Here we show that the derivative 2-O-benzyl-myo-inositol 1,3,4,5,6-pentakisphosphate (2-O-Bn-InsP5) exhibits more efficient and potent activity than InsP5 not only in inhibiting Akt phosphorylation but also in inducing apoptosis in different human cancer cell lines. The gene discussed is AKT1; the disease is cancer.