1. PI3K/Akt/mTOR Autophagy
  2. PTEN Autophagy
  3. VO-Ohpic trihydrate

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

VO-Ohpic trihydrate Chemical Structure

CAS No. : 476310-60-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 32 publication(s) in Google Scholar

Other Forms of VO-Ohpic trihydrate:

Top Publications Citing Use of Products
WB

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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 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].

    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.
    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
    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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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)

    g

    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
    References
    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

    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.

    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
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    VO-Ohpic trihydrate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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