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-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-107396
    YM-750
    Inhibitor 99.88%
    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-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-N6706
    Enniatin complex
    Inhibitor 99.81%
    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 .
    Enniatin complex
  • 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-108341
    PF-06424439
    Inhibitor
    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
    PF-06424439
  • 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
  • HY-N3807
    Enniatin B1
    Inhibitor
    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-125319
    Amidepsine A
    Inhibitor
    Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.
    Amidepsine A
  • HY-107571
    VULM 1457
    Inhibitor 99.95%
    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-16437
    RP-64477
    Inhibitor 99.68%
    RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
    RP-64477
  • HY-133968
    24-Methylenecholesterol
    Activator
    24-Methylenecholesterol (Ostreasterol), a natural marine sterol, stimulates cholesterol acyltransferase in human macrophages. 24-Methylenecholesterol possess anti-aging effects in yeast. 24-methylenecholesterol enhances honey bee longevity and improves nurse bee physiology.
    24-Methylenecholesterol
  • HY-101576
    RP 70676
    Inhibitor 99.74%
    RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.
    RP 70676
  • HY-15197
    ABT-046
    Inhibitor 98.13%
    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-111417
    GSK2973980A
    Inhibitor
    GSK2973980A is a potent and selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 3 nM.
    GSK2973980A
  • HY-N10224
    Terpendole C
    Inhibitor
    Terpendole C, produced by Albophoma yamanashiensis, shows potent inhibitory activity against acyl-CoA: cholesterol acyltransferase (ACAT).
    Terpendole C
  • HY-139025
    ACAT-IN-8
    Inhibitor
    ACAT-IN-8 (example 206) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-8 inhibits NF-κB mediated transcription.
    ACAT-IN-8
  • 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-126455
    Penicillide
    Inhibitor
    Penicillide (Vermixocin A), isolated from Talaromyces derxii cultivated on rice, shows inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT).
    Penicillide
  • HY-139024
    ACAT-IN-7
    Inhibitor
    ACAT-IN-7 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-7 inhibits NF-κB mediated transcription.
    ACAT-IN-7
Cat. No. Product Name / Synonyms Application Reactivity

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