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

Acyltransferase

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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-50861
    AZD3988
    Inhibitor 99.89%
    AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity.
    AZD3988
  • HY-101722
    Melinamide
    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-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-107416
    RHC 80267
    Inhibitor 99.41%
    RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
    RHC 80267
  • 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-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-108339
    PF-06471553
    Inhibitor 98.29%
    PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
    PF-06471553
  • 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-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-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-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-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-19286
    Eflucimibe
    98.60%
    Eflucimibe (F 12511) is a new acyl-coenzyme A cholesterol O-acyltransferase (ACAT) inhibitor. Eflucimibe can be used in the research of atherosclerosis.
    Eflucimibe
  • 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-155938
    Cyano-myracrylamide
    Inhibitor 98.0%
    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-111880
    γ-Sanshool
    Inhibitor 99.23%
    γ-Sanshool can be isolated from Zanthoxylum piperitum. γ-Sanshool inhibits human ACAT-1 and ACAT-2 activities with IC50s of 12.0 and 82.6 μM.
    γ-Sanshool
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity

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