1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Acyltransferase

Acyltransferase

Diacylglycerol acyltransferase; Diglyceride acyltransferase; acyl-CoA:cholesterol acyltransferase; mono- acylglycerol acyltransferase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N9524
    Ilexoside XLVIII
    Inhibitor
    Ilexoside XLVIII is an acyl CoA cholesteryl acyl transferase (ACAT) inhibitor. Ilexoside XLVIII is a triterpene saponin isolated from an aqueous extract of the leaves of Ilex kudincha.
    Ilexoside XLVIII
  • HY-129295
    Amidepsine D
    Inhibitor
    Amidepsine D is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.
    Amidepsine D
  • HY-16281
    Lecimibide
    Inhibitor
    Lecimibide (DuP 128) is a potent and specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor for antihyperlipidemia research.
    Lecimibide
  • HY-106902
    F-1394
    Inhibitor
    F-1394 is an orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that inhibits dietary cholesterol absorption in mice. F-1394 can be used in cardiovascular disease research.
    F-1394
  • HY-N3806S
    Enniatin B-13C33
    Enniatin B-13C33 is the 13C-labeled Enniatin B (HY-N3806). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes. Enniatins B decreases the activation of ERK (p44/p42).
    Enniatin B-<sup>13</sup>C<sub>33</sub>
  • HY-16088
    BAY 74-4113
    Inhibitor
    BAY 74-4113 is a DGAT1 inhibitor (IC50: 72 nM). BAY 74-4113 can be used in obesity research.
    BAY 74-4113
  • HY-107176
    (E)-Hyzetimibe
    Inhibitor
    (E)-Hyzetimibe ((E)-HS-25) (Compound I-1Z) is the trans isomer of Hyzetimibe (HY-107176A), a cholesterol-lowering agent. (E)-Hyzetimibe has cholesterol acyltransferase (ACTA) inhibitory activity, but its cholesterol-lowering effect is relatively weak. (E)-Hyzetimibe can inhibit the entry of hepatitis C virus (HCV) into host cells, and it has a synergistic effect when used in combination with interferon-α. (E)-Hyzetimibe can be used for the study of HCV infection.
    (E)-Hyzetimibe
  • 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-19251
    CL-283796
    Inhibitor
    CL-283796 is a potent and orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.
    CL-283796
  • 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-N6702S
    Enniatin A-13C36
    Enniatin A-13C36 is the 13C-labeled Enniatin A (HY-N6702). Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes.
    Enniatin A-<sup>13</sup>C<sub>36</sub>
  • HY-123666
    Bay-02752
    Inhibitor
    Bay-02752 (Bay o 2752) is a lipid-lowering agent. Bay-02752 inhibits acyl-CoA activity in liver microsomes (IC50 = 0.95 μg/mL). Bay-02752 inhibits intestinal cholesterol absorption in rats. Bay-02752 inhibits gallstone formation in hamsters.
    Bay-02752
  • HY-182248
    Teglicar chloride
    Inhibitor
    Teglicar chloride (ST1326 chloride) is an orally active, reversible, mixed-type, selective inhibitor of hepatic carnitine palmitoyltransferase I (L-CPT I), with an IC50 of 1.1 μM against rat L-CPT I. Teglicar chloride reduces serum glucose levels. Teglicar chloride exhibits antiketotic activity in normal fasted rats. Teglicar chloride can be used in research related to type 2 diabetes and ketoacidosis.
    Teglicar chloride
  • 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-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-N17326
    Ilekudinol B
    Inhibitor
    Ilekudinol B is an inhibitor of ACAT and PTP1B, with an IC50 of 5.3 μM and a Ki of 11.6 μM against human PTP1B. Ilekudinol B inhibits the classical pathway of the complement system, with an IC50 of 51 μM. Ilekudinol B inhibits TNF-α-induced cellular IL-8 secretion, promotes glucose uptake in skeletal muscle myotubes, and acts as an insulin mimetic and insulin sensitizer. Ilekudinol B can be used in research related to type 2 diabetes, obesity, and inflammatory diseases.
    Ilekudinol B
  • 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
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