[CAS NO. 171202-16-7] bpV(phen)trihydrate
PRODUCTS SPECIFICATIONS [171202-16-7]
DESCRIPTION [171202-16-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 404.29 |
| Molecular Formula | C12H14KN2O8V |
| SMILES | O=[V+3]12([N]3=CC=C4)([O-][O-]1)([O-][O-]2)[N]5=C6C3=C4C=CC6=CC=C5.O.O.O.[K+] |
2 Publications Citing Use of MCE
Summary
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC 50 s of 38 nM, 343 nM and 920 nM for PTEN , PTP-β and PTP-1B , respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis , and has anti-angiogenic and anti-tumor activity [1] [2] [3] [4] [5] .
IC50 & Target
In Vitro
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment causes a further decrease of cell viability in H/R-injured H9c2 cells
[1]
.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells
[1]
.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells
[1]
.
After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited
[1]
.
bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | Hypoxia/reoxygenation (H/R)-injured H9c2 cells |
| Concentration: | 5 μM |
| Incubation Time: | 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes) |
| Result: | Caused a further decrease of cell viability. |
Apoptosis Analysis [1]
| Cell Line: | Hypoxia/reoxygenation (H/R)-injured H9c2 cells |
| Concentration: | 5 μM |
| Incubation Time: | 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes) |
| Result: | Increased the apoptosis of H/R-injured H9c2 cells. |
Western Blot Analysis [1]
| Cell Line: | Hypoxia/reoxygenation (H/R)-injured H9c2 cells |
| Concentration: | 5 μM |
| Incubation Time: | 24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes) |
| Result: | Showed an increased release of Cytochrome C. |
In Vivo
bpV(phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days; male BALB/c nude (nu/nu) athymic mice) treatment causes a significant reduction in average tumor volume [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells [2] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 38 days |
| Result: | Caused a significant reduction in average tumor volume. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 18.18 mg/mL ( 44.97 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4735 mL | 12.3674 mL | 24.7347 mL |
| 5 mM | 0.4947 mL | 2.4735 mL | 4.9469 mL |
| 10 mM | 0.2473 mL | 1.2367 mL | 2.4735 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (61.84 mM); Clear solution; Need ultrasonic and warming
References
- [1] Tang W, et al. PTEN-mediated mitophagy and APE1 overexpression protects against cardiac hypoxia/reoxygenation injury. In Vitro Cell Dev Biol Anim. 2019 Oct;55(9):741-748.
- [2] Caron D, et al. Protein tyrosine phosphatase inhibition induces anti-tumor activity: evidence of Cdk2/p27 kip1 and Cdk2/SHP-1 complex formation in human ovarian cancer cells. Cancer Lett. 2008 Apr 18;262(2):265-75.
- [3] Schmid AC, et al. Bisperoxovanadium compounds are potent PTEN inhibitors. FEBS Lett. 2004 May 21;566(1-3):35-8.
- [4] Band CJ, et al. Early signaling events triggered by peroxovanadium [bpV(phen)] are insulin receptor kinase (IRK)-dependent: specificity of inhibition of IRK-associated protein tyrosine phosphatase(s) by bpV(phen). Mol Endocrinol. 1997 Dec;11(13):1899-910.
- [5] Chen Q, et al. Potassium Bisperoxo(1,10-phenanthroline)oxovanadate (bpV(phen)) Induces Apoptosis and Pyroptosis and Disrupts the P62-HDAC6 Protein Interaction to Suppress the Acetylated Microtubule-dependent Degradation of Autophagosomes. J Biol Chem. 201