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GSK1059615 is inhibitor of pan-PI3K with IC50 values of 0.4nM, 0.6nM, 5nM, 2nM and 12nM for PI3Kα, P13Kβ, P13Kγ, P13Kδ and mTOR, respectively [1].

GSK1059615 is a potent and reversible inhibitor of P13K. It also has inhibition efficacy to the oncogenic mutants of PI3Kα. The thiazolidinedione ring of GSK1059615 forms an interaction with the catalytic lysine (Lys833) within the ATP-binding pocket. In cellular assay, GSK1059615 is reported to induce G1 arrest and apoptosis in a variety of cell lines. Among these, the breast tumor cells display more sensitive. Moreover, GSK1059615 significantly suppresses tumor growth and increases plasma insulin levels in xenograft mice [1, 2].

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