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Description

A cell-permeable DM-PIT-1 (Cat. No. 524619) analog that is more selective and potent than DM-PIT-1 against PH domain-mediated PIP3 (Cat. No. 524615) binding to Akt1 (IC50 = 13.4 and 27.1 µ,M, respectively) and PDK1 (IC50 = 52.3 and 80.5 µ,M, respectively), while being much less active than DM-PIT-1 against PIP3 GRP1 PH domain binding (12% vs 84% inhibition with 100 µ,M respective compound). PIT-7 is also shown to be more effective than DM-PIT-1 in inhibiting human glioblastoma U87MG survival (IC50 = 6.6 vs. 33.9 µ,M, respectively) and cellular Akt Ser473 phosphorylation in cultures in vitro.