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-N0631
    Cornuside
    		Inhibitor 99.99%
    Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.
    Cornuside
  • HY-50861
    AZD3988
    		Inhibitor 99.89%
    AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity.
    AZD3988
  • HY-N4193
    Glabrol
    		Inhibitor 99.83%
    Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity.
    Glabrol
  • HY-101722
    Melinamide
    		99.9%
    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
  • HY-132924
    BMS-963272
    		Inhibitor 99.02%
    BMS-963272 is an orally active and selective MGAT2 inhibitor (IC50 = 7.1 nM), used for the study of metabolic disorders and inflammatory diseases.
    BMS-963272
  • 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-175341
    Rac1-IN-5
    		99.84%
    Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer.
    Rac1-IN-5
  • HY-50670
    DGAT-1 inhibitor 2
    		Inhibitor
    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
  • HY-161906
    SD-066-4
    		Inhibitor 99.96%
    SD-066-4 is an orally active acyltransferase inhibitor. SD-066-4 can be used in cancer research.
    SD-066-4
  • 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-15197
    ABT-046
    		Inhibitor 98.57%
    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-135784
    OSMI-2
    		Inhibitor 99.59%
    OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
    OSMI-2
  • HY-170794
    ALT-007
    		Inhibitor 99.81%
    ALT-007 is an orally active serine palmitoyltransferase (SPT) inhibitor that selectively reduces the levels of toxic very-long-chain deoxysphingolipids to enhance protein homeostasis. ALT-007 restores aging-related loss of muscle mass in a mouse model of sarcopenia. ALT-007 enhances protein homeostasis in both mouse and C. elegans models of aging and disease. ALT-007 can be used for age-related neuromuscular diseases research.
    ALT-007
  • HY-105445
    CP-113818
    		Inhibitor 99.70%
    CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease.
    CP-113818
  • HY-100399
    Nevanimibe
    		Inhibitor 98.99%
    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-W104819
    4-Hydroxyphenylglyoxylate
    		Inhibitor 99.69%
    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-N6723
    Fumonisin B2
    		Inhibitor 99.99%
    Fumonisin B2 is a selective ceramide synthase inhibitor and carcinogenic mycotoxin with toxicity comparable to that of Fumonisin B1 (HY-N6719). Fumonisin B2 inhibits de novo sphingolipid biosynthesis by blocking the amide bond formation between fatty acids and dihydrosphingosine, which leads to a massive intracellular accumulation of free dihydrosphingosine, altered sphingosine levels, subsequent inhibition of cell proliferation, and induction of cell death. Fumonisin B2 is used to investigate the pathogenesis of diseases associated with Fusarium verticillioides contamination, including equine leukoencephalomalacia, porcine pulmonary edema syndrome, human esophageal cancer, and rat hepatocellular carcinoma.
    Fumonisin B2
  • HY-117651
    2-Fluoropalmitic acid
    		Inhibitor 98.0%
    2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines.
    2-Fluoropalmitic acid
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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