Acyltransferase Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S0359	T863 (DGAT-3)	T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) that acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells.	J Virol, 2024, 98(11):e0110324 J Cell Sci, 2024, 137(20)jcs262162
S0820	RP-64477	RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). This compound inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively.
S9162	Rubimaillin	Rubimaillin (Mollugin), found in the Chinese medical plant Rubia cordifola, is a dual inhibitor of acetyl-CoA cholesterol Acyltransferase 1 (ACAT1) and acetyl-CoA cholesterol Acyltransferase 2 (ACAT2), but is more selective for the ACAT2 isozyme.
E0941	K-604 dihydrochloride	K-604 dihydrochloride, a potent and selective inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1), suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels.
S9921	PF-06424439 Methanesulfonate	PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM.
E7561	Pradigastat	Pradigastat (LCQ-908) is a potent and selective inhibitor of DGAT1 with an IC50 of 57 nM in hDGAT1. It also inhibits OATP1B1, OATP1B3 , and OAT3 activity in a concentration-dependent manner, with an IC50 of 1.66 μM, 3.34 μM, and 0.973 μM, respectively.
S6971	Ervogastat	Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).
S2187	Avasimibe	Avasimibe inhibits ACAT with an IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with an IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.	J Lipid Res, 2025, 66(8):100854 Hepatol Commun, 2025, 9(6)e0714 Nat Commun, 2024, 15(1):8301
S7889	Xanthohumol	Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. This compound inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. It is also a potent antiviral agent against a series of DNA and RNA viruses. This chemical induces growth inhibition and apoptosis in cancer cells. Phase 1.	Oncotarget, 2025, 16:532-544 J Cell Sci, 2024, 137(20)jcs262162 Antiviral Res, 2022, 207:105416
S3021	Rimonabant (SR141716)	Rimonabant (SR141716) is a selective antagonist of CB1 with an IC50 of 13.6 nM and an EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane, and it is also a dual inhibitor of acyl CoA:cholesterol acyltransferases (ACAT) 1 and 2 that inhibits mycobacterial MmpL3.	Biol Pharm Bull, 2025, 48(6):769-781 Toxicol Lett, 2023, 374:48-56 Int J Biol Sci, 2022, 18(4):1401-1414
S2674	A-922500 (DGAT-1 Inhibitor 4a)	A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related Acyltransferase, hERG, and a panel of anti-targets.	Cell Death Discov, 2025, 11(1):21 Nature, 2023, 621(7977):171-178 Cell Rep, 2022, 41(11):111827
S7192	PF-04620110	PF-04620110 is an orally active, selective and potent diglyceride Acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.	Cell Rep, 2025, 44(8):116100 Commun Biol, 2025, 8(1):1169 J Pharm Biomed Anal, 2019, 170:176-186
S4189	Cyclandelate	Cyclandelate (BS 572, 3,5,5-Trimethylcyclohexyl mandelate) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol Acyltransferase (ACAT) with IC50 of 80 μM.