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-156259
    PF-07202954
    		Inhibitor
    PF-07202954 is a weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2. PF-07202954 lowers liver triglyceride content in a Western-diet-fed rat model.
    PF-07202954
  • HY-112487
    Sandoz 58-035
    		Inhibitor 98.70%
    Sandoz 58-035 is a competitive inhibitor of cholesterol acyltransferase (ACAT). Sandoz 58-035 effectively inhibits (>98%) hormonally stimulated cholesterol esterification in cells.
    Sandoz 58-035
  • HY-N3807
    Enniatin B1
    		Inhibitor 99.34%
    Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
    Enniatin B1
  • HY-100401A
    Pactimibe sulfate
    		Inhibitor ≥98.0%
    Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
    Pactimibe sulfate
  • HY-107571
    VULM 1457
    		Inhibitor 99.71%
    VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia.
    VULM 1457
  • HY-105445
    CP-113818
    		Inhibitor 99.13%
    CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease.
    CP-113818
  • HY-101627
    YM17E
    		Inhibitor 98.34%
    YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
    YM17E
  • HY-100401
    Pactimibe
    		Inhibitor 99.98%
    Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
    Pactimibe
  • HY-19286
    Eflucimibe
    		98.60%
    Eflucimibe (F 12511) is a new acyl-coenzyme A cholesterol O-acyltransferase (ACAT) inhibitor. Eflucimibe can be used in the research of atherosclerosis.
    Eflucimibe
  • HY-107570
    IWP-12
    		Inhibitor ≥99.0%
    IWP-12 is a potent inhibitor of porcupine (PORCN) and inhibits cell-autonomous Wnt signaling with an IC50 of 15 nM.
    IWP-12
  • HY-15197
    ABT-046
    		Inhibitor 98.13%
    ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1.
    ABT-046
  • HY-100399
    Nevanimibe
    		Inhibitor
    Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
    Nevanimibe
  • HY-N6706
    Enniatin complex
    		Inhibitor 99.81%
    Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .
    Enniatin complex
  • HY-118486
    LDL-IN-1
    		Inhibitor ≥99.0%
    LDL-IN-1 (Compound 1) is an antioxidant, and is active against copper mediated LDL oxidation (IC50 = 52 μM). LDL-IN-1 is also an Acyl-CoA:cholesterol acyltransferase-1 and -2 (ACAT-1/2) inhibitor, with IC50s of 60 μM. LDL-IN-1 can be used for anti-atherosclerotic research.
    LDL-IN-1
  • HY-111880
    γ-Sanshool
    		Inhibitor 99.23%
    γ-Sanshool can be isolated from Zanthoxylum piperitum. γ-Sanshool inhibits human ACAT-1 and ACAT-2 activities with IC50s of 12.0 and 82.6 μM.
    γ-Sanshool
  • HY-W012946S
    2-Furoic acid-d3
    2-Furoic acid-d3 is the deuterium labeled 2-Furoic acid[1]. 2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation[2]. 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats[3].
    2-Furoic acid-d<sub>3</sub>
  • HY-N6739S
    Beauvericin-13C45
    		Inhibitor ≥99%
    Beauvericin-13C45 is 13C labeled 2,5-Dimethylpyrazine (HY-34439). 2,5-Dimethylpyrazine is an endogenous metabolite.
    Beauvericin-<sup>13</sup>C<sub>45</sub>
  • HY-119738A
    (Rac)-OSMI-1
    		Inhibitor
    (Rac)-OSMI-1 is the racemate of OSMI-1. OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.
    (Rac)-OSMI-1
  • HY-125319
    Amidepsine A
    		Inhibitor 98.38%
    Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.
    Amidepsine A
  • HY-139630
    ANAT inhibitor-2
    		Inhibitor 99.23%
    ANAT inhibitor-2 is a ANAT inhibitor for canavan disease, with an IC50 value of 20 μM.
    ANAT inhibitor-2
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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