化合物VO-Ohpic trihydrate T7012

Product Introduction
Bioactivity


英文名: VO-Ohpic trihydrate

描述: VO-Ohpic trihydrate (VO-Ohpic) 是一种有效的磷酸酶和张力蛋白同源物（PTEN）抑制剂，IC50 为 35 nM。

细胞实验: Cell proliferation is determined by estimating the amount of bromodeoxyuridine (BrdU) incorporation into DNA by a colorimetric immunoassay. 3×103 cells are cultured in 96-well plates with varying concentrations of VO-OHpic for 72 hours. BrdU is added 24 hours before the end of the treatments. Results are expressed as the percentage inhibition of BrdU incorporation over the control.(Only for Reference)

激酶实验: VO-OHpic is dissolved in DMSO (100 μM) 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 to initialise the reaction. Background absorbance (malachite green assay) and fluorescence (OMFP assay) are determined with VO-OHpic in assay buffer and corrected in the data analysis[1].

体外活性: VO-OHpic is a potent small-molecule compound that specifically inhibits PTEN's cellular enzymatic activity, which in turn activates downstream targets such as Akt and FoxO3a. Glucose uptake into adipocytes is dramatically enhanced upon PTEN inhibition with VO-OHpic. PTEN inhibitor accelerates wound healing in fibroblasts[1]. VO-OHpic inhibits cell viability, cell proliferation and colony formation, and induces senescence-associated β-galactosidase activity in Hep3B (low PTEN expression) and to a lesser extent in PLC/PRF/5 (high PTEN expression) cells, but not in PTEN-negative SNU475 cells[2].

体内活性: VO-Ohpic significantly inhibits tumor growth in nude mice bearing xenografts of Hep3B cells[2]. VO-Ohpic administered to C57BL6 mice 30 minutes prior to Kcl-induced asystolic cardiac arrest significantly increases survival, LVPmax and dP/dt max with continued benefit. VO-OHpic also significantly increases lactate clearance and decreases plasma glucose level[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 67 mg/mL (161.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Autophagy | Inhibitor | VOOhpic trihydrate | VO Ohpic trihydrate | PTEN | inhibit | VO-Ohpic Trihydrate | Phosphatase and tensin homolog | MMAC1

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相关库: Antioxidant Compound Library | Anti-Liver Cancer Compound Library | Oxidation-Reduction Compound Library | Neuronal Differentiation Compound Library | Anti-Lung Cancer Compound Library | Phosphatase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library

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