PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a KD value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer.
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[1].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[1].
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[1].
References:
[1]. Gu J, et, al. Construction of a synthetic methodology-based library and its application in identifying a GIT/PIX protein-protein interaction inhibitor. Nat Commun. 2022 Nov 23;13(1):7176.