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Acyltransferase inhibitors act on enzymes that transfer acyl groups from coenzyme A thioesters. Such reactions build cholesteryl esters, triacylglycerols and acylated proteins, so these enzymes sit at branch points of lipid metabolism. Human acyl-coenzyme A:cholesterol acyltransferase 1 (ACAT1) was cloned in 1993, and nevanimibe, CI 976 and VULM 1457 inhibit these cholesterol acyltransferases. PF-06471553 inhibits monoacylglycerol acyltransferase 3 (MGAT3), which forms diacylglycerol during intestinal lipid absorption. GOAT-IN-1 blocks ghrelin O-acyltransferase (GOAT), identified in 2008 as the enzyme that attaches octanoate to the hormone ghrelin. Etomoxir (sodium salt) inhibits carnitine palmitoyltransferase 1 (CPT-1), which commits fatty acids to mitochondrial oxidation. Enzymes that instead hydrolyze lipids appear under the sibling categories Lipase and Phospholipases.
SOAT-IN-1 is a potent and selective inhibitor of sodium-dependent organic anion transporters (SOAT). With an IC50 value of 1.6 µM for SOAT, it demonstrates significant inhibition compared to 14.3 µM for NTCP. This compound is valuable for research applications involving the modulation of SOAT-mediated transport processes, contributing to studies in drug metabolism and disposition.
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.
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.
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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-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.
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.
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.
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.
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.
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.
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-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.
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.
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.
Synonyms: CS-505 free base
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.
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.
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.
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.
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.
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.
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.
Synonyms: CS-505
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.
Synonyms: F 12511
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.
Synonyms: 4-Hydroxyphenylglyoxylic acid; 4-HPGA
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.
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.
