2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Acyltransferase

Acyltransferase

Diacylglycerol acyltransferase; Diglyceride acyltransferase; acyl-CoA:cholesterol acyltransferase; mono- acylglycerol acyltransferase

Acyltransferase

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Acyltransferase (AT) catalyzes the transfer of an acyl moiety from acyl-coenzyme A (acyl-CoA) to an acceptor. Acyltransferases play important roles in the maintenance of homeostasis in the human body and have been linked to various diseases. The Acyltransferase family includes acyl-CoA:cholesterol AT (ACAT), diacylglycerol AT (DGAT), and monoacylglycerol AT (MGAT) for the metabolism of lipids.

ACAT (acyl-coenzyme A:cholesterol acyltransferase) is an intracellular enzyme that catalyzes the formation of cholesterol esters from cholesterol and fatty acyl-coenzyme A. In mammals, two isoenzymes, ACAT1 and ACAT2, encoded by two different genes, exist. ACATs play important roles in cellular cholesterol homeostasis in various tissues.

DGAT (acyl-CoA:diacylglycerol acyltransferase) is an integral membrane enzyme that catalyses the last step of triacylglycerol synthesis from diacylglycerol and acyl-CoA. DGAT activity resides mainly in two distinct membrane bound polypeptides, known as DGAT1 and DGAT2.

MGAT (acyl-CoA:monoacylglycerol acyltransferase) catalyzes the synthesis of diacylglycerol, the precursor of physiologically important lipids such as triacylglycerol and phospholipids. In the intestine, MGAT plays a major role in the absorption of dietary fat because resynthesis of triacylglycerol is required for the assembly of lipoproteins that transport absorbed fat to other tissues.

Acyltransferase Isoform Specific Products:

Acyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16266
    JNJ-DGAT1-A
    		Inhibitor
    JNJ-DGAT1-A is a selective DGAT1 inhibitor. JNJ-DGAT1-A inhibits DGAT1 activity and TG synthesis.
    JNJ-DGAT1-A
  • HY-U00430
    MGAT2-IN-2
    		Inhibitor
    MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
    MGAT2-IN-2
  • HY-100288
    RP 73163 Racemate
    RP 73163 Racemate is the racemate of RP 73163. RP 73163 is a potent ACAT inhibitor, with cholesterol lowering activity.
    RP 73163 Racemate
  • HY-117466
    FR186054
    		Inhibitor
    FR186054 is an oral active acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with the IC50 of 99 nM. FR186054 shows hypocholesterolemic effect and can be used for study of hypercholesterolemia and atherosclerosis.
    FR186054
  • HY-119265
    LDL-IN-4
    		Inhibitor
    LDL-IN-4 (Compound 2) inhibits human acyl-CoA:cholesterol acyltransferase-1 and -2 activities. LDL-IN-4 inhibits copper-mediated low density lipoprotein (LDL) oxidation, with an IC50 of 3 μM. LDL-IN-4 has anti-atherosclerotic biological activity.
    LDL-IN-4
  • HY-167664
    KY-455
    		Inhibitor
    KY-455 is a novel inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). KY-455 inhibita rabbit intestinal, hepatic, macrophage and adrenal ACAT with IC50 values of 0.4, 0.9, 2.9 and 4.1 μmol/L, respectively.
    KY-455
  • HY-155938
    Cyano-myracrylamide
    		Inhibitor
    Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras.
    Cyano-myracrylamide
  • HY-135785
    OSMI-3
    		Inhibitor
    OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
    OSMI-3
  • HY-101648
    ACAT-IN-1 cis isomer
    		Inhibitor
    ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM.
    ACAT-IN-1 cis isomer
  • HY-U00114
    ZSET-845
    		Activator
    ZSET-845 is a cognitive enhancer which enhances choline acetyltransferase activity in the hippocampus in the rat.
    ZSET-845
  • HY-U00369
    FCE 28654
    		Inhibitor
    FCE 28654 is an inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
    FCE 28654
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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