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-16437
    RP-64477
    		Inhibitor 99.62%
    RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
    RP-64477
  • HY-103479
    GOAT-IN-1
    		Inhibitor 99.38%
    GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
    GOAT-IN-1
  • HY-16434
    DGAT1-IN-3
    		Inhibitor 99.92%
    DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.
    DGAT1-IN-3
  • HY-107396
    YM-750
    		Inhibitor 99.95%
    YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.
    YM-750
  • 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-175646
    AGPAT4-IN-1
    		Inhibitor 99.04%
    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-N0853A
    Alisol A 24-acetate
    		Activator 98.0%
    Alisol A 24-acetate (Alisol A monoacetate) is an orally active derivative of protostane-type tetracyclic triterpenoid. Alisol A 24-acetate upregulates the expression of adiponectin, AMPKα, CPT1, and ACOX1; downregulates the expression of SREBP-1c, ACC, FAS, Bcl-2, Bcl-xl, PPAR-γ, perilipin A, and NFATc1; inhibits the activity of PI3K/Akt/mTOR and HMGR; and activates the PKA and ERK signaling pathways. Alisol A 24-acetate regulates cell apoptosis (apoptosis), autophagy (Autophagy, hepatic lipid accumulation, inflammatory response, neuroprotection, MRSA membrane integrity, and osteoclast differentiation. Alisol A 24-acetate can be used in research related to non-alcoholic fatty liver disease, nephrotoxicity, obesity, global cerebral ischemia-reperfusion injury, bacterial infection, and osteoporosis.
    Alisol A 24-acetate
  • HY-116073
    L-Penicillamine
    		Inhibitor 99.71%
    L-Penicillamine is an orally active serine palmitoyltransferase (SPT) inhibitor. L-Penicillamine inactivates the PLP cofactor by forming adducts, thereby inhibiting SPT activity and reducing sphingolipid biosynthesis. L-Penicillamine not only blocks tumor access to vitamin B6, but also stabilizes the human papillomavirus 16 E6 oncoprotein monomer and inhibits its polymerization, exhibiting a unique anticancer mechanism. L-Penicillamine effectively delays the growth of Sarcoma-180, induces tumor necrosis and prolongs survival (though long-term use may lead to Pyridoxine (HY-B1328) deficiency and weight loss).
    L-Penicillamine
  • HY-159904
    ChAT IN-1
    		Inhibitor 98.51%
    ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD).
    ChAT IN-1
  • 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-159698A
    IONIS-DGAT 2Rx sodium
    		Inhibitor
    IONIS-DGAT 2Rx (ION-224) sodium is a DGAT2 inhibitor, which is promising for research of atherosclerosis.
    IONIS-DGAT 2Rx sodium
  • HY-169499
    (R)-2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxylic Acid
    		99.9%
    (R)-2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxylic Acid is an intermediate in the synthesis of the diacylglycerol acyltransferase 2 (DGAT-2) inhibitor Ervogastat.
    (R)-2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxylic Acid
  • HY-108339
    PF-06471553
    		Inhibitor 98.29%
    PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
    PF-06471553
  • HY-121254
    GERI-BP002-A
    		Inhibitor 99.77%
    GERI-BP002-A is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) produced by Aspergillus fumigatus F93, which can be used in cancer research.
    GERI-BP002-A
  • HY-157521
    AANAT-IN-1
    		Inhibitor 99.87%
    AANAT-IN-1 is an arylalkylamine N-acetyltransferase (AANAT) inhibitor with a sheep AANAT IC50 of 9.9 μM. AANAT-IN-1 binds to the active site of sheep AANAT, interacting with amino acid residues via hydrogen bonds, hydrophobic interactions, ionic interactions, and water bridges, inhibiting the enzyme's catalytic activity. AANAT-IN-1 can be used for the researches of circadian rhythm-associated neuropsychiatric conditions, seasonal affective disorder, and other diseases associated with abnormally elevated melatonin levels.
    AANAT-IN-1
  • HY-W420033
    (S)-(+)-Etomoxir
    		Control 98.65%
    (S)-(+)-Etomoxir is the S enantiomer of Etomoxir (HY-50202). Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
    (S)-(+)-Etomoxir
  • HY-149663
    BMS-986172
    		Inhibitor 99.48%
    BMS-986172 is an orally active and selective Monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 4.6 nM and 20 nM for hMGAT2 and mMGAT2, respectively. BMS-986172 reduces food intake and body weight. BMS-986172 can be used for the researches of metabolic diseases, such as obesity .
    BMS-986172
  • HY-139630
    ANAT inhibitor-2
    		Inhibitor 98.38%
    ANAT inhibitor-2 is a ANAT inhibitor for canavan disease, with an IC50 value of 20 μM.
    ANAT inhibitor-2
  • HY-N6739S
    Beauvericin-13C45
    		Inhibitor ≥99%
    Beauvericin-13C45 is 13C labeled Beauvericin (HY-N6739). Beauvericin is a cyclohexapeptide Fusarium toxin with insecticidal, antibacterial, anticancer, antiviral and cytotoxic activities. Beauvericin causes cellular genotoxicity by producing DNA breaks, chromosomal aberrations and micronuclei, and inhibits the PI3K/AKT pathway to induce apoptosis, thereby inhibiting the growth of HCC. In addition, Beauvericin affects immune function by inhibiting lymphocyte proliferation and interfering with the differentiation process of human monocytes into macrophages.
    Beauvericin-<sup>13</sup>C<sub>45</sub>
  • HY-101576
    RP 70676
    		Inhibitor 99.74%
    RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.
    RP 70676
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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