A cell-permeable benzoylthiourea compound that acts as a PIP3(phosphatidylinositol-3,4,5-triphosphate) mimic and inhibits PI 3-K/PIP3/Akt signaling. Shown to efficiently disrupt PIP3/Akt1 PH (pleckstrin-homology) domain interaction over PIP3/PDK1 PH (IC50=13.4 and 52.3uM) in a reversible manner, and remain inactive toward PIP3/Btk, PIP3/ARNO, PIP3/GRP1 and PIP2/PLC-d/TAPP1/TAPP2 PH domains. Blocks phosphorylation of Akt-Ser473 and -Thr308 and its downstream targets, GSK-3B-Ser9 and S6-Ser235/236 and induces metabolic stress and cell death (IC50=6.6uM) in PTEN-deficient U87MG cells. Further, synergizes with Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 and Akt Inhibitor X.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
