GSK-690693

Description: GSK690693, an aminofurazan derivative, is a novel, potent and ATP-competitive pan-Akt inhibitor targeting Akt1/2/3 with potential anticancer activity. It inhibits Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays. The antiproliferative effects of GSK690693 was selective for the cancer cells, asit did not inhibit the proliferation of normal human CD4(+)peripheral T lymphocytes as well as mouse thymocytes. Phosphorylation ofdownstream substrates of AKT was reduced in both sensitive andinsensitive cell lines on treatment with GSK690693, suggesting that thecause of resistance was not related to the lack of AKT kinaseinhibition.

References: Expert Opin Investig Drugs. 2010 Nov; 19(11):1355-66.