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-119738
    OSMI-1
    		Inhibitor 99.88%
    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.
    OSMI-1
  • HY-10038
    A 922500
    		Inhibitor 99.33%
    A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
    A 922500
  • HY-13215
    Avasimibe
    		Inhibitor 99.85%
    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.
    Avasimibe
  • HY-108341A
    PF-06424439 methanesulfonate
    		Inhibitor 99.93%
    PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
    PF-06424439 methanesulfonate
  • HY-32219
    T863
    		Inhibitor 99.83%
    T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1) inhibitor with an IC50 of 15 nM. T863 has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
    T863
  • HY-181943
    SPT-IN-2
    		Inhibitor 99.45%
    SPT-IN-2 is an orally active serine palmitoyltransferase (SPT) inhibitor (with an IC50 of 0.71 nM against human SPT2). SPT-IN-2 inhibits ceramide synthesis, suppresses cancer cell growth, and exhibits in vivo anti-tumor activity, favorable metabolic stability and cell membrane permeability in xenograft mouse models. SPT-IN-2 blocks the de novo sphingolipid synthesis pathway, significantly reducing intracellular ceramide levels and the levels of 3-ketodihydrosphingosine (3-KDS), the immediate downstream product of SPT. SPT-IN-2 can be used in research related to lung adenocarcinoma, acute promyelocytic leukemia and breast cancer.
    SPT-IN-2
  • HY-182274
    DM245
    		Activator
    DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure.
    DM245
  • HY-133491
    ST1060
    		Inhibitor
    ST1060, FTY720 (HY-12005) derivative, is a selective ceramide synthase 2 (CerS2) inhibitor. ST1060 can reduce the level of long-chain dihydroceramide (dhCer) catalyzed by CerS2 with IC50 values of 63.6, and 61.3 μM for C24:0 and C24:1
    ST1060
  • HY-108341
    PF-06424439
    		Inhibitor 99.98%
    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
    PF-06424439
  • HY-114361
    OSMI-4
    		Inhibitor 99.69%
    OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells.
    OSMI-4
  • HY-135425
    10,12-Tricosadiynoic acid
    		Inhibitor 99.95%
    10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism. 10,12-Tricosadiynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    10,12-Tricosadiynoic acid
  • HY-N6719
    Fumonisin B1
    		Inhibitor 99.96%
    Fumonisin B1 is a mycotoxin produced from Fusarium moniliforme. Fumonisin B1 is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis. Fumonisin B1 is the most abundant and toxic fumonisin.
    Fumonisin B1
  • HY-N1067
    Xanthohumol
    		Inhibitor 99.94%
    Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity against bovine viral diarrhea virus (BVDV), rhinovirus, HSV-1, HSV-2 and cytomegalovirus (CMV).
    Xanthohumol
  • HY-100400A
    K-604 dihydrochloride
    		Inhibitor 99.42%
    K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.
    K-604 dihydrochloride
  • HY-13009
    PF-04620110
    		Inhibitor 99.60%
    PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC50 of 19 nM.
    PF-04620110
  • HY-112489
    FSG67
    		Inhibitor 99.95%
    FSG67 is a glycerol 3-phosphate acyltransferase (GPAT) inhibitor with an IC50 of 24 μM.
    FSG67
  • HY-W015239
    KAT8-IN-1
    		99.61%
    KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases.
    KAT8-IN-1
  • HY-113054
    DL-Glyceraldehyde 3-phosphate
    		Inhibitor
    DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase.
    DL-Glyceraldehyde 3-phosphate
  • HY-P5282
    ApoA-I mimetic peptide
    		Activator 98.90%
    ApoA-I mimetic peptide is an ApoA-I mimetic peptide. ApoA-I mimetic peptide has good phosphatidylcholine: cholesterol acyltransferase (LCAT) activation activity. ApoA-I mimetic peptide can be used to synthesize peptide/lipid complexes. ApoA-I mimetic peptide can be used in atherosclerosis research. (The sequence is: PVLDLFRELLNELLEALKQKLK).
    ApoA-I mimetic peptide
  • HY-117656
    ESI-05
    		Inhibitor 99.78%
    ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
    ESI-05
Cat. No. Product Name / Synonyms Application Reactivity
Acyltransferase Isoform Comparison

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