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. Synonyms: N-(4-Hydroxybiphenyl-3-ylcarbamothioyl)-3,5-dimethylbenzamide, Phosphatidylinositol-3,4,5-triphosphate Antagonist, PITenin-7, PIT-7, Akt Inhibitor XX, PDK1 Inhibitor V Molecular Formula: C22H20N2O2S Molecular Weight: 376.5 Appearance: Yellow-white semi-solid Solubility: DMSO (100mg/ml) Method for Determining Identity: Proton NMR Spectroscopic and Mass Spectrometric analysis Storage and Stability: Lyophilized and reconstituted products are stable for 6 months after receipt at 4C. Reconstitute with DMSO. Store at 4C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molecular Weight:
376.5
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