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-139629
    ANAT inhibitor-1
    ANAT inhibitor-1 is a human aspartate N-acetyltransferase (ANAT) inhibitor for canavan disease.
    ANAT inhibitor-1
  • HY-19112
    447C88
    Inhibitor
    447C88 is an acyl-coenzyme A cholesterol acyltransferase (ACAT) inhibitor with an IC50 of 23 nM. 447C88 can reduce plasma cholesterol levels and can be used in the research of endocrine and metabolic diseases such as hyperlipidemia.
    447C88
  • HY-120082
    FR-182980
    Inhibitor
    FR-182980 is an orally active ACAT1 inhibitor (IC50: 30 nM). FR-182980 has hypocholesterolemic activity and can be used for research of atherosclerosis.
    FR-182980
  • HY-162978
    DGAT2-IN-3
    Inhibitor
    DGAT2-IN-3 (compound 9) is a DGAT2 inhibitor, with IC50 of 0.4 nM. DGAT2-IN-3 can be used in the research of steatohepatitis, diabetes and cardiovascular diseases.
    DGAT2-IN-3
  • 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-181719
    NAT8L-IN-1
    Inhibitor
    NAT8L-IN-1 is a NAT8L inhibitor with an IC50 value of 0.3 μM. NAT8L-IN-1 can be used for the research of Canavan disease.
    NAT8L-IN-1
  • HY-N18066
    Esculeogenin A
    Inhibitor
    Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.
    Esculeogenin A
  • 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
  • HY-113671
    Belfosdil
    Inhibitor
    Belfosdil is an orally active and highly specific calcium channel blocker that also inhibits the activity of acyl coenzyme A cholesterol acyltransferase.
    Belfosdil
  • HY-133968S1
    24-Methylenecholesterol-13C
    Activator
    24-Methylenecholesterol-13C (Ostreasterol-13C) is the 13C labeled 24-Methylenecholesterol (HY-133968). 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-<sup>13</sup>C
  • HY-114952
    SM-32504
    Inhibitor
    SM-32504 is an effective ACAT inhibitor that can significantly reduce serum cholesterol levels in mouse models fed with high-fat and high-cholesterol diets. SM-32504 can be used for research on hypercholesterolemia and atherosclerosis.
    SM-32504
  • HY-139019
    ACAT-IN-2
    Inhibitor
    ACAT-IN-2 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 187. ACAT-IN-2 inhibits NF-κB mediated transcription.
    ACAT-IN-2
  • HY-19183
    E-5324
    Inhibitor
    E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.
    E-5324
  • HY-133968R
    24-Methylenecholesterol (Standard)
    Activator
    24-Methylenecholesterol (Ostreasterol) (Standard) is the analytical standard of 24-Methylenecholesterol (HY-133968). This product is intended for research and analytical applications. 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 (Standard)
  • HY-180395
    (Rac)-GSK2973980A
    Inhibitor
    (Rac)-GSK2973980A (Compound 215) is a DGAT1 inhibitor with an IC50 of 1.8 nM for hDGAT1. (Rac)-GSK2973980A can be used for research on obesity and obesity-related diseases.
    (Rac)-GSK2973980A
  • HY-138942
    PF-06427878
    Inhibitor
    PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC50s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases.
    PF-06427878
  • HY-19140
    YM-17E hydrochloride
    Inhibitor
    YM17E hydrochloride is an acyl CoA:cholesterol acyltransferase (ACAT) inhibitor, with IC50 of 44 nM. YM17E hydrochloride has hypocholesterolemic effect.
    YM-17E hydrochloride
  • HY-N10234
    Phenylpyropene A
    Inhibitor
    Phenylpyropene A, a fungal metabolite, is a potent acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor with an IC50 of 0.8 μM.
    Phenylpyropene A
  • HY-16149
    SDZ-CPI 975
    Inhibitor
    SDZ-CPI-975 is a novel, reversible, and selective CPT I inhibitor. SDZ-CPI-975 effectively inhibits fatty acid oxidation and lowers blood glucose levels.
    SDZ-CPI 975
  • HY-182273
    DM243
    Inhibitor
    DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769 for EPAC1. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts.
    DM243
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