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VO-Ohpic trihydrate

PTEN inhibitor CAS# 476310-60-8

VO-Ohpic trihydrate

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Chemical structure

VO-Ohpic trihydrate

3D structure

Chemical Properties of VO-Ohpic trihydrate

Cas No. 476310-60-8 SDF Download SDF
PubChem ID 91866958 Appearance Powder
Formula C12H15N2O11V+ M.Wt 414.2
Type of Compound N/A Storage Desiccate at -20°C
Synonyms VO-Ohpic
Solubility DMSO : ≥ 50 mg/mL (120.42 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name hydrido-hydroxy-oxovanadium;hydron;3-hydroxypyridine-2-carboxylic acid;trihydrate
SMILES [H+].C1=CC(=C(N=C1)C(=O)O)O.C1=CC(=C(N=C1)C(=O)O)O.O.O.O.O[VH]=O
Standard InChIKey QCNGUXCDZCQXOY-UHFFFAOYSA-N
Standard InChI InChI=1S/2C6H5NO3.4H2O.O.V.H/c2*8-4-2-1-3-7-5(4)6(9)10;;;;;;;/h2*1-3,8H,(H,9,10);4*1H2;;;/q;;;;;;;+1;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of VO-Ohpic trihydrate

DescriptionVO-Ohpic trihydrate is an extremely potent inhibitor of PTEN with IC50 of 46±10 nM.In Vitro:VO-OHpic with two OHpic ligands and an oxo ligand is a sterically demanding molecule, and one will therefore expect that binds substrate will affect the subsequent binding of the inhibitor due to steric hindrance. VO-OHpic significantly inhibits PTEN activity in low nanomolar concentrations (IC50, 46±10 nM), which is in agreement with the previously determined potency (IC50, 35±2 nM) in a PIP3-based assay. The inhibition constants Kic and Kiu are determined to be 27±6 and 45±11 nM, respectively[1]. VO-OHpic is an encouragingly specific and potent PTEN inhibitor. VO-OHpic is the most potent inhibitor (IC50=35 nM) of the PTEN lipid phosphatase activity[2].In Vivo:PTEN is inhibited in mice by intra-peritoneal injection of VO-OHpic (10 μg/kg) 30 min before ischemia and then 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 is significantly decreased in VO-treated mice (25±6 vs. 56±5 %, n=7, P<0.01). There is no difference in the area at risk between these two groups (46±3 vs. 57±3 %, n=7, P>0.05)[3].

References:
[1]. Mak LH, et al. Characterisation of the PTEN inhibitor 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 Chem Biol. 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.

Protocol

Kinase Assay [1]
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].

Animal Administration [3]
Mice[3] The experiment is performed with male C57BL6 mice. Briefly, mice are anesthetized with pentobarbital (70 mg/kg). The left coronary artery is occluded about 1-2 mm below the left auricle. Reperfusion is accomplished by loosening the ligature. The PTEN inhibitor VO-OHpic is administered by intra-peritoneal injection at the dosage of 10 μg/kg once 30 min before ischemia. Saline is used as control. At the end of the experiment, the animals are euthanized by transecting the aorta and removing the heart for infarct size determination.

References:
[1]. Mak LH, et al. Characterisation of the PTEN inhibitor 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 Chem Biol. 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.

VO-Ohpic trihydrate Dilution Calculator

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VO-Ohpic trihydrate Molarity Calculator

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Preparing Stock Solutions of VO-Ohpic trihydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4143 mL 12.0715 mL 24.1429 mL 48.2859 mL 60.3573 mL
5 mM 0.4829 mL 2.4143 mL 4.8286 mL 9.6572 mL 12.0715 mL
10 mM 0.2414 mL 1.2071 mL 2.4143 mL 4.8286 mL 6.0357 mL
50 mM 0.0483 mL 0.2414 mL 0.4829 mL 0.9657 mL 1.2071 mL
100 mM 0.0241 mL 0.1207 mL 0.2414 mL 0.4829 mL 0.6036 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on VO-Ohpic trihydrate

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.

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References on VO-Ohpic trihydrate

MiR-21 promotes pterygium cell proliferation through the PTEN/AKT pathway.[Pubmed:30967746]

Mol Vis. 2018 Jul 23;24:485-494. eCollection 2018.

Purpose: To evaluate the effect of the overexpression of miR-21 on the properties of pterygium and examine whether miR-21 promotes the proliferation of pterygium cells through targeting the PTEN/AKT signaling pathway. Methods: Information regarding patient gender, age, and pterygium severity was gathered. Expression of miR-21 was obtained through examination of excised pterygium tissues and superior conjunctiva tissues with real-time PCR. Human pterygium fibroblasts (HPFs) were obtained from pterygium surgery and subjected to primary culture. The HPF cell lines were divided into a negative control group, an miR-21 inhibitor group, and an miR-21 inhibitor + VO-Ohpic trihydrate group, and then the cell viability and apoptosis and the expression of PTEN and AKT were examined. Results: Fifty-eight subjects with unilateral primary pterygium were included. An increase in the miR-21 levels in pterygium tissue was evident compared with that in the paired normal conjunctival tissues (independent-samples t test, p<0.01). As the severity of the pterygium increased, the miR-21 levels increased (p=0.004, rs=0.373, Spearman's rank correlation coefficient). The miR-21 inhibitor suppressed the proliferation and induced apoptosis of HPF cells through increasing the PTEN expression, and further decreasing the expression of p-AKT, which could be reversed by the PTEN inhibitor VO-Ohpic trihydrate. Conclusions: Aberrant miR-21 overexpression in the pterygium could target PTEN, which contributes to abnormal proliferation of the HPF cells through depressing the PTEN/AKT pathway. The results also suggested the potential of miR-21 and the PTEN/AKT pathway as a novel therapeutic strategy for pterygium.

Description

VO-Ohpic trihydrate is a highly potent inhibitor of PTEN with an IC50 of 46±10 nM.

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