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PtdIns-(3,4,5)-P₃ (PIP₃) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP₃ is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. PIT-1 is a selective nonphosphoinositide inhibitor that specifically disrupts PIP₃/Akt PH domain binding with an IC₅₀ value of 31 μM. PIT-1 suppresses PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC₅₀ = 37 μM).

PIT 1 is an apoptosis inducing selective PIP3 antagonist.

1) Maio?et al.?(2010),?Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PI3) binding to pleckstrin homology domains; Proc. Natl. Acad. Sci. USA,?107?20126 2) McNamare and Degterev?(2011),?Small-molecule inhibitor of the PI3K signaling network; Future Med. Chem.,?3?549