GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.

Phosphatidylcholine:15.5 ± 9 nM(EC50), β-ketoyl reductase:7.7 nM

GSK2194069 (100 nM; 24 h) suppresses fatty acid synthase (FAS) activity in cancer cell lines (KATO-III, MKN45, A549, SNU-1) while maintaining FAS protein production levels.[1]
GSK2194069 (5 μM and 20 μM) shows higher efficacy in FASN-positive LNCaP cells rather than FASN-negative PC3 cells, with the higher FASN Expression level in LNCaP cells.[2]
GSK2194069 (50 μM; 24 h) inhibits the growth of LNCaP-LN3 human prostate cancer cells.[3]
GSK2194069 (60.4 nM; 24 h) displays properties of metabolomics, including L-acetyl carnitine, stearoyl carnitine, vaccenyl carnitine, and palmitoyl-L-carnitine decrease in LNCaP-LN3 cells.[3]