EGPI-1 is a potent small molecule that inhibits the translation initiation factors eIF4E/eIF4G interaction.
EGPI-1 has potent antiproliferative and proapoptotic activity in multiple myeloma cells, Jurkat cells, and A549 lung cancer cell lines, inhibits A549 proliferation with IC50 of 2.61 uM, which is better than that of 4EGI-1 (IC50=58.6 uM), inhibits cancer cell growth by inhibiting eIF4E phosphorylation and inhibiting PI3K/Akt/mTOR signal pathway.
EGPI-1 induces autophagy, apoptosis, G0/G1 cell cycle arrest and ROS generation in A549 cells, disrupts the mitochondrial membrane potential (∆ψ m).
EGPI-1 demonstrated in vivo anti-tumor activities in A549-xenografted athymic mice (25 mg/kg/day, 50 mg/kg/day, i.p.).
