PIT-1
PH domain antagonist / PH domain antagonist. Specifically blocks the binding of PIP3 to the Akt pleckstrin homology domain (IC50 = 31 μM). Suppresses PI3K-PDK1-Akt-dependent phosphorylation. Induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM)1. Inhibiting the binding of PIP3 to effector PH domains is new point of intervention in the PI3K signaling network2.
Biochemicals & reagents
53501-41-0
1) Miao et al. (2010), Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains; Proc. Natl. Acad. Sci. USA, 107 20126 2) McNamara and Degterev (2011), Small-molecule inhibitors of the PI3K signaling network; Future Med. Chem., 3 549
RT
TARGET: Kinase -- PATHWAY: PI3K; Apoptosis inducer -- RESEARCH AREA: Cell death