VO-Ohpic-trihydrate-VO-Ohpic-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVO-Ohpic trihydrateCat. No.: HY-13074CAS No.: 476310-60-8Synonyms: VO-Ohpic分式: CHNOV分量: 415.2作靶点: PTEN作通路: PI3K/Akt/mTOR储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (120.42 mM)H

2、2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.02 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.02 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.02 mM); Pr

3、ecipitated solution; Need warmingBIOLOGICAL ACTIVITY物活性 VO-Ohpic trihydrate种效的 PTEN 抑制剂，IC50 为 4610 nM。IC50 & Target IC50: 4610 nM (PTEN) 1体外研究 VO-OHpic with two OHpic ligands and an oxo ligand is a sterically demanding molecule, and one willtherefore expect that binds substrate will affect the subs

4、equent binding of the inhibitor due to sterichindrance. VO-OHpic significantly inhibits PTEN activity in low nanomolar concentrations (IC50, 4610 nM),which is in agreement with the previously determined potency (IC50, 352 nM) in a PIP3-based assay. Theinhibition constants Kic and Kiu are determined

5、to be 276 and 4511 nM, respectively 1. VO-OHpic is anencouragingly specific and potent PTEN inhibitor. VO-OHpic is the most potent inhibitor (IC50=35 nM) of thePTEN lipid phosphatase activity 2.体内研究 PTEN is inhibited in mice by intra-peritoneal injection of VO-OHpic (10 g/kg) 30 min before ischemia

6、andthen 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 issignificantly decreased in VO-treated mice (256 vs. 565 %, n=7, P0.05) 3.PROTOCOLKinase Assay 1 VO

7、-OHpic is dissolved in DMSO (100 M) and diluted further to the required concentration with 1% DMSO.For inhibition studies, PTEN is preincubated with VO-OHpic at RT for 10 min before substrate is added toinitialise the reaction. Background absorbance (malachite green assay) and fluorescence (OMFP ass

8、ay) aredetermined with VO-OHpic in assay buffer and corrected in the data analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 The experiment is performed with male C57BL6 mice. Briefly, mice are anesthetized with pen

9、tobarbital (70mg/kg). The left coronary artery is occluded about 1-2 mm below the left auricle. Reperfusion isaccomplished by loosening the ligature. The PTEN inhibitor VO-OHpic is administered by intra-peritonealinjection at the dosage of 10 g/kg once 30 min before ischemia. Saline is used as contr

10、ol. At the end of theexperiment, the animals are euthanized by transecting the aorta and removing the heart for infarct sizedetermination.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Cancer

11、 Cell. 2019 Apr 15;35(4):677-691 Bone Res. 2018 Nov 10;6:32. Theranostics. 2019 Jul 9;9(16):4764-4778. Theranostics. 2019 Jul 9;9(18):5200-5213. Redox Biol. 2019 Jan;20:390-401.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Mak LH, et al. Characterisation of the PTEN inhibitor

12、 VO-OHpic. J Chem Biol. 2010 Oct;3(4):157-63.2. Rosivatz, E, et al. A small molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN). ACS ChemBiol. 2006 Dec 15;1(12):780-90.3. Zu L, et al. PTEN inhibitors cause a negative inotropic and chronotropic effect in mice. Eur J Pharmacol. 2011 Jan 10;650(1):298-302.McePdfHeightCaution: