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-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)
  • HY-50670R
    DGAT-1 inhibitor 2 (Standard)
    Inhibitor
    DGAT-1 inhibitor 2 (Standard) is the analytical standard of DGAT-1 inhibitor 2 (HY-50670). This product is intended for research and analytical applications. DGAT-1 inhibitor 2 is an orally active DGAT-1 inhibitor with IC50 values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively. DGAT-1 inhibitor 2 increases ROS concentration, GRP78, and PERK protein abundance. DGAT-1 inhibitor 2 increases SREBF1, CPT1A, and MTTP mRNA in fatty acid-treated cells. DGAT-1 inhibitor 2 improves obesity.
    DGAT-1 inhibitor 2 (Standard)
  • HY-135505
    JTP-103237
    Inhibitor
    JTP-103237 is a MGAT2 inhibitor (IC50: 0.019 μM and 6.423 μM for hMGAT2 and hMGAT3 respectively). JTP-103237 modulates fat absorption, decreases plasma glucose levels and prevents diet-induced obesity.
    JTP-103237
  • HY-101722R
    Melinamide (Standard)
    Melinamide (Standard) is the analytical standard of Melinamide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N14525
    Glisoprenin A
    Inhibitor
    Glisoprenin A is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea.
    Glisoprenin A
  • HY-136707
    DGAT-1 inhibitor 3
    Inhibitor
    DGAT-1 inhibitor 3 (compound 10) is a potent DGAT-1 inhibitor with an IC50 value of 0.038 µM. DGAT-1 inhibitor 3 has the potential for the research of obesity and diabetes.
    DGAT-1 inhibitor 3
  • HY-N14813
    Glisoprenin D
    Inhibitor
    Glisoprenin D is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea.
    Glisoprenin D
  • HY-16266
    JNJ-DGAT1-A
    Inhibitor
    JNJ-DGAT1-A is a selective DGAT1 inhibitor. JNJ-DGAT1-A inhibits DGAT1 activity and TG synthesis.
    JNJ-DGAT1-A
  • HY-169085
    LRAT-IN-1
    Inhibitor
    LRAT-IN-1 (compound 1) is a retinol acyltransferase (LRAT) inhibitor (IC50=21.1 μM). LRAT-IN-1 provides anti-aging effects by inhibiting the esterification of retinol to form retinol esters, increasing the available retinol in the skin. Research on LRAT-IN-1 as an anti-aging ingredient in cosmetics.
    LRAT-IN-1
  • HY-N14574
    Glisoprenin C
    Inhibitor
    Glisoprenin C is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea.
    Glisoprenin C
  • HY-13215R
    Avasimibe (Standard)
    Inhibitor
    Avasimibe (Standard) is the analytical standard of Avasimibe. This product is intended for research and analytical applications. Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
    Avasimibe (Standard)
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