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-139026
    ACAT-IN-9
    		Inhibitor
    ACAT-IN-9 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 207. ACAT-IN-9 inhibits NF-κB mediated transcription.
    ACAT-IN-9
  • HY-139021
    ACAT-IN-4
    		Inhibitor
    ACAT-IN-4 (Example 208) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-4 inhibits NF-κB mediated transcription.
    ACAT-IN-4
  • HY-N9530
    1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone
    		Inhibitor
    1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a quinolone alkaloid, is a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, with IC50s of 20.1 μM and 34.1 μM, respectively. 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone shows potent anti-Helicobacter pylori activity with the MIC of 10 μg/mL.
    1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone
  • HY-139027A
    ACAT-IN-10 dihydrochloride
    		Inhibitor
    ACAT-IN-10 dihydrochloride is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 dihydrochloride weakly inhibits NF-κB mediated transcription.
    ACAT-IN-10 dihydrochloride
  • HY-175646
    AGPAT4-IN-1
    		Inhibitor
    AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. AGPAT4-IN-1 covalently binds to AGPAT4 at Cys228 and significantly inhibits acyltransferase activity, LPA-to-PA conversion and downstream mTOR/S6K pathways. AGPAT4-IN-1 sensitizes hepatocellular carcinoma (HCC) tumors to Sorafenib (HY-10201) and significantly induces apoptosis with a synergistic response. AGPAT4-IN-1 has antitumor activity and reduces tumorigenicity and stemness in HCC xenograft mouse models.
    AGPAT4-IN-1
  • HY-115734
    Phenylpyropene C
    		Inhibitor
    Phenylpyropene C (S14-95), a JAK/STAT pathway inhibitor, can inhibit IFN-γ mediated expression of the reporter gene (IC50=5.4~10.8 μM). Phenylpyropene C also is an inhibitor of acyl-CoA, with an IC50 of 16.0 μM.
    Phenylpyropene C
  • HY-139023
    ACAT-IN-6
    		Inhibitor
    ACAT-IN-6 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 200. ACAT-IN-6 potently inhibits NF-κB mediated transcription.
    ACAT-IN-6
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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