VO-Ohpic trihydrate

Name: VO-Ohpic trihydrate
Brand: MedChemExpress
SKU: HY-13074
Rating: 5.0 (35 reviews)

Cat. No.: HY-13074 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

VO-Ohpic trihydrate Chemical Structure

CAS No. : 476310-60-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 26	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 319	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 462	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 682	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 35 publication(s) in Google Scholar

Other Forms of VO-Ohpic trihydrate:

VO-OHPic Get quote

30 Publications Citing Use of MCE VO-Ohpic trihydrate

: VO-Ohpic trihydrate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2019 Jan;20:390-401. [Abstract]; Immunoblotting analysis show that RES treatment markedly inhibited Ang II-induced degradation of PTEN, activation of AKT and mTOR and inactivation of AMPK, but this effect is reversed by VO-OHpic.

: VO-Ohpic trihydrate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2019 Jan;20:390-401. [Abstract]; Western analysis of related genes expression in mice with the treatment of TAC, TAC+RES, and TAC+RES+VO-Ophic.

: VO-Ohpic trihydrate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2019 Jan;20:390-401. [Abstract]; Immunoblotting analysis show that RES treatment markedly inhibited Ang II-induced degradation of PTEN, activation of AKT and mTOR and inactivation of AMPK, but this effect is reversed by VO-OHpic.

: VO-Ohpic trihydrate purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2019 Jul 29;10(1):217. [Abstract]; Western blot showing the levels of phosphorylated and non-phosphorylated PTEN, AKT, and mTOR proteins before and after VO-OHpic trihydrate treatment.

: VO-Ohpic trihydrate purchased from MedChemExpress. Usage Cited in: Mol Vis. 2018 Jul 23;24:485-494. [Abstract]; The miR-21 inhibitor promotes the expression of the PTEN protein and inhibits the expression of p-AKT, and VO-Ohpic trihydrate reverses the effect.

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Biological Activity
Protocol
Purity & Documentation
References
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Description

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

IC₅₀ & Target

IC50: 46±10 nM (PTEN)^[1]

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 K_ic and K_iu 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

415.20

Formula

C₁₂H₁₆N₂O₁₁V

CAS No.

476310-60-8

Appearance

Solid

Color

Light green to green

SMILES

O[V+2]([N]1=CC=CC(O)=C1C2=O)([O-]2)([O-]C3=CC=CN=C3C4=O)([O-]4)=O.[H+].[3H2O]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (120.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4085 mL	12.0424 mL	24.0848 mL
5 mM	0.4817 mL	2.4085 mL	4.8170 mL
10 mM	0.2408 mL	1.2042 mL	2.4085 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (287 KB) SDS (252 KB)

COA (261 KB) Elemental Analysis Report (119 KB)

Handling Instructions (2659 KB)

References

[1]. Mak LH, et al. Characterisation of the PTEN inhibitor VO-OHpic. J Chem Biol. 2010 Oct;3(4):157-63. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Mak LH, et al. Characterisation of the PTEN inhibitor VO-OHpic. J Chem Biol. 2010 Oct;3(4):157-63. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4085 mL	12.0424 mL	24.0848 mL	60.2119 mL
	5 mM	0.4817 mL	2.4085 mL	4.8170 mL	12.0424 mL
	10 mM	0.2408 mL	1.2042 mL	2.4085 mL	6.0212 mL
	15 mM	0.1606 mL	0.8028 mL	1.6057 mL	4.0141 mL
	20 mM	0.1204 mL	0.6021 mL	1.2042 mL	3.0106 mL
	25 mM	0.0963 mL	0.4817 mL	0.9634 mL	2.4085 mL
	30 mM	0.0803 mL	0.4014 mL	0.8028 mL	2.0071 mL
	40 mM	0.0602 mL	0.3011 mL	0.6021 mL	1.5053 mL
	50 mM	0.0482 mL	0.2408 mL	0.4817 mL	1.2042 mL
	60 mM	0.0401 mL	0.2007 mL	0.4014 mL	1.0035 mL
	80 mM	0.0301 mL	0.1505 mL	0.3011 mL	0.7526 mL
	100 mM	0.0241 mL	0.1204 mL	0.2408 mL	0.6021 mL