[CAS NO. 476310-60-8] VO-Ohpictrihydrate
PRODUCTS SPECIFICATIONS [476310-60-8]
DESCRIPTION [476310-60-8]
Overview
| MDL | MFCD11045907 |
|---|---|
| Molecular Weight | 415.20 |
| Molecular Formula | C12H16N2O11V |
| SMILES | O[V+2]([N]1=CC=CC(O)=C1C2=O)([O-]2)([O-]C3=CC=CN=C3C4=O)([O-]4)=O.[H+].[3H2O] |
24 Publications Citing Use of MCE
- [1]Cell Stem Cell. 2022 Apr 7;29(4):545-558.e13.
- [2]Bone Res. 2018 Nov 10;6:32.
- [3]Redox Biol. 2019 Jan;20:390-401.
- [4]Theranostics. 2019 Jul 9;9(16):4764-4778.
- [5]Theranostics. 2019 Jul 9;9(18):5200-5213.
- [6]Clin Transl Med. 2022 Sep;12(9):e1061.
- [7]Clin Transl Med. 2020 Dec;10(8):e240.
- [8]Environ Sci Technol. 2020 Sep 1;54(17):10783-10796.
- [9]Cell Death Dis. 2019 May; 10(5): 329.
- [10]Mol Nutr Food Res. 2019 Dec;63(24):e1900418.
- [11]Transl Psychiatry. 2021 Mar 26;11(1):185.
- [12]Stem Cell Res Ther. 2019 Jul 29;10(1):217.
- [13]Biochem Pharmacol. 2020 Jan;171:113715.
- [14]Biochem Pharmacol. 2019 Oct;168:82-90.
- [15]J Cell Mol Med. 2019 Nov;23(11):7535-7544.
- [16]Biochim Biophys Acta Mol Basis Dis. 25 October 2021, 166292.
- [17]Int Immunopharmacol. 2021 Dec 23;103:107840.
- [18]Cancer Med. 2019 Aug;8(9):4265-4277.
- [19]BMC Cancer. 2019 Apr 25;19(1):391.
- [20]Int J Mol Med. 2021 Apr 19.
- [21]Eur Rev Med Pharmacol Sci. 2019 May;23(10):4406-4413.
- [22]Mol Vis. 2018 Jul 23;24:485-494.
- [23]Mol Med Rep. 2022 Jul;26(1):246.
- [24]Mol Med Rep. 2018 Dec;18(6):5489-5501.
Summary
VO-Ohpic trihydrate is a highly potent inhibitor of PTEN with an IC 50 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 (IC 50 , 46±10 nM), which is in agreement with the previously determined potency (IC 50 , 35±2 nM) in a PIP 3 -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 (IC 50 =35 nM) of the PTEN lipid phosphatase activity [2] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : ≥ 50 mg/mL ( 120.42 mM )
H 2 O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 |
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1.
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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
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.