Catalog No.
Product Name
Application
Product Information
Citations
-
CPT-1 irreversible inhibitor
Etomoxir is an inhibitor of carnitine palmitoyltransferase A (CPT1), which is required for the oxidation of long-chain acyl CoA esters. Also a strong inhibitor of mitochondrial CPT1 and a candidate as an anti-diabetic drug.- Dina Baier, .et al. , Adv Sci (Weinh), 2023, Nov;10(32):e2301939 PMID: 37752764
- Theresa Mendrina, .et al. , Pharmaceutics, 2023, Feb 16;15(2):677 PMID: 36839999
- A. Geneste, .et al. , BMC Pharmacol Toxicol, 2020, 21: 61 PMID: 32795383
-
MGAT3 inhibitor
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM. -
ACAT1 Inhibitor
ATR-101 is in clinical development for the treatment of adrenocortical carcinoma (ACC). -
ACAT/SOAT inhibitor
CI 976 is a trimethoxy fatty acid anilide inhibitor of liver and intestinal acyl coenzyme A cholesterol acyltransferase (ACAT) and sterol O-acyltransferase (SOAT). Cl 976 lowers non-high density lipoprotein (non-HDL) cholesterol and increases HDL-cholesterol concentrations. -
ACAT inhibitor
Cyclandelate is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. -
Ghrelin O-acyltransferase (GOAT) inhibitor
GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer's disease, Parkinson's disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors. -
MGAT2 inhibitor
MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively. -
ACAT inhibitor
ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM. -
ACAT inhibitor
RP 73163 Racemate is the racemate of RP 73163. RP 73163 is a potent ACAT inhibitor, with cholesterol lowering activity. -
ACAT1 inhibitor
Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. -
ACAT-1 inhibitor
K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45??0.06 μM. -
CerS1 inhibitor
P053 is a potent, non-competitive, and selective inhibitor of ceramide synthase 1 (CerS1), exhibiting an IC₅₀ of 0.5 μM. It functions as an endogenous regulator of mitochondrial fatty acid oxidation in skeletal muscle, influencing cellular energy metabolism. By modulating ceramide synthesis, P053 also acts as a systemic regulator of whole-body adiposity, making it a valuable compound for studying lipid metabolism, energy homeostasis, and metabolic disorders. -
ACAT inhibitor
Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties. -
OGT inhibitor
OSMI-1 is a potent cell-permeable inhibitor of O-GlcNAc transferase (OGT), with an IC50 value of 2.7 μM. This compound effectively decreases protein O-linked N-acetylglucosamine (O-GlcNAcylation) levels in various mammalian cell lines while maintaining the integrity of cell surface N- and O-linked glycans. OSMI-1 serves as a valuable tool for studying the regulatory roles of O-GlcNAcylation in cellular processes and diseases. -
Ionophore
Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines . -
SPT Inhibitor
SPT-IN-2 is a potent inhibitor of serine palmitoyltransferase (SPT) with an IC50 of 0.71 nM against human SPT2. It effectively inhibits ceramide synthesis, leading to reduced intracellular ceramide and 3-ketodihydrosphingosine levels. This compound demonstrates anti-tumor activity in vivo and is characterized by favorable metabolic stability and cell membrane permeability, making it useful in cancer research. SPT-IN-2 is particularly relevant for studies involving lung adenocarcinoma, acute promyelocytic leukemia, and breast cancer. -
ACAT Inhibitor
447C88 is a potent acyl-coenzyme A cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 23 nM. It effectively reduces plasma cholesterol levels, making it valuable for research into endocrine and metabolic disorders, particularly hyperlipidemia. This compound can be utilized in studies aimed at understanding cholesterol metabolism and its implications in various diseases. -
GPAT Inhibitor
FSG67 is a potent glycerol 3-phosphate acyltransferase (GPAT) inhibitor, exhibiting an IC50 value of 24 μM. This compound is valuable for research into lipid metabolism, energy homeostasis, and related metabolic disorders. Its inhibitory action on GPAT makes it a useful tool for studying the roles of glycerolipid synthesis in various biological contexts. -
KAT8 Inhibitor
KAT8-IN-1 is an inhibitor of lysine acetyltransferase 8 (KAT8), with an IC50 of 141 μM against KAT8, alongside IC50 values of 221 μM for KAT2B and 106 μM for KAT3B. This selective inhibition of KAT8 impacts histone acetylation, making it relevant in the study of various biological processes associated with cancer and inflammatory diseases. KAT8-IN-1 is a valuable tool for researchers investigating the role of histone acetylation in gene regulation and its implications in disease mechanisms. -
SOAT2/ACAT2 Inhibitor
Pyripyropene A is a potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2) and acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2), exhibiting an IC50 of 0.07 µM. This compound effectively modulates cholesterol metabolism and has demonstrated the ability to reduce hypercholesterolemia and atherosclerosis in vivo. Pyripyropene A serves as a valuable tool for research into cholesterol-related diseases and therapeutic interventions targeting lipid metabolism. -
ACAT Inhibitor
Sandoz 58-035 is a competitive inhibitor of cholesterol acyltransferase (ACAT), demonstrating potent inhibition of cholesterol esterification in response to hormonal stimulation. This compound effectively achieves over 98% inhibition of ACAT activity in cellular models, making it valuable for research on lipid metabolism and related disorders. Sandoz 58-035 is particularly relevant for studies investigating the role of cholesterol acyltransferase in atherosclerosis and other metabolic conditions. -
zDHHC20 Inhibitor
Cyano-myracrylamide is a potent inhibitor of the zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20), with an IC50 value of 1.35 µM. This compound effectively inhibits S-acylation of various substrates, including EGFR, CD36, Legionella E3 ligase GobX, MyD88, and Ras, in HEK293T cells expressing recombinant variants or endogenous protein. Its ability to modulate the S-acylation process makes Cyano-myracrylamide a valuable tool for studying palmitoylation and its impact on cellular signaling pathways. -
OGT Inhibitor
ST045849 is a small-molecule inhibitor targeting O-GlcNAc transferase (OGT) with an IC50 of 30 μM against the soluble form of OGT (sOGT) and 53 μM against the nuclear/cytoplasmic form (ncOGT). This compound is valuable for studying the role of OGT in metabolism-related diseases, providing insights into regulatory mechanisms involving O-GlcNAcylation. Its application aids in understanding the biological implications of OGT inhibition in various pathological conditions. -
ACAT-1/2 Inhibitor
γ-Sanshool is a selective inhibitor of acyl-CoA cholesterol acyltransferase 1 (ACAT-1) and acyl-CoA cholesterol acyltransferase 2 (ACAT-2). This compound, derived from Zanthoxylum piperitum, exhibits inhibitory activity with IC50 values of 12.0 μM for ACAT-1 and 82.6 μM for ACAT-2. γ-Sanshool is valuable for research focused on cholesterol metabolism and cardiovascular diseases, offering insights into lipid regulation and potential therapeutic targets. -
DGAT2 Inhibitor
JNJ-DGAT2-A is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2), demonstrating an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. This compound is instrumental in studying triglyceride synthesis and its regulation, making it valuable for research focused on lipid metabolism and related metabolic disorders. Its specificity for DGAT2 allows for targeted investigations into pathways influencing energy storage and fat accumulation. -
DGAT2 Inhibitor
PF-07202954 is a potent and selective inhibitor of DGAT2, with an IC50 of 10 nM for human and 17 nM for rat DGAT2. This compound effectively reduces triglyceride synthesis, diminishes hepatic triglyceride accumulation, and lowers plasma triglyceride levels. Additionally, PF-07202954 inhibits de novo lipogenesis and suppresses the hepatic SREBP signaling pathway along with the expression of SREBP target genes. It is relevant for research on non-alcoholic steatohepatitis and related metabolic disorders. -
GPAT Inhibitor
GPAT-IN-1 is a selective inhibitor of glycerol-3-phosphate acyltransferase (GPAT), exhibiting an IC50 value of 8.9 μM. This compound effectively disrupts lipid metabolism and may play a crucial role in obesity research by influencing fatty acid synthesis and storage. Its applications extend to studies investigating metabolic disorders and exploring therapeutic strategies targeting GPAT activity. -
MGAT2 Inhibitor
BMS-963272 is a selective inhibitor of MGAT2, exhibiting an IC50 of 7.1 nM. This compound is primarily utilized in research focused on metabolic disorders and inflammatory diseases, contributing to valuable insights into underlying biochemical pathways. Its oral bioavailability enables convenient in vivo studies, enhancing its utility in preclinical models. -
Acyltransferase Inhibitor
Glabrol is a potent non-competitive inhibitor of acyl-coenzyme A: cholesterol acyltransferase (ACAT), with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity. This isoprenyl flavonoid is derived from the ethanol extract of licorice roots. Glabrol is primarily utilized in research focused on lipid metabolism and cholesterol homeostasis, providing valuable insights into acyltransferase activity in various biological systems. -
ACAT1/2 Inhibitor
Pactimibe is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2), exhibiting IC50 values of 4.9 µM and 3.0 µM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells with IC50s of 2.0 µM, 2.7 µM, and 4.7 µM. Additionally, Pactimibe noncompetitively inhibits oleoyl-CoA with a Ki of 5.6 µM and reduces cholesteryl ester formation with an IC50 of 6.7 µM. This compound demonstrates significant anti-atherosclerotic potential by lowering plasma cholesterol levels, making it valuable for research in cardiovascular diseases and lipid metabolism. -
OGT Inhibitor
OSMI-2 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), designed for cellular permeability. This compound has been shown to enhance the splicing of retained introns in various cell types, making it a valuable tool for studying the regulation of alternative splicing and OGT's role in cellular processes. OSMI-2 is applicable in various research fields, including cancer biology and neurodegenerative disorders, where OGT activity is implicated. -
Baicalin Derivative
BEC2 is an ester derivative of Baicalin that functions as a potent activator of carnitine palmitoyltransferase 1A (CPT1A). This compound exhibits significant lipid-lowering activity, making it a valuable tool for studies related to metabolic disorders and lipid metabolism. BEC2's unique mechanism of action facilitates research into fat oxidation processes and therapeutic interventions for obesity and associated cardiovascular diseases. -
Acyltransferase Inhibitor
SD-066-4 is an orally active inhibitor of acyltransferases, enzymes involved in the transfer of acyl groups across various biological processes. This compound demonstrates significant potential in cancer research by modulating lipid metabolism and cellular signaling pathways associated with tumor growth and progression. Its application in studies of cancer biology may help elucidate the role of acyltransferases in oncogenesis and therapeutic resistance. -
ACAT Inhibitor
CP-113818 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), targeting cholesterol metabolism. This compound is utilized in research focusing on Alzheimer's disease, where it may help elucidate the role of cholesterol in neurodegeneration and amyloid plaque formation. Its ability to modulate lipid metabolism makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders. -
SPT Inhibitor
ALT-007 is a selective serine palmitoyltransferase (SPT) inhibitor that effectively reduces the accumulation of toxic very-long-chain deoxysphingolipids, promoting protein homeostasis. This compound has demonstrated the ability to restore age-related muscle mass loss in mouse models of sarcopenia, and enhances protein homeostasis in both murine and C. elegans models related to aging and disease. ALT-007 is a valuable tool for research focused on age-related neuromuscular disorders. -
DGAT-1 Inhibitor
DGAT1-IN-3 is a selective inhibitor of diacylglycerol O-acyltransferase 1 (DGAT-1), demonstrating potent inhibition with IC50 values of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. This compound is useful for investigating biochemical pathways related to obesity, dyslipidemia, and metabolic syndrome, offering insights into lipid metabolism and energy homeostasis. Its oral bioavailability supports in vivo studies, making it a valuable tool for researchers examining metabolic disorders. -
Ceramide Synthase Inhibitor
Fumonisin B2 is a selective inhibitor of ceramide synthase that disrupts de novo sphingolipid biosynthesis. By blocking the amide bond formation between fatty acids and dihydrosphingosine, it leads to significant intracellular accumulation of free dihydrosphingosine and altered sphingosine levels, which inhibit cell proliferation and induce cell death. Fumonisin B2 is utilized in research to study the pathogenesis of diseases linked to Fusarium verticillioides contamination, such as equine leukoencephalomalacia, porcine pulmonary edema syndrome, human esophageal cancer, and rat hepatocellular carcinoma. -
Acyl-CoA Synthetase Inhibitor
2-Fluoropalmitic acid is an acyl-CoA synthetase inhibitor that demonstrates potential as an anti-glioma agent. This compound effectively reduces the viability and stem-like characteristics of glioma stem cells (GSCs) while also inhibiting the proliferation and invasion of glioma cell lines. Its ability to target cancer cell metabolism makes it a valuable tool in glioma research and therapeutics. -
ACAT1/2 Inhibitor
Pactimibe sulfate is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2) with IC50 values of 4.9 μM and 3.0 μM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells, demonstrating IC50s of 2.0 μM, 2.7 μM, and 4.7 μM, respectively. Pactimibe sulfate also noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM and significantly inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Additionally, it exhibits anti-atherosclerotic properties by reducing plasma cholesterol levels, making it valuable for research in lipid metabolism and cardiovascular disease. -
ACAT Inhibitor
Eflucimibe is an acyl-coenzyme A cholesterol O-acyltransferase (ACAT) inhibitor that specifically targets the enzyme involved in cholesteryl ester synthesis. This compound exhibits significant biological activity in the modulation of lipid metabolism and is primarily utilized in research related to atherosclerosis and cardiovascular disease. Eflucimibe may provide insights into therapeutic strategies for managing hyperlipidemia and associated disorders. -
CPT I Inhibitor
4-Hydroxyphenylglyoxylate is a selective inhibitor of carnitine palmitoyltransferase I (CPT I), a key enzyme in fatty acid metabolism. This compound is instrumental in investigating the modulation of CPT I activity in liver mitochondria and examining the impact on fatty acid oxidation in isolated hepatocytes. Its ability to inhibit fatty acid oxidation makes it a valuable tool in metabolic research and studies related to energy homeostasis. -
SPT Inhibitor
L-Penicillamine is an orally active inhibitor of serine palmitoyltransferase (SPT), targeting the PLP cofactor to form adducts that inhibit SPT activity and subsequently reduce sphingolipid biosynthesis. This compound not only restricts tumor access to vitamin B6 but also stabilizes the human papillomavirus 16 E6 oncoprotein monomer, inhibiting its polymerization and demonstrating a distinct anticancer mechanism. In preclinical studies, L-Penicillamine has been shown to delay the growth of Sarcoma-180, induce tumor necrosis, and extend survival. Caution is advised for long-term use due to potential risks of Pyridoxine deficiency and weight loss.
