VO-Ohpic trihydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VO-Ohpic 三水合物 (VO-Ohpic) 是一种有效的、选择性的、可逆的 PTEN 抑制剂，体外 IC50 为 35 nM。

VO-Ohpic trihydrate (VO-Ohpic) is a potent, selective and reversible PTEN inhibitor with IC50 of 35 nM in vitro; 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); increases cellular PIP3 levels, phosphorylation of Akt, and glucose uptake in adipocytes at nanomolar concentrations; decreases left ventricular systolic pressure and heart rate before ischemia in mice.

VO-OHpic with two OHpic ligands and an oxo ligand is a sterically demanding molecule, and one will therefore expect that binds substrate will affect the subsequent binding of the inhibitor due to steric hindrance. VO-OHpic significantly inhibits PTEN activity in low nanomolar concentrations (IC50, 46±10 nM), which is in agreement with the previously determined potency (IC50, 35±2 nM) in a PIP3-based assay. The inhibition constants Kic and Kiu are determined to be 27±6 and 45±11 nM, respectively. VO-OHpic is an encouragingly specific and potent PTEN inhibitor. VO-OHpic is the most potent inhibitor (IC50=35 nM) of the PTEN lipid phosphatase activity.

PTEN is inhibited in mice by intra-peritoneal injection of VO-OHpic (10 μg/kg) 30 min before ischemia and then exposed them to 30 min of ischemia and 120 min of reperfusion. At the end of the experiment, myocardial infarct size is measured by triphenyltetrazolium chloride (TTC). Myocardial infarct size is significantly decreased in VO-treated mice (25±6 vs. 56±5 %, n=7, P<0.01). There is no difference in the area at risk between these two groups (46±3 vs. 57±3 %, n=7, P>0.05).

VO-Ohpic | VO Ohpic

Others

PTEN

PTEN

Cancer

——

476310-60-8

415.2032

C12H16N2O11V+

>98% (HPLC)

10 mM in DMSO; H2O: < 0.1 mg/mL

O=[V](OC(C1=NC=CC=C1O)=O)(O)OC(C2=NC=CC=C2O)=O.O.O.O

Vanadate(1-), aqua(3-hydroxy-2-pyridinecarboxylato-κN1,κO2)[3-(hydroxy-κO)-2-pyridinecarboxylato(2-)-κO2]oxo-, hydrogen, trihydrate, (OC-6-45)- (9CI)

(-20℃)

With Ice Pack

≥ 2 years