Acyltransferase

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.

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

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

Cyclandelate (BS 572), a direct-acting smooth muscle relaxant, is used to dilate blood vessels.

Eflucimibe (L0081) is an acyl coenzyme A: cholesterol acyltransferase inhibitor for the treatment of cardiovascular disease and endocrine and metabolic disorders, and can be used to study atherosclerosis and hyperlipidemia.

Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A: cholesterol acyltransferase (ACAT), which can be used to study diseases due to high lipids.

RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM.RU-SKI 43 has anticancer activity and is a potential compound for the treatment of lung adenocarcinomas.RU-SKI 43 reduces Gli-1 activation through smoothing-independent non-canonical signalling and inhibits Akt and mTOR pathway activity.

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

TMP-153 is a novel and potent ACAT inhibitor with an IC50 value of 5-10 nM for intestinal and hepatic ACAT in animals.TMP-153 has a hypocholesterolemic effect, inhibiting cholesterol uptake and lowering plasma cholesterol in rats and hamsters.

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.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

BMS-986172 is an orally active, highly selective inhibitor of MGAT2, demonstrating inhibitory concentrations (IC50) of 4.6 nM for human MGAT2 (hMGAT2) and 20 nM for mouse MGAT2 (mMGAT2). It exhibits a half-life (T1/2) greater than 120 minutes in vitro and is known to decrease food intake and body weight. This compound is considered promising for the research of metabolic disorders, including obesity and non-alcoholic steatohepatitis (NASH) [1].

Eldacimibe (WAY-ACA-147) is an ACAT2 inhibitor for the treatment of cardiovascular disease and endocrine and metabolic disorders, study of atherosclerosis and hypercholesterolemia.

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].

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 ).

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.

(R)-HTS-3, a lysophosphatidylcholinacyltransferase 3 (LPCAT3) inhibitor, remodels polyunsaturated phospholipid content in human cells and reduces RSL3-induced iron death in cancer cells.

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).

BAY-3827 is a potent and selective AMPK inhibitor with potential antitumor activity, showing antiproliferative activity in an androgen-dependent prostate cancer model. BAY-3827 inhibits the phosphorylation of acetyl CoA carboxylase 1.

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

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.

Beauvericin, a Fusarium mycotoxin, inhibits acyl-CoA:cholesterol acyltransferase (ACAT) in rat liver microsomal enzyme assays with an IC50 value of 3 μM.

ACAT-IN-1 cis isomer is a potent ACAT inhibitor (IC50: 100 nM) for the study of immune system-related diseases.

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

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).

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

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.

Monatepil 2maleate is an orally active Ca2+-channel antagonist and ACAT inhibitor with alpha(1)-adrenergic receptor blocking activity and antiarrhythmic properties that inhibit vasoconstriction.Monatepil 2maleate may be used to study atherosclerosis.

24-Methylenecholesterol (24 Methylenecholesterol) is a natural marine sterol, which stimulates cholesterol acyl transferase (ACAT) in human macrophages.

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.

Lateritin (Bassiatin) is An Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor and a platelet aggregation inhibitor from the mycelial cake of Gibberella lateritium. Bassiatin is the (3S,6R) isomer.

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.

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

BMS-963272 is a selective and potent MGAT2 inhibitor with an IC50 value of 7.1 nM used in the study of metabolic disorders and obesity.

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