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.

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).

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.

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

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.

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

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

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

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

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

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.

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

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

BAY-3827 is a potent and selective AMPK inhibitor with potential antitumor activity, demonstrating antiproliferative effects in an androgen-dependent prostate cancer model and inhibiting the phosphorylation of acetyl CoA carboxylase 1 (ACC-1).

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.

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

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

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

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

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

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

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.

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

Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A:cholesterol acyltransferase (ACAT), useful for studying high-lipid-related diseases.

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.

2-Furoic acid (Furan-2-carboxylic acid) reduces serum cholesterol and triglyceride levels and exhibits anti-lipidemic effects.

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

RHC 80267 (U-57908) is a selective inhibitor of DAGL, with an IC50 of 4 μM in canine platelets.

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.

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.

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.

Fumonisin B1 (Fumonisin-B1) is a mycotoxin produced by Fusarium oxysporum that is widely present in crops, contaminating them and posing a significant food safety hazard.Fumonisin B1 is structurally a sphingosine and sphingomyelin analog, and inhibits the biosynthesis of complex sphingolipids through the inhibition of ceramidic synthases.

DL-Glyceraldehyde-3-phosphate (3-Phosphoglyceraldehyde) is an important intermediate in glycogen or starch fermentation in organisms and inhibits acyltransferases. DL-Glyceraldehyde-3-phosphate inhibits the growth of Escherichia coli at high concentrations.

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

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.

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].

DGAT2-IN-3 (compound 9) is an inhibitor of DGAT2 with an IC50 value of 0.4 nM. It is utilized in research related to fatty liver disease, diabetes, and cardiovascular diseases.

ChAT IN-1 is a selective inhibitor of Choline Acetyltransferase (ChAT) that is utilized in studying mechanisms related to non-neuronal ChAT overexpression in cancers such as colon cancer and lung cancer, as well as in research concerning Alzheimer's disease (AD).

KY-455 is a novel acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor. It demonstrates inhibition of ACAT in rabbit intestines, liver, macrophages, and adrenal glands with IC50 values of 0.4, 0.9, 2.9, and 4.1 μmol L, respectively.

Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. It also inhibits the S-palmitoylation of EGFR and CD36. In HEK293T cells expressing recombinant E. coli GobX, recombinant human MyD88, or endogenous Ras, Cyano-myracrylamide inhibits the S-palmitoylation of E. coli E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6.

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

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

Diacylglycerolacyltransferaseinhibitor-2 (Example 8) acts as an inhibitor for diacylglycerol acyltransferase 2 (DGAT2), exhibiting an IC50 value of 3.7 nM.