is utilized in research to investigate the mechanisms underlying alcohol use disorder. By downregulating ALDH2, Lefelsiran sodium may provide insights into metabolic pathways associated with alcohol consumption and the potential therapeutic approaches for treating alcohol-related conditions. -
ALDH1a2 Inhibitor
Win 18446 is a selective inhibitor of the testes-specific enzyme ALDH1a2, exhibiting an IC50 of 0.3 μM. This compound effectively reverses spermatogenesis across various species and disrupts the biosynthesis of retinoic acid from retinol within the testes. It is valuable for research applications focused on reproductive biology and the modulation of retinoid signaling pathways. -
ALDH18A1 Inhibitor
YG1702 is a selective inhibitor of ALDH18A1, a key enzyme involved in the biosynthesis of polyamines. This compound has demonstrated significant inhibitory effects on the proliferation of MYCN-amplified neuroblastoma cells and leads to down-regulation of MYCN expression. YG1702 binds to ALDH18A1 with high affinity, suggesting it may alter the enzyme’s activity and function. This reagent is valuable for research applications focused on neuroblastoma and cellular growth regulation. -
ALDH-2 Inhibitor
CVT-10216 is a highly selective, reversible inhibitor of aldehyde dehydrogenase-2 (ALDH-2), demonstrating an IC50 of 29 nM. This compound also exhibits inhibitory effects on ALDH-1 with an IC50 of 1.3 μM. CVT-10216 has been shown to reduce excessive alcohol consumption in alcohol-preferring rat models and exhibits anxiolytic properties, making it valuable for research into alcohol use disorders and anxiety-related conditions. -
ALDH3A1 Inhibitor
ALDH3A1-IN-3 is a selective inhibitor of the enzyme ALDH3A1, exhibiting a Ki value of 4.7 μM and an IC50 value of 16 μM. This compound shows no inhibitory activity against ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, or ALDH2 in vitro. ALDH3A1-IN-3 is suitable for investigations in cellular oxidation processes and cancer research, making it a valuable tool for studying the role of ALDH3A1 in various biological contexts. -
ALDH3A1 Inhibitor
ALDH3A1-IN-1 is a potent inhibitor of the aldehyde dehydrogenase 3A1 (ALDH3A1) enzyme, exhibiting an IC50 of 1.61 μM. This compound demonstrates superior efficacy compared to DEAB in targeting patient-derived primary prostate tumor epithelial cells, both as a standalone treatment and in combination with docetaxel. ALDH3A1-IN-1 is a valuable tool for investigating ALDH3A1's role in cancer biology and therapeutic resistance. -
ALDH1B1 Inhibitor
IGUANA-1 is a selective inhibitor of ALDH1B1, exhibiting potent activity against this target. It demonstrates minimal mitochondrial toxicity, making it suitable for various experimental applications. Its antitumor properties position IGUANA-1 as a valuable compound for cancer research and drug development. -
ALDH1A3 Inhibitor
ALDH1A3-IN-3 is a potent inhibitor of aldehyde dehydrogenase 1A3 (ALDH1A3), exhibiting an IC50 of 0.26 μM. This compound shows potential as a research tool for studying prostate cancer and can aid in understanding the role of ALDH1A3 in tumor biology. However, it functions as a substrate for ALDH3A1, which may limit its specificity as a selective inhibitor. -
ALDH1A3 Inhibitor
ALDH1A3-IN-1 is a potent inhibitor of aldehyde dehydrogenase 1A3 (ALDH1A3), exhibiting an IC50 value of 0.63 μM and a Ki of 0.46 μM. This compound plays a significant role in cancer research, particularly in the study of prostate cancer, by modulating metabolic pathways associated with tumor progression. Researchers can utilize ALDH1A3-IN-1 to explore the implications of ALDH1A3 inhibition in cellular and molecular contexts pertaining to oncology. -
ALDH1A1 Inhibitor
CM037 is a highly selective and competitive inhibitor of the enzyme ALDH1A1, with an IC50 of 4.6 μM. By blocking the catalytic activity of ALDH1A1, CM037 inhibits the activation of the HIF-1α/VEGF signaling pathway. This reagent is primarily utilized to investigate the role of ALDH1A1 in the regulation of cancer stem cells and angiogenesis, particularly in breast cancer models, highlighting its potential to obstruct tumor angiogenesis and stem cell properties. -
ALDH3A1 Inhibitor
EN40 is a selective inhibitor of aldehyde dehydrogenase 3A1 (ALDH3A1), functioning as a covalent ligand with an IC50 value of 2 µM. This compound demonstrates significant inhibitory activity, making it a valuable tool for research focused on cellular metabolism and oxidative stress. Its application extends to the study of various diseases where ALDH3A1 plays a role, providing insights into potential therapeutic interventions. -
ALDH1A Inhibitor
CM010 is a selective inhibitor of the aldehyde dehydrogenase 1A (ALDH1A) family, exhibiting IC50 values of 1700 nM, 740 nM, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. This compound does not inhibit other members of the ALDH family, making it a valuable tool for specific enzyme studies. CM010 demonstrates potential in regulating metabolic processes and exhibits anti-cancer activity, making it relevant for cancer research applications. -
Dehydrogenase
ALDH (Aldehyde dehydrogenase (NAD(P))) is an enzyme that catalyzes the oxidation of aldehydes into their corresponding carboxylic acids, simultaneously reducing the cofactors NAD(P) to NAD(P)H. This enzymatic activity is crucial for cellular detoxification and metabolism, making ALDH significant in biochemical research. It is frequently employed in studies investigating aldehyde stress responses and metabolic pathways related to aldehyde processing. -
ALDH1A3 Inhibitor
ALDH1A3-IN-2 is a selective inhibitor of aldehyde dehydrogenase 1A3 (ALDH1A3) with an IC50 of 1.29 μM. This compound demonstrates significant potential for studying the role of ALDH1A3 in various malignancies, particularly in prostate cancer where ALDHs are frequently overexpressed. ALDH1A3-IN-2 can be utilized in research focusing on cancer pathways and therapeutic strategies targeting ALDH-related enzymatic activity. -
ALDH1A3 Inhibitor
MCI-INI-3 is a selective competitive inhibitor of human ALDH1A3, exhibiting a Ki value of 0.55 μM for ALDH1A3 and a Ki value of 78.2 μM for ALDH1A1. This compound effectively disrupts retinoic acid biosynthesis, leading to a reduction in viability of glioblastoma stem cells GSC-83 and GSC-326. MCI-INI-3 is a valuable tool for research focused on cancer biology and the therapeutic targeting of glioblastoma. -
ALDH1A3 Inhibitor
KOTX1 is a selective inhibitor of the ALDH1A3 enzyme, demonstrating oral bioactivity. This compound has been shown to enhance glucose tolerance, promote insulin secretion, and regulate blood sugar levels in diabetic mouse models. KOTX1 is a valuable tool for investigating metabolic disorders and the role of ALDH1A3 in diabetes research. -
aldh1a1 Inhibitor
ALDH1A1-IN-2 is a selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), an enzyme crucial for the oxidation of cytotoxic aldehydes. By inhibiting ALDH1A1, this compound may contribute to studies focusing on cancer, inflammation, and obesity-related pathways. Its biological activity positions it as a valuable tool for researchers investigating the roles of ALDH enzymes in diverse pathophysiological conditions. -
aldehyde dehydrogenase inhibitor
Nitrefazole is a 4-nitroimidazole derivative functioning as a potent inhibitor of aldehyde dehydrogenase (ALDH). It exhibits strong and sustained inhibition of ALDH, an enzyme critical in alcohol metabolism. This compound is valuable for research applications focused on alcoholism, metabolic studies, and pharmacological modulation of ALDH activity. -
Stable Isotope
4-Hydroxynonenal-d3 is a deuterated form of 4-Hydroxynonenal, an α,β-unsaturated hydroxyalkenal recognized as a biomarker for oxidative and nitrosative stress. It serves as both a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2), influencing various signaling pathways by forming covalent adducts with nucleophilic sites in proteins, nucleic acids, and membrane lipids. As a significant player in cancer biology, 4-Hydroxynonenal impacts mitochondrial function and cellular signaling processes, making it valuable for research in oxidative stress and its implications in disease. -
Aldehyde Dehydrogenase (ALDH) Inhibitor
S-Methyl-N,N-diethylthiolcarbamate is an effective inhibitor of aldehyde dehydrogenase (ALDH). This compound serves as the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram, generated through the methylation of diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate exhibits significant biological activity, demonstrated by its ability to inhibit rat liver low Km ALDH with an ID50 value of 15.5 mg/kg. In vivo studies indicate that a dose of 20.6 mg/kg can reduce mean arterial pressure and elevate heart rate in rats under ethanol stimulation, highlighting its potential applications in cardiovascular and metabolic research. -
ALDH1A2 Inhibitor
ALDH1A2-IN-1 is a reversible inhibitor targeting the active site of ALDH1A2, demonstrating an IC50 of 0.91 μM and a Kd of 0.26 μM. This compound is characterized by multiple hydrophobic interactions, making it an effective tool for studying the enzyme's role in biological pathways. It is applicable in research focused on cancer metabolism, stem cell differentiation, and neurotransmitter synthesis modulation. -
ALDH1 B1 Inhibitor
IGUANA-1 free base is a selective inhibitor of aldehyde dehydrogenase 1 B1 (ALDH1 B1) with an IC50 value of 30 nM. This compound demonstrates significant anti-proliferative activity against SW480 colorectal cancer cells, achieving IC50 values of 2.46 μM under adherent conditions and 0.39 μM in spheroid cultures. IGUANA-1 free base is a valuable tool for cancer research, particularly in studying the role of ALDH1 B1 in tumor growth and progression. -
ALDH-2/MAO Inhibitor
7-Hydroxy-4-phenylcoumarin is a dual inhibitor of aldehyde dehydrogenase-2 (ALDH-2) and monoamine oxidase (MAO), demonstrating IC50 values of 1.5 µM and 0.5 µM, respectively. This compound exhibits significant biological activity that may influence cellular metabolism and neurotransmitter regulation. It is suitable for research applications focused on neuroprotection and metabolic studies. -
ALDH2 Agonist
ALDH2 activator 1 is an allosteric agonist of aldehyde dehydrogenase 2 (ALDH2). This compound enhances cardiac function and mitigates myocardial necrosis in murine models of myocardial ischemia-reperfusion. It holds potential for advancing research in cardiovascular diseases, particularly in the context of myocardial infarction. -
ALDH Enhancer
Taraxerone is an ALDH enhancer derived from Sedum sarmentosum. It significantly increases the activities of alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH), exhibiting EC50 values of 512.42 μM and 500.16 μM, respectively. This compound is valuable for studies focused on alcohol metabolism and enzyme regulation in biochemical research.
