VO-OHpic, a vanadyl complexed to hydroxypicolinic acid,is a highly specific and potent inhibitor of PTEN which increases cellular PtdIns(3,4,5)P3 levels, phosphorylation of Akt, and glucose uptake in adipocytes at nanomolar concentrations. Compared with other 7 vanadium compounds, VO-OHpic is the most potent inhibitor with IC50 of 35 nM against PTEN lipid phosphatase activity[1]. VO-OHpic impairs proliferation and induces senescence in Pten+/- MEFs cells but no activity in wild-type cells. Thus, PTEN inhibitors may represent a powerful class of molecules for pro-senescence therapy in PTEN heterozygous tumors and cells [2]. The PTEN inactivation by VO-OHpic demonstrates to be fully reversible and noncompetitive. Phosphatase substrate 3-O- methylfluorescein phosphate (OMFP) also acts as a suitable substrate for PTEN inhibition studies and PTEN drug screening [3]. Intraperitoneal injection of VO-OHpic decreases left ventricular systolic pressure and heart rate before ischemia, but causes an increase in cardiac functional recovery and a decrease in myocardial infarct size after ischemia–reperfusion [4].
Chemical Properties
Cas No.: 476310-60-8
M. Wt.: 415.20
Formula: C12H10N2O8V·3H2O
Purity:≥98%
SYNONYM: 3-hydroxypicolinate vanadium(IV) complex
Chemical Name: Hydroxy(oxo)vanadium 3-hydroxypyridine-2-carboxylic acid trihydrate
Appearance: Gray solid
Solubility: Soluble in water (≥5 mg/mL) and DMSO (10 mg/mL)
Storage: Store solid at -20 ºC for the stability of two years, keep desiccated.