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-117656
    ESI-05
    Inhibitor 99.78%
    ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
    ESI-05
  • HY-W012946
    2-Furoic acid
    Inhibitor 99.98%
    2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation. 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats.
    2-Furoic acid
  • HY-16278
    Pradigastat
    Inhibitor 99.88%
    Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro.
    Pradigastat
  • HY-133968
    24-Methylenecholesterol
    Activator 99.78%
    24-Methylenecholesterol (Ostreasterol) is a regulator targeting acyl-CoA cholesterol acyltransferase (ACAT) with anti-aging and neuroprotective effects. 24-Methylenecholesterol mimics the effects of nerve growth factor (NGF), can extend yeast lifespan through an anti-oxidative stress mechanism, and exhibits neuroprotective activity in PC12 cells. 24-Methylenecholesterol can reduce intracellular reactive oxygen species (ROS) and malondialdehyde (MDA) levels, activate anti-oxidative stress pathways (such as UTH1, SOD-related genes), and promote synaptic growth.
    24-Methylenecholesterol
  • HY-155938
    Cyano-myracrylamide
    Inhibitor 98.13%
    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-126015
    P053
    Inhibitor
    P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5 μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator.
    P053
  • HY-117832
    Pyripyropene A
    Inhibitor 99.37%
    Pyripyropene A is an orally active, potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC50 of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.
    Pyripyropene A
  • HY-112487
    Sandoz 58-035
    Inhibitor 99.35%
    Sandoz 58-035 is a selective acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. Sandoz 58-035 inhibits this enzyme in intact cells and isolated microsomal fractions. Sandoz 58-035 blocks the esterification of exogenous vesicle-derived cholesterol and the incorporation of oleic acid into cellular cholesterol esters, reducing the formation and accumulation of cholesterol esters. Sandoz 58-035 causes a slight increase in cellular free cholesterol, and at high concentrations, it also causes a slight reduction in overall cellular protein synthesis. Sandoz 58-035 can be used in studies related to cellular cholesterol regulation.
    Sandoz 58-035
  • HY-W018026
    Oxfenicine
    Inhibitor 99.98%
    Oxfenicine (L-p-Hydroxyphenylglycine) is an orally active carnitine palmitoyltransferase-1 inhibitor. Oxfenicine inhibits the oxidation of fatty acids in the heart, protecting cardiac tissue from necrotic damage during ischemia, and also has an inhibitory effect on cardiac tissue apoptosis. In addition, Oxfenicine promotes lipolysis in a high-fat diet rat model. Oxfenicine can be used in the study of cardiovascular and metabolic diseases.
    Oxfenicine
  • HY-107572
    PD 128042
    Inhibitor 99.97%
    PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway.
    PD 128042
  • HY-153855
    Zamaporvint
    Inhibitor 99.76%
    Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research.
    Zamaporvint
  • HY-136282
    ST045849
    Inhibitor 99.96%
    ST045849 (OGT-IN-2) is a small-molecule OGT inhibitor with an IC50 of 30 μM against sOGT and 53 μM against ncOGT. ST045849 is applicable to research on metabolism-related diseases.
    ST045849
  • HY-111880
    γ-Sanshool
    Inhibitor 98.53%
    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-15497
    AZD7687
    Inhibitor 98.74%
    AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research.
    AZD7687
  • HY-156259
    PF-07202954
    Inhibitor 98.82%
    PF-07202954 is an orally active, highly selective DGAT2 inhibitor with an IC50 of 10 nM against human DGAT2 and an IC50 of 17 nM against rat DGAT2. PF-07202954 reduces triglyceride synthesis, decreases hepatic triglyceride content and plasma triglyceride levels, inhibits de novo lipogenesis, and suppresses the hepatic SREBP signaling pathway as well as the expression of SREBP target genes. PF-07202954 is applicable to research related to non-alcoholic steatohepatitis.
    PF-07202954
  • HY-12425
    DGAT1-IN-1
    Inhibitor 98.0%
    DGAT1-IN-1 is a diacylglycerol O-acyltransferase 1 (DGAT1) inhibitor with a human IC50 of <10 nM and a mouse IC50 of <50 nM. DGAT1-IN-1 is applicable to the research of obesity-related diseases, type 2 diabetes and diabetes-related diseases.
    DGAT1-IN-1
  • 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-101857
    TP-020
    Inhibitor 99.94%
    TP-020 (MGAT2-IN-1), a chemical probe, is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
    TP-020
  • HY-110381
    JNJ-DGAT2-A
    Inhibitor 98.26%
    JNJ-DGAT2-A is a selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. JNJ-DGAT2-A can be used for the research of triglyceride (TG) synthesis.
    JNJ-DGAT2-A
  • 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
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