LCH-7749944

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> PAK

Signaling Pathways >> Cell Cycle/DNA Damage >> PAK

PAK4:14.93 μM (IC50)

LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner[1]. LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells[1]. LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase[1]. LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner[1]. Cell Proliferation Assay[1] Cell Line: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells Concentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM Incubation Time: 24 hours Result: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner. Apoptosis Analysis[1] Cell Line: SGC7901 cells Concentration: 5, 10, 20 μM Incubation Time: 12, 24, 48 hours Result: Induced apoptosis of SGC7901 cells. Cell Cycle Analysis[1] Cell Line: SGC7901 cells Concentration: 5, 10, 20 μM Incubation Time: 12, 24, 48 hours Result: Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase. Western Blot Analysis[1] Cell Line: SGC7901 cells Concentration: 5, 10, 20, 30 μM Incubation Time: 24 hours Result: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.

[1]. Zhang J, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells. Cancer Lett. 2012 Apr 1;317(1):24-32.