产品描述:
GSK2194069 is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 7.7 nM in an assay detecting released CoA.{35126} It is a competitive inhibitor that is selective for the KR domain over the KS domain of FASN, with IC50 values of 29 and >10,000 nM, respectively, in vitro. GSK2194069 decreases incorporation of 13C-labeled acetate into cellular lipids in a dose-dependent manner in KATO-III, MKN-45, and SNU-1 gastric, and A549 non-small cell lung cancer cell lines. It also reduces cell growth of A549 cells (EC50 = 15 nM) and inhibits lipid synthesis without decreasing FASN protein expression.