Acyltransferases

YM 750 is reported to act as a SOAT (acyl-CoA:cholesterol acyltransferase, ACAT) inhibitor.

Etomoxir is an inhibitor of carnitine palmitoyltransferase A (CPT1), which is required for the oxidation of long-chain acyl CoA esters. Also a strong inhibitor of mitochondrial CPT1 and a candidate as an anti-diabetic drug.

PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

ATR-101 is in clinical development for the treatment of adrenocortical carcinoma (ACC).

VULM 1457 is an Acyl-CoA: cholesterol acyltransferase (ACAT) or SOAT inhibitor. VULM 1457 decreases cholesterol levels in the liver and plasma.

CI 976 is a trimethoxy fatty acid anilide inhibitor of liver and intestinal acyl coenzyme A cholesterol acyltransferase (ACAT) and sterol O-acyltransferase (SOAT). Cl 976 lowers non-high density lipoprotein (non-HDL) cholesterol and increases HDL-cholesterol concentrations.

Cyclandelate is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM.

GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer's disease, Parkinson's disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.

FR-190809 is a potent, nonadrenotoxic, orally efficacious ACAT inhibitor.

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells.

RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.

MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM.

YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.

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

E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.

RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).

Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM.

K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45??0.06 μM.

P053 is a potent, non-competitive, and selective inhibitor of ceramide synthase 1 (CerS1), exhibiting an IC₅₀ of 0.5 μM. It functions as an endogenous regulator of mitochondrial fatty acid oxidation in skeletal muscle, influencing cellular energy metabolism. By modulating ceramide synthesis, P053 also acts as a systemic regulator of whole-body adiposity, making it a valuable compound for studying lipid metabolism, energy homeostasis, and metabolic disorders.

Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties.

OSMI-1 is a potent cell-permeable inhibitor of O-GlcNAc transferase (OGT), with an IC50 value of 2.7 μM. This compound effectively decreases protein O-linked N-acetylglucosamine (O-GlcNAcylation) levels in various mammalian cell lines while maintaining the integrity of cell surface N- and O-linked glycans. OSMI-1 serves as a valuable tool for studying the regulatory roles of O-GlcNAcylation in cellular processes and diseases.

Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .