VO-OHpic is a potent small-molecule compound that specifically inhibits PTEN's cellular enzymatic activity, which in turn activates downstream targets such as Akt and FoxO3a. Glucose uptake into adipocytes is dramatically enhanced upon PTEN inhibition with VO-OHpic. PTEN inhibitor accelerates wound healing in fibroblasts[1]. VO-OHpic inhibits cell viability, cell proliferation and colony formation, and induces senescence-associated β-galactosidase activity in Hep3B (low PTEN expression) and to a lesser extent in PLC/PRF/5 (high PTEN expression) cells, but not in PTEN-negative SNU475 cells[2].

VO-Ohpic significantly inhibits tumor growth in nude mice bearing xenografts of Hep3B cells[2]. VO-Ohpic administered to C57BL6 mice 30 minutes prior to Kcl-induced asystolic cardiac arrest significantly increases survival, LVPmax and dP/dt max with continued benefit. VO-OHpic also significantly increases lactate clearance and decreases plasma glucose level[3].