| S2187 |
Avasimibe
|
Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with 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. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol 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 IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and 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 acyltransferases, hERG, and a panel of anti-targets. |
-
Cell Death Discov, 2025, 11(1):21
-
Nature, 2023, 621(7977):171-178
-
Nature, 2023, 621(7977):171-178
|
|
| 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
|
|
| S0820 |
RP-64477
|
RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 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. |
|
|
| S0359 |
T863 (DGAT-3)
|
T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht 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
|
|
| 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. |
|
|
| 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 IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with 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. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol 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 IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and 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 acyltransferases, hERG, and a panel of anti-targets. |
- Cell Death Discov, 2025, 11(1):21
- Nature, 2023, 621(7977):171-178
- Nature, 2023, 621(7977):171-178
|
|
| 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
|
|
| S0820 |
RP-64477
|
RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 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. |
|
|
| S0359 |
T863 (DGAT-3)
|
T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht 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
|
|
| 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. |
|
|
| 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). |
|
|