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

VO-Ohpic trihydrate 

Cat. No.: HY-13074 Purity: >98.0%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 290 In-stock
Estimated Time of Arrival: December 31
100 mg USD 420 In-stock
Estimated Time of Arrival: December 31
200 mg USD 620 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Mol Vis. 2018 Jul 23;24:485-494.

    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.

    VO-Ohpic trihydrate purchased from MCE. Usage Cited in: Redox Biol. 2019 Jan;20:390-401.

    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 MCE. Usage Cited in: Redox Biol. 2019 Jan;20:390-401.

    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 MCE. Usage Cited in: Redox Biol. 2019 Jan;20:390-401.

    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 MCE. Usage Cited in: Stem Cell Res Ther. 2019 Jul 29;10(1):217. 

    Western blot showing the levels of phosphorylated and non-phosphorylated PTEN, AKT, and mTOR proteins before and after VO-OHpic trihydrate treatment.
    • 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].

    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].

    Molecular Weight

    415.20

    Formula

    C₁₂H₁₆N₂O₁₁V

    CAS No.

    476310-60-8

    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)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: 2.5 mg/mL (6.02 mM); Precipitated solution; Need warming

    *All of the co-solvents are provided by MCE.
    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
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    KeyWords:

    VO-Ohpic | PTEN | Autophagy | Phosphatase and tensin homolog | MMAC1 | Inhibitor | inhibitor | inhibit

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    Product name:
    VO-Ohpic trihydrate
    Cat. No.:
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