The vanadium complex VO-OHpic is a potent reversible allosteric inhibitor of phosphatase and tensin homologue deleted on chromosome 10 (PTEN) which hydrolyzes the 3-phosphate from phosphatidylinositol 3 4 5-trisphosphate (PIP3). PIP3 formed from PI(4 5)P2 though phosphorylation by PI 3-kinase activates numerous signaling pathways resulting in cell proliferation growth survival glucose transport and protein synthesis. VO-OHpic is reported to be selective for PTEN (IC50~35 nM) compared with other cysteine-based phosphatases (PTPβ SAC MTM & SopB IC50>4 μM). Treatment of insulin-stimulated NIH 3T3 and L1 fibroblasts caused an increase in Akt-phosphorylation indicating inhibition of PTEN in vivo.Publications Powered by Bioz See more details on Bioz