Fumonisin B2 is a mycotoxin produced by Fusarium moniliforme in various grains. It also is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase). Which disrupts de novo sphingolipid biosynthesis.

Penicillide is a fungal metabolite originally isolated from Penicillium that has diverse biological activities. It is an inhibitor of calpain 2/m-calpain (IC50 = 7.1 μM) and acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 22.9 μM). It is also an antagonist of oxytocin receptors (IC50 = 67 μM). Penicillide inhibits RNA synthesis in P388 murine leukemia cells.

H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

Pactimibe sulfate (CS-505) 是一种双重的 ACAT1/2 抑制剂，能够作用于 ACAT1 (IC50: 4.9 μM)、ACAT2 (IC50: 3.0 μM)。Pactimibe sulfate 对 ACAT 表现出抑制作用，在肝细胞中 IC50=2.0 μM，在巨噬细胞中 IC50=2.7 μM，在 THP-1 细胞中 IC50=4.7 μM。Pactimibe sulfate 能够非竞争性地抑制 oleoyl-CoA (Ki: 5.6 μM)，显著抑制胆固醇酯的形成 (IC50: 6.7 μM)。Pactimibe sulfate 能够降低血浆胆固醇的活性，具有抗动脉粥样硬化的潜力。

PF-06471553 is an effective and selective inhibitor of monoacylglycerol acyltransferase 3 (IC50: 92 nM).

ANAT inhibitor-2 is a ANAT inhibitor for canavan disease, with an IC 50 value of 20 μM.

Acyl-Coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 value of approximately 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 μM.

RP 73163 Racemate is the racemate of RP 73163. RP 73163 is a potent inhibitor of ACAT, shows cholesterol lowering activity.

Nevanimibe is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).