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Field of application
ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD).
Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor (DGAT2i). Ervogastat alone reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Ervogastat combination with Clesacostat (an acetyl CoA-carboxylase inhibitor (ACCi)) can be used for the research of NASH with liver fibrosis therapy.
YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.
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).
Yakuchinone B is an Acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitor with hypocholesterolemic activity, which is found in the seeds of Zingiberaceae. Yakuchinone B inhibits rat hepatic ACAT with an IC50 value of 20.6 μM. Yakuchinone B is promising for research of hypercholesterolemia and atherosclerosis.
Epicochlioquinone A can inhibit rat liver microsomal ACAT with IC50 of 1.7 μM, inhibit plasma lecithin cholesterol acyltransferase (LCAT) with IC50 of 15.8 μM, and inhibit cholesterol absorption in rats by 50% at 75 mg/kg.
Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras.
ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD).
ALT-007 is an orally effective serine palmitoyltransferase (SPT) inhibitor. SPT is the rate-limiting enzyme for the de novo synthesis of ceramide. In a mouse model of age-related sarcopenia, ALT-007 can effectively restore the muscle mass and function impaired by aging. ALT-007 may enhance protein homeostasis in Caenorhabditis elegans and mouse models of aging and age-related diseases and play the role of a ceramide inhibitor.