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-115938
    BEC2
    		Inhibitor ≥98.0%
    BEC2 is an ester derivative of Baicalin, with good lipid-lowering activity. BEC2 can direct activate the carnitine palmitoyltransferase 1A (CPT1A).
    BEC2
  • HY-135784
    OSMI-2
    		Inhibitor 98.73%
    OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
    OSMI-2
  • HY-50670
    DGAT-1 inhibitor 2
    		Inhibitor
    DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.
    DGAT-1 inhibitor 2
  • HY-N3807
    Enniatin B1
    		Inhibitor 99.34%
    Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
    Enniatin B1
  • HY-101722
    Melinamide
    		99.94%
    Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.
    Melinamide
  • HY-112487
    Sandoz 58-035
    		Inhibitor 99.35%
    Sandoz 58-035 is a competitive inhibitor of cholesterol acyltransferase (ACAT). Sandoz 58-035 effectively inhibits (>98%) hormonally stimulated cholesterol esterification in cells.
    Sandoz 58-035
  • HY-N6723
    Fumonisin B2
    		Inhibitor 99.46%
    Fumonisin B2, a mycotoxin produced by Fusarium moniliforme in various grains, is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis.
    Fumonisin B2
  • HY-15197
    ABT-046
    		Inhibitor 98.57%
    ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1.
    ABT-046
  • HY-153628
    GPAT-IN-1
    		Inhibitor
    GPAT-IN-1 is a glycerol-3-phosphate acyltransferase (GPAT) inhibitor with an IC50 value of 8.9 μM. GPAT-IN-1 can be used for the research of obesity.
    GPAT-IN-1
  • HY-16434
    DGAT1-IN-3
    		Inhibitor 99.92%
    DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.
    DGAT1-IN-3
  • HY-156259
    PF-07202954
    		Inhibitor
    PF-07202954 is a weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2. PF-07202954 lowers liver triglyceride content in a Western-diet-fed rat model.
    PF-07202954
  • HY-117651
    2-Fluoropalmitic acid
    		Inhibitor ≥98.0%
    2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines.
    2-Fluoropalmitic acid
  • HY-100401A
    Pactimibe sulfate
    		Inhibitor ≥98.0%
    Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
    Pactimibe sulfate
  • HY-105445
    CP-113818
    		Inhibitor 99.13%
    CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease.
    CP-113818
  • HY-107571
    VULM 1457
    		Inhibitor 99.71%
    VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia.
    VULM 1457
  • HY-100401
    Pactimibe
    		Inhibitor 99.98%
    Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
    Pactimibe
  • HY-101627
    YM17E
    		Inhibitor 98.34%
    YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
    YM17E
  • HY-16437
    RP-64477
    		Inhibitor 99.62%
    RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
    RP-64477
  • HY-107396
    YM-750
    		Inhibitor 99.95%
    YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.
    YM-750
  • HY-119738A
    (Rac)-OSMI-1
    		Inhibitor
    (Rac)-OSMI-1 is the racemate of OSMI-1. OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.
    (Rac)-OSMI-1
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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