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VO-Ohpic trihydrate Sale

(Synonyms: VO-OHPIC三水合物,VO-Ohpic;VO Ohpic) 目录号 : GC11007

A specific inhibitor of PTEN

VO-Ohpic trihydrate Chemical Structure

Cas No.:476310-60-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥462.00
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5mg
¥420.00
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10mg
¥644.00
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50mg
¥1,921.00
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100mg
¥3,150.00
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200mg
¥4,760.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Phosphate release assay

For the detection of PTEN and Sac1 activities, bismuth was added to the phosphate release assay in order to improve its stability and sensitivity. All enzyme preparations were tested for linearity to ensure that suitable amounts of enzyme were employed in the inhibitor assays. Enzymes were incubated with VO-Ohpic Trihydrate at various concentrations prior to starting the phosphatase reaction by adding the corresponding substrates presented in octylglucoside mixed micelles.

Cell experiment [1]:

Cell lines

NIH 3T3 and L1 fibroblasts

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0, 10, 20, 40, 75, 150 and 500 nM; 15 mins

Applications

In NIH 3T3 and L1 fibroblasts, VO-Ohpic Trihydrate dose-dependently increased Akt phosphorylation at site Ser473 and Thr308. This effect reached saturation at 75 nM.

Animal experiment [2]:

Animal models

In-vivo ischemia and reperfusion mouse model

Dosage form

10 μg/kg; i.p.

Applications

Inhibition of PTEN by VO-Ohpic Trihydrate decreased left ventricular systolic pressure and heart rate before ischemia, but resulted in an increase in cardiac functional recovery and a decrease in myocardial infarct size after ischemia-reperfusion.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Rosivatz E, Matthews J G, McDonald N Q, et al. A small-molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN). ACS chemical biology, 2006, 1(12): 780-790.

[2]. Zu L, Shen Z, Wesley J, Cai ZP. PTEN inhibitors cause a negative inotropic and chronotropic effect in mice. Eur J Pharmacol. 2011 Jan 10;650(1):298-302.

产品描述

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].
References:
[1] Rosivatz E, Matthews J G, McDonald N Q, et al. A small-molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN). ACS chemical biology, 2006, 1(12): 780-790.
[2] Alimonti A, Nardella C, Chen Z, et al. A novel type of cellular senescence that can be enhanced in mouse models and human tumor xenografts to suppress prostate tumorigenesis. The Journal of clinical investigation, 2010, 120(3): 681.

Chemical Properties

Cas No. 476310-60-8 SDF
别名 VO-OHPIC三水合物,VO-Ohpic;VO Ohpic
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 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4143 mL 12.0715 mL 24.1429 mL
5 mM 0.4829 mL 2.4143 mL 4.8286 mL
10 mM 0.2414 mL 1.2071 mL 2.4143 mL
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