Home PI3K/Akt/mTOR PTEN inhibitor VO-Ohpic trihydrate

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VO-Ohpic trihydrate PTEN inhibitor

Cat.No.S8174

VO-Ohpic is a potent inhibitor of PTEN (phosphatase and tensin homolog) with IC50 of 35 nM.
VO-Ohpic trihydrate PTEN inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 415.20

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 415.20 Formula

C12H9N2O8V.3H2O.H

 Storage (From the date of receipt)
CAS No. 476310-60-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles [H+].C1=CC(=C(N=C1)C(=O)[O-])O.C1=CC(=C(N=C1)C(=O)[O-])[O-].O.O[V]=O

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (173.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
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Mechanism of Action

Targets/IC50/Ki
PTEN [1]
(Cell-free assay)
35 nM
In vitro
VO-OHpic is a potent small-molecule compound that specifically inhibits PTEN’s cellular enzymatic activity, which in turn activates downstream targets such as Akt and FoxO3a. Glucose uptake into adipocytes is dramatically enhanced upon PTEN inhibition with VO-OHpic. PTEN inhibitor accelerates wound healing in fibroblasts[1]. VO-OHpic inhibits cell viability, cell proliferation and colony formation, and induces senescence-associated β-galactosidase activity in Hep3B (low PTEN expression) and to a lesser extent in PLC/PRF/5 (high PTEN expression) cells, but not in PTEN-negative SNU475 cells[2].
In vivo
VO-Ohpic significantly inhibits tumor growth in nude mice bearing xenografts of Hep3B cells[2]. VO-Ohpic administered to C57BL6 mice 30 minutes prior to Kcl-induced asystolic cardiac arrest significantly increases survival, LVPmax and dP/dt max with continued benefit. VO-OHpic also significantly increases lactate clearance and decreases plasma glucose level[3].
References

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