Acyltransferase 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.

Ilekudinol B is an inhibitor of ACAT and PTP1B, with an IC₅₀ of 5.3 μM and a K_i 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.

ACAT-IN-3 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-3 inhibits NF-κB mediated transcription.

TA-7552 is a potent cholesterol-lowering agent.

BW813U is a blood-brain barrier-permeable choline acetyltransferase (ChAT) inhibitor. BW813U reduces acetylcholine secretion, decreases cancer cell viability, and slows tumor growth rate. BW813U alters reference memory and causes working memory dysfunction. BW813U shows a synergistic effect with age factors in memory deficits of rats. BW813U can be used in studies related to Alzheimer's disease and lung cancer.

IONIS-DGAT 2Rx sodium scrambled negative control is the sequence scrambled negative control of IONIS-DGAT 2Rx sodium.

JTT-553 is a DGAT1 inhibitor (IC₅₀: 2.38 nM). JTT-553 reduces plasma concentrations of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and hepatic triglycerides (TG). JTT-553 improves insulin-dependent glucose uptake and glucose intolerance in adipose tissue of DIO mice. JTT-553 reduces TNF-α mRNA levels and increases GLUT4 mRNA levels in adipose tissue of KK-Ay mice. JTT-553 improves adipose tissue insulin resistance and systemic glucose metabolism by reducing body weight. JTT-553 can be used in the study of obesity and type 2 diabetes mellitus (T2DM).

Lateritin is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), isolated from the mycelial cake of Gibberella lateritium IFO 7188. Lateritin also inhibits the growth of a mini-panel of human cancer cell lines, gram-positive bacteria, and Candida albicans.

IONIS-DGAT 2Rx (ION-224) is a DGAT2 inhibitor, which is promising for research of atherosclerosis.

Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.

Aphadilactone C is a potent and selective DGAT-1 inhibitor with an IC₅₀ of 0.46 μM. Aphadilactone C shows significant antimalarial activities with an IC₅₀ value of 170 nM.

Quinine (sulfate hydrate) (Standard) is the analytical standard of Quinine (sulfate hydrate). This product is intended for research and analytical applications. Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM.

ACAT-IN-5 (example 19) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-5 inhibits NF-κB mediated transcription.

Ent-Calquiquelignan E (Compound 8) is a flavonoid lignan compound. Ent-Calquiquelignan E can selectively inhibit diacylglycerol acyltransferase 1 (DGAT1) with an IC₅₀ of 71.5 μM. Ent-Calquiquelignan E can be used for the research of metabolic diseas.

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.

NTE-122 (dihydrochloride) is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with the IC₅₀ in liver and aorta of cholesterol-fed rabbits of 7.6nM, 4.4nM and 9.6 nM, respectively, that plays an important role in atherosclerosis.

PD 128042 (Standard) is the analytical standard of PD 128042. This product is intended for research and analytical applications. PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway.

Nevanimibe hydrochloride (Standard) is the analytical standard of Nevanimibe hydrochloride. This product is intended for research and analytical applications. Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.

RHC 80267 (Standard) is the analytical standard of RHC 80267 (HY-107416). This product is intended for research and analytical applications. RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC₅₀ of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC₅₀ of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).

DGAT-1 inhibitor 2 (Standard) is the analytical standard of DGAT-1 inhibitor 2 (HY-50670). This product is intended for research and analytical applications. DGAT-1 inhibitor 2 is an orally active DGAT-1 inhibitor with IC₅₀ values of 15 nM and 9 nM for human DGAT-1 and rat DGAT-1, respectively. DGAT-1 inhibitor 2 increases ROS concentration, GRP78, and PERK protein abundance. DGAT-1 inhibitor 2 increases SREBF1, CPT1A, and MTTP mRNA in fatty acid-treated cells. DGAT-1 inhibitor 2 improves obesity.