LCH-7749944

Description: LCH-7749944, formerly known as GNF-Pf-2356, is a novel and highly potent PAK4 inhibitor with an IC50 of 14.93 uM. It effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway. In addition, LCH-7749944 significantly inhibited the migration and invasion of human gastric cancer cells in conjunction with concomitant blockage of PAK4/LIMK1/cofilin and PAK4/MEK-1/ERK1/2/MMP2 pathways. Interestingly, LCH-7749944 also inhibited the formation of filopodia and induced cell elongation in SGC7901 cells. Importantly, LCH-7749944 caused successful inhibition of EGFR activity due to its inhibitory effect on PAK4. Taken together, these results provided novel insights into the development of PAK4 inhibitor and potential therapeutic strategies for gastric cancer ( Cancer Lett. 2012 Apr 1; 317(1):24-32 )

References: LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppressesproliferation and invasion in human gastric cancer cells. Cancer Lett.2012 Apr 1; 317(1):24-32.