GSK2194069

GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC₅₀ value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC₅₀ or K_i values of 4.8 nM and 5.6 nM, respectively^[1][2][3]. In Vitro: GSK2194069 (100 nM; 24 h) inhibits fatty acid synthase (FAS) in cancer cell lines (KATO-III, MKN45, A549, SNU-1) without reducing FAS production protein level^[1].
GSK2194069 decreases phosphatidylcholine levels in A549 cells with a half-maximum effective concentration (EC50) value of 15.5 ± 9 nM (n = 78), correlating with the decreased palmitate synthesis^[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].