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-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-139629
    ANAT inhibitor-1
    ANAT inhibitor-1 is a human aspartate N-acetyltransferase (ANAT) inhibitor for canavan disease.
    ANAT inhibitor-1
  • HY-168428
    CHI-KAT8i5
    		Inhibitor
    CHI-KAT8i5 is a selective KAT8 inhibitor with a KD value of 19.72 μM. CHI-KAT8i5 induces Apoptosis in a dose-dependent manner. CHI-KAT8i5 suppresses inhibit tumor growth in esophageal squamous cell carcinoma, colon cancer, melanoma, gastric cancer, non-small cell adenocarcinoma, and liver cancer.
    CHI-KAT8i5
  • 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-169813
    Yakuchinone B
    		Inhibitor
    Yakuchinone B is an Acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitor with hypocholesterolemic activity, which is found in the seeds of Zingiberaceae. Yakuchinone B inhibits rat hepatic ACAT with an IC50 value of 20.6 μM. Yakuchinone B is promising for research of hypercholesterolemia and atherosclerosis.
    Yakuchinone B
  • 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
  • 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), 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-<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 (Standard)
  • HY-170794
    ALT-007
    		Inhibitor
    ALT-007 is an orally effective serine palmitoyltransferase (SPT) inhibitor. SPT is the rate-limiting enzyme for the de novo synthesis of ceramide. In a mouse model of age-related sarcopenia, ALT-007 can effectively restore the muscle mass and function impaired by aging. ALT-007 may enhance protein homeostasis in Caenorhabditis elegans and mouse models of aging and age-related diseases and play the role of a ceramide inhibitor.
    ALT-007
  • 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-106938
    Eldacimibe
    		Inhibitor
    Eldacimibe is an ACAT2 inhibitor. Eldacimibe can lower plasma cholesterol levels by blocking cholesterol absorption and can prevent macrophages from turning into foam cells. Eldacimibe can be used in the study of cardiovascular diseases (atherosclerosis), endocrine and metabolic diseases (hypercholesterolemia) .
    Eldacimibe
  • HY-N8331
    Terpendole I
    		Inhibitor
    Terpendole I, a fungal indoloditerpene, is a ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor (IC50=145 µM).
    Terpendole I
  • HY-W104819
    4-Hydroxyphenylglyoxylate
    		Inhibitor
    4-Hydroxyphenylglyoxylate (4-Hydroxyphenylglyoxylic acid) is an inhibitor of carnitine palmitoyltransferase I (CPT I). 4-Hydroxyphenylglyoxylate can be used to study sensitivity changes in CPT I of liver mitochondria and fatty acid oxidation by isolated hepatocytes. 4-Hydroxyphenylglyoxylate can inhibits fatty acid oxidation.
    4-Hydroxyphenylglyoxylate
  • HY-16278A
    Pradigastat sodium
    		Inhibitor
    Pradigastat sodium (LCQ 908 sodium) 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 sodium
  • HY-145624
    Obeversen
    		Inhibitor
    Obeversen is an antisense oligonucleotide that inhibits the synthesis of diacylglycerol acyltransferase 2 (DGAT-2). Obeversen can be used in the research of nonalcoholic fatty liver disease.
    Obeversen
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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