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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.
CL-283796 is a potent and orally active inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). This compound effectively reduces low-density lipoprotein (LDL) cholesterol levels while not influencing cholesterol absorption, as demonstrated in studies with African green monkeys. CL-283796 is suitable for research focused on hypercholesterolemia and related lipid metabolic disorders.
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Enniatin A is an acyltransferase inhibitor derived from the Fusarium species. It specifically inhibits acyl-CoA:cholesterol acyltransferase (ACAT) with an IC50 of 22 μM, demonstrating its effectiveness in modulating cholesterol metabolism. This compound is primarily utilized in research investigating lipid metabolism and related disorders.
AS-183 is a selective inhibitor of cholesterol acyltransferase (ACAT), with an IC50 of 0.94 µM. It effectively inhibits cholesterol ester formation in HepG2, CaCo2, and THP-1 cells, demonstrating IC50 values of 18.1, 25.5, and 34.5 µM, respectively. This compound is valuable for research on atherosclerosis and hypercholesterolemia, providing insights into lipid metabolism and related cardiovascular diseases.
Pyripyropene B is a potent inhibitor of acyl-CoA: cholesterol acyltransferase 2 (ACAT2), derived from the fungus Aspergillus fumigatus FO 1289. This compound exhibits significant inhibitory activity with an IC50 value of 117 nM, making it a valuable tool for studying cholesterol metabolism. Pyripyropene B is utilized in research applications focused on lipid regulation and related metabolic disorders.
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NTE-122 dihydrochloride is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), demonstrating an IC50 of 7.6 nM in liver and 4.4 nM in aorta tissues of cholesterol-fed rabbits. This compound is significant for research into atherosclerosis, as it modulates cholesterol esterification processes, potentially impacting lipid metabolism and cardiovascular health. Its application may provide insights into therapeutic strategies for managing atherosclerotic diseases.
JTP-103237 is a selective inhibitor of the MGAT2 enzyme, exhibiting an IC50 of 0.019 μM for human MGAT2 and 6.423 μM for human MGAT3. This compound effectively modulates fat absorption, reduces plasma glucose levels, and serves as a preventative agent against diet-induced obesity. JTP-103237 is valuable for research in metabolic disorders and obesity-related studies.
MGAT2-IN-7 is a selective inhibitor of monoacylglycerol acyltransferase 2 (MGAT2). This benzenesulfonamide derivative plays a significant role in research related to obesity and metabolic dysfunction, particularly in the context of metabolic dysfunction-associated steatotic liver disease (MASLD). Its inhibition of MGAT2 facilitates the investigation of lipid metabolism and potential therapeutic strategies for related disorders.
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Purpactin B is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), a key enzyme involved in cholesterol metabolism. This compound exhibits significant biological activity by modulating cholesterol esterification, which may influence lipid metabolism and cellular cholesterol homeostasis. Purpactin B is valuable in research applications related to atherosclerosis, lipid disorders, and cardiovascular disease studies.
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KY-455 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), effectively targeting various organs including rabbit intestinal, hepatic, macrophage, and adrenal ACAT with IC50 values of 0.4, 0.9, 2.9, and 4.1 μmol/L, respectively. This compound is valuable for research applications related to lipid metabolism and cholesterol homeostasis. Its selective action makes it an important tool in studies aimed at understanding ACAT's role in diseases such as atherosclerosis.
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Purpactin C is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), a key enzyme involved in cholesterol metabolism. By inhibiting ACAT, Purpactin C effectively decreases cholesterol esterification, contributing to lipid homeostasis. This compound is valuable for research applications focused on dyslipidemia, cardiovascular diseases, and metabolic disorders.
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Gypsetin is a potent acylcoenzyme A:cholesterol acyltransferase (ACAT) inhibitor that effectively inhibits rat liver microbody ACAT with an IC50 of 18 μM. Its mechanism of action is competitive with the oleoyl-CoA substrate, exhibiting a Ki value of 5.5 μM. Additionally, Gypsetin significantly hinders the formation of cholesterol esters from oleic acid, with an IC50 of 0.65 μM. This compound is valuable for research applications focusing on lipid metabolism and cholesterol homeostasis.
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Purpactin A is a specific inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), derived from the fungus Penicillium purpurogenum FO-6. This compound has demonstrated significant biological activity by modulating cholesterol metabolism, making it useful in research focused on lipid disorders and cardiovascular diseases. Its ability to inhibit ACAT provides valuable insights into cholesterol-related pathways and therapeutic approaches targeting hyperlipidemia.
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Pomonic acid is an acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor that effectively reduces the esterification of free cholesterol to cholesteryl esters. By decreasing intracellular cholesteryl ester accumulation, it serves as a valuable tool for studying lipid metabolism disorders. Pomonic acid is particularly relevant in research focused on atherosclerosis and related cardiovascular diseases.
Glisoprenin B is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). This compound demonstrates significant biological activity by disrupting cholesterol esterification, which can play a crucial role in lipid metabolism and cardiovascular disease research. It is valuable in studies focused on atherosclerosis and other conditions related to cholesterol homeostasis.
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Phenylpyropene B is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with an IC50 value of 12.8 μM. This compound demonstrates significant biological activity by reducing cholesterol esterification, making it a valuable tool in studies related to lipid metabolism and cardiovascular disease. Phenylpyropene B can be utilized in research applications focusing on cholesterol homeostasis, atherosclerosis, and related metabolic disorders.
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FCE 28654 is an acyltransferase inhibitor that targets acylCoA:cholesterol acyltransferase (ACAT). It demonstrates weak inhibition of ACAT in microsomes from rabbit aorta and intestine, as well as monkey liver, with IC50 values of 2.55, 1.08, and 5.69 μM, respectively. This compound can be utilized in research exploring cholesterol metabolism and the regulation of lipid profiles.
