VO-OHpic, featuring two OHpic ligands and an oxo ligand, is a molecule with substantial steric bulk, suggesting that substrate binding may influence inhibitor binding due to steric hindrance. It markedly inhibits PTEN activity at low nanomolar concentrations (IC50, 46±10 nM), aligning with its previously established potency (IC50, 35±2 nM) in a PIP3-based assay. The inhibition constants Kic and Kiu have been calculated to be 27±6 and 45±11 nM, respectively[1]. VO-OHpic stands out as a notably specific and potent inhibitor of PTEN. It is identified as the most effective inhibitor of PTEN lipid phosphatase activity, with an IC50 value of 35 nM[2].
体内研究
PTEN activity is suppressed in mice through intraperitoneal injection of VO-OHpic (10 μg/kg) administered 30 minutes prior to ischemia, followed by 30 minutes of ischemia and 120 minutes of reperfusion. Myocardial infarct size is significantly reduced in VO-OHpic treated mice, as determined by triphenyltetrazolium chloride (TTC) staining (25±6 vs. 56±5 %, n=7, P<0.01). The area at risk remains comparable between the two groups (46±3 vs. 57±3 %, n=7, P>0.05)[3].
体外研究
VO-OHpic, featuring two OHpic ligands and an oxo ligand, is a molecule with substantial steric bulk, suggesting that substrate binding may influence inhibitor binding due to steric hindrance. It markedly inhibits PTEN activity at low nanomolar concentrations (IC50, 46±10 nM), aligning with its previously established potency (IC50, 35±2 nM) in a PIP3-based assay. The inhibition constants Kic and Kiu have been calculated to be 27±6 and 45±11 nM, respectively[1].
VO-OHpic stands out as a notably specific and potent inhibitor of PTEN. It is identified as the most effective inhibitor of PTEN lipid phosphatase activity, with an IC50 value of 35 nM[2].
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