Diacylglycerol Acyltransferase Inhibitor-1, a diacylglycerol acyltransferase (DGAT1) inhibitor, effectively suppresses the activity of DGAT1.

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

2-Furoic acid (Furan-2-carboxylic acid) 2-Furoic acid can reduce serum cholesterol and triglyceride levels and has anti-lipidemic effects.

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

DGAT-1 inhibitor 2 is an effective DGAT-1 inhibitor; anti-obesity drug. Objective: DGAT-1 acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step of triglyceride synthesis. The discovery of transgenic mice and pharmacological studies indicate that inhibiting DGAT1 is a promising strategy for treating obesity and type 2 diabetes.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

OGT-IN-2 is a potent O-GlcNAc transferase (OGT) inhibitor. OGT-IN-2 inhibits sOGT and ncOGT with IC50 values of 30 μM and 53 μM, respectively[1]. OGT-IN-2 can be used for the research of articular diseases[1].

Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K shows weak antiviral activity against Herpes simplex virus types I and II.

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular signaling, vesicle fission and fusion, as well as mitochondrial division and fusion. It stimulates respiratory burst in neutrophils independent of diacylglycerol and activates monoacylglycerol acyltransferase, phospholipase C (PLC), Ras, and phosphatidylinositol 4-phosphate (PIP4) kinase in several cell lines. Phosphatidic acids (egg) is a mixture of phosphatidic acids isolated from chicken egg with fatty acids of variable chain lengths.

PF-07202954, a weakly basic diacylglycerol O-acyltransferase 2 (DGAT2) inhibitor, exhibits an inhibition concentration half-maximum (IC50) of 10 nM against human DGAT2 and effectively reduces liver triglyceride content in a rat model fed on a Western diet [1].

JNJ-DGAT2-B is a selective inhibitor of Diacylglycerol acyltransferase 2.

VULM 1457 is a potent ACAT inhibitor. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells.

RP 70676 is a potent ACAT inhibitor(rat and rabbit ACAT with IC50 of 25 and 44 nM ).

DGAT1-IN-1 is a potent inhibitor of diacylglycerol O- acyltransferase type 1(DGAT1, IC50 of < 10 nM).

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, exhibits IC50 values of 20.1 μM and 34.1 μM, respectively. Additionally, it demonstrates significant anti-Helicobacter pylori activity, boasting a minimum inhibitory concentration (MIC) of 10 μg/mL [1] [2] [3].

H2-005 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

Xanthohumol, also known as 2', 4, 4'-trihydroxy-6'-methoxy-3'-prenylchalcone or desmethylxanthohumol, is a member of the class of compounds known as 3-prenylated chalcones. It inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).

Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor. Ervogastat reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).

Aphadilactone C shows significant antimalarial activity with the IC50 value of 170 ± 10 nM. It shows potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 uM, selectivity index > 217).

7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone shows diacylglycerol acyltransferase (DGAT)1 inhibition with IC(50) values of 47.0 microM (for rat liver microsomes) and 160.7 microM (for HepG2 cell microsomes),

ALN29882 is a glycerolipid, that is located at the plasma membrane. It is made up of two fatty acid chains that are covalently attached to a single glycerol molecule with the help of an ester linkage. 18:1 DG has been used as a diacyl-glycerol source in diacylglycerol O-acyltransferase 1 (DGAT1) assay. It has also been used as substrate to assess compounds as potential inhibitors of DGAT-1 in DGAT-1 enzyme assay. It is suitable to use in lipid-protein overlay screen assay with the recombinant protein His-AtROP6.

YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.

AZD3988 is an orally active and highly potent inhibitor of diacylglycerol acyltransferase-1 (DGAT-1) for the study of diabetes and obesity.

10,12-Tricosadiynoic acid is a highly selective and orally active inhibitor of acyl-CoA oxidase-1 (ACOX1). It can treat the high-fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism.

Cochlioquinone A is an inhibitor of diacylglycerol kinase (DGK) and diacylglycerol acyltransferase (DGAT). It has been shown to reduce the concentration of phosphatidic acid in T cell lymphoma and has also been shown to compete with macrophage inflammatory protein-1α for binding to human CCR5 chemokine receptors.

PF-06424439 is an oral and selective inhibitor of imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) (IC50 of 14 nM).

PD 128042 (CI 976) is a potent orally active and selective ACAT inhibitor(IC50: 73 nM) and a potent lysophospholipid acyltransferase(LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

1-Palmitoyl-3-oleoyl-rac-glycerol, a diacylglycerol featuring palmitic acid at the sn-1 position and oleic acid at the sn-3 position, serves as a substrate for diacylglycerol acyltransferase (DAGAT) in myotubes.

YM-750 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC50 value of 0.18 μM. ACAT is an enzyme that catalyzes the conversion of cholesterol and long-chain fatty-acyl-coenzyme A into cholesteryl esters.

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of acyl-CoA: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959. J. Antibiot. (Tokyo) 55(11), 1004-1008 (2002).|2. Lee, S.W., Rho, M.C., Choi, J.H., et al. Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959. J. Microbiol. Biotechnol. 18(11), 1785-1788 (2008).|3. Horikoshi, R., Goto, K., Mitomi, M., et al. Identification of pyripyropene A as a promising insecticidal compound in a microbial metabolite screening. J. Antibiot. (Tokyo) 70(3), 272-276 (2017).

K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 inhibitor with an IC50 of 0.45±0.06 μM.

RHC 80267 (U-57908) is a selective inhibitor of DAGL (IC50 : 4 μM in canine platelets)

PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2.

PF-06427878 is an orally active, potent and selective diacylglycerol acyltransferase 2 inhibitor.

RP-64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor.

H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

Avasimibe (PD-148515) is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the arterial wall. It also inhibits human P450 isoenzymes CYP2C9/1A2/2C19 (IC50: 2.9/13.9/26.5 μM).

ESI-05 (NSC-116966) is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.

5-Methylcytosine is a methylated nucleotide base found in eukaryotic DNA. It is an epigenetic modification formed by the action of DNA methyltransferases.