VO-Ohpic trihydrate |
| رقم الكتالوجGC11007 |
A specific inhibitor of PTEN
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 476310-60-8
Sample solution is provided at 25 µL, 10mM.
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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.
| Kinase experiment [1]: | |
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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]: | |
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Cell lines |
NIH 3T3 and L1 fibroblasts |
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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]: | |
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Animal models |
In-vivo ischemia and reperfusion mouse model |
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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. |
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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. |
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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. | |
| Cas No. | 476310-60-8 | SDF | |
| Formula | C12H15N2O11V+ | M.Wt | 414.2 |
| الذوبان | ≥ 121.8 mg/mL in DMSO, ≥ 45.8 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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