In Vitro: PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 0-50 μM) inhibits the interaction between GIT1 and β-Pix in living cells. PPI-GIT1/β-Pix interaction-IN-1 (0-50 μM; 24 h; MGC803 cells and MKN45 cells) inhibits gastric cancer cell invasion in a dose-dependent manner and disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42.
In Vivo: PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 10 and 30 mg/kg; i.g.; 24 h) inhibits gastric cancer cell invasion in female nude mice with MGC803 xenografts.