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-N10788
    Pomonic acid
    		Inhibitor
    Pomonic acid is a triterpenoid that significantly inhibits cholesterol ester accumulation and suppresses the acyl coenzyme A:cholesterol acyltransferase (ACAT) activity.
    Pomonic acid
  • HY-129340
    AS-183
    		Inhibitor
    AS-183 is an inhibitor of cholesterol acyltransferase (ACAT) (IC50=0.94 µM). AS-183 also inhibits the formation of cholesterol esters in HepG2, CaCo2 and THP-1 cells with IC50 values ​​of 18.1, 25.5 and 34.5 µM, respectively. AS-183 can be used in the study of atherosclerosis and hypercholesterolemia.
    AS-183
  • HY-139020
    ACAT-IN-3
    		Inhibitor
    ACAT-IN-3 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-3 inhibits NF-κB mediated transcription.
    ACAT-IN-3
  • HY-100253
    TA-7552
    		Inhibitor
    TA-7552 is a potent cholesterol-lowering agent.
    TA-7552
  • HY-106818A
    Monatepil maleate
    		Inhibitor
    Monatepil maleate (AJ-2615) is a potent and orally active Ca2+-channel antagonist and a noncompetitive ACAT inhibitor. Monatepil maleate decreases blood pressure and improves plasma lipid metabolism. Monatepil maleate has the potential for the research of hyperlipidemia.
    Monatepil maleate
  • HY-123765
    JTT-553
    		Inhibitor
    JTT-553 is a DGAT1 inhibitor (IC50: 2.38 nM). JTT-553 reduces plasma concentrations of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and hepatic triglycerides (TG). JTT-553 improves insulin-dependent glucose uptake and glucose intolerance in adipose tissue of DIO mice. JTT-553 reduces TNF-α mRNA levels and increases GLUT4 mRNA levels in adipose tissue of KK-Ay mice. JTT-553 improves adipose tissue insulin resistance and systemic glucose metabolism by reducing body weight. JTT-553 can be used in the study of obesity and type 2 diabetes mellitus (T2DM).
    JTT-553
  • HY-121407
    Lateritin
    		Inhibitor
    Lateritin is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), isolated from the mycelial cake of Gibberella lateritium IFO 7188. Lateritin also inhibits the growth of a mini-panel of human cancer cell lines, gram-positive bacteria, and Candida albicans.
    Lateritin
  • HY-124064
    TMP-153
    		Inhibitor
    TMP-153 is an orally active inhibitor of ACAT with an IC50 value of approximately 5-10 nM against hepatic and intestinal ACAT in varicose animals. TMP-153 exhibits cholesterol-lowering effects and can be utilized in the research of atherosclerosis.
    TMP-153
  • HY-159698
    IONIS-DGAT 2Rx
    		Inhibitor
    IONIS-DGAT 2Rx (ION-224) is a DGAT2 inhibitor, which is promising for research of atherosclerosis.
    IONIS-DGAT 2Rx
  • HY-112851
    Diacylglycerol acyltransferase inhibitor-1
    		Inhibitor
    Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
    Diacylglycerol acyltransferase inhibitor-1
  • HY-N7281
    Aphadilactone C
    		Inhibitor
    Aphadilactone C is a potent and selective DGAT-1 inhibitor with an IC50 of 0.46 μM. Aphadilactone C shows significant antimalarial activities with an IC50 value of 170 nM.
    Aphadilactone C
  • HY-117651R
    2-Fluoropalmitic acid (Standard)
    		Inhibitor
    Quinine (sulfate hydrate) (Standard) is the analytical standard of Quinine (sulfate hydrate). This product is intended for research and analytical applications. Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM.
    2-Fluoropalmitic acid (Standard)
  • HY-157521
    AANAT-IN-1
    		Inhibitor
    AANAT-IN-1 (compound 30) is a potent inhibitor (IC50: 10μM) of aralkylamine N-acetyltransferase (AANAT). AANAT is responsible for the synthesis of melatonin, which is involved in disorders such as seasonal affective disorder (SAD) in which melatonin levels are abnormally high.
    AANAT-IN-1
  • HY-139022
    ACAT-IN-5
    		Inhibitor
    ACAT-IN-5 (example 19) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-5 inhibits NF-κB mediated transcription.
    ACAT-IN-5
  • HY-E70260
    16-NBD-16:0 Coenzyme A triammonium
    16-NBD-16:0 Coenzyme A triammonium can be used as a substrate to measure the in vitro activity of other Acyltransferase .
    16-NBD-16:0 Coenzyme A triammonium
  • HY-N6702
    Enniatin A
    		Inhibitor
    Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes.
    Enniatin A
  • HY-N14614
    Pyripyropene B
    		Inhibitor
    Pyripyropene B is a powerful acyl-CoA: cholesterol acyltransferase 2 (ACAT2) inhibitor found in the fungus Aspergillus fumigatus FO 1289. Pyripyropene B inhibits acyl-CoA: cholesterol acyltransferase with an IC50 of 117 nM.
    Pyripyropene B
  • HY-121762
    NTE-122 dihydrochloride
    		Inhibitor
    NTE-122 (dihydrochloride) is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with the IC50 in liver and aorta of cholesterol-fed rabbits of 7.6nM, 4.4nM and 9.6 nM, respectively, that plays an important role in atherosclerosis.
    NTE-122 dihydrochloride
  • HY-107572R
    PD 128042 (Standard)
    		Inhibitor
    PD 128042 (Standard) is the analytical standard of PD 128042. This product is intended for research and analytical applications. 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 (Standard)
  • HY-100399AR
    Nevanimibe hydrochloride (Standard)
    		Inhibitor
    Nevanimibe hydrochloride (Standard) is the analytical standard of Nevanimibe hydrochloride. This product is intended for research and analytical applications. Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
    Nevanimibe hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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