產(chǎn)品目錄

規(guī)格	10mg 25mg 500mg 1g
CAS	476310-60-8 N/A
別名	VO-Ohpic;VO Ohpic
化學(xué)名	N/A
分子式	C12H15N2O11V+
分子量	414.2
溶解度	≥ 121.8 mg/mL in DMSO, ≥ 45.8 mg/mL in EtOH with ultrasonic
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

VO-Ohpic is a highly selective small-molecule inhibitor of phosphatase and tensin homologue deleted on chromosome 10 (PTEN) with IC50 value of 35 nM [1].

Many research studies show that the lipid phosphatase activity of PTEN has certain cellular impacts, such as inhibition of proliferation, survival and regulation of insulin signaling. Meanwhile, the inhibition of PTEN's lipid phosphatase activity increases glucose uptake triggered by the increase of PtdIns (3, 4, 5) P3. These suggest that small-molecule inhibitor of PTEN may have the potential of enhancing insulin sensitivity and overcoming insulin resistance, which would be beneficial for the development of diabetes therapeutics. VO-Ohpic is a specific vanadium-based inhibitor screened out from a range of synthesized vanadates and bpV complexes. [1]

In vitro, VO-Ohpic inhibited the lipid phosphatase activity of recombinant PTEN with IC50 value of 35 nM. It was highly selective against PTEN over other recombinant phosphatases including CBPs, SopB, myotubularin, SAC1 and PTP-β. It inhibited CBPs and SopB with IC50 values in micromolar range and high nanomolar range, respectively. In NIH 3T3 and L1 fibroblasts, VO-Ohpic dose-dependently increased Akt phosphorylation at site Ser473 and Thr308. This effect reached saturation at 75 nM. VO-OHpic had no effect on insulin-stimulated tyrosine phosphorylation at concentrations up to 10 μM. Besides that, VO-Ohpic treatment was found to cause the functional activation of Akt, demonstrated by a corresponding reduction of the transcriptional activity of FoxO3a [1].

In mice bearing MDA PCa-2b cell xenografts, administration of VO-Ohpic showed significant tumor growth suppression. Moreover, long term treatment of VO-Ohpic resulted in an increased survival of the treated animals. The tumors treated with VO-Ohpic displayed increased β-gal staining and decreased Ki-67 staining compared with the untreated control tumors [2].

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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