VO-Ohpic trihydrate (VO-Ohpic) is a potent, selective and reversible PTEN inhibitor with IC50 of 35 nM in vitro。
VO-Ohpic specifically inhibits PTEN’s cellular enzymatic activity, which in turn activates downstream targets such as Akt and FoxO3a, inhibits cell viability, cell proliferation and colony formation, and induces senescence-associated β-galactosidase activity in Hep3B cells (low PTEN expression)。
VO-Ohpic increases cellular PIP3 levels, phosphorylation of Akt, and glucose uptake in adipocytes at nanomolar concentrations。
VO-Ohpic decreases left ventricular systolic pressure and heart rate before ischemia in mice.
