PeptideDB

bpV(phen)

CAS No.: 42494-73-5

bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor (IC50s: 343 nM, 920 nM, and 38 nM for PTP-β
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Description bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor (IC50s: 343 nM, 920 nM, and 38 nM for PTP-β, PTP-1B, and PTEN).
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 and increases the apoptosis of H/R-injured H9c2 cells. bpV(phen) (5 μM; 24.5 hours; H9c2 cellfs) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells. After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited [1].
In vivo bpV(phen) (5 mg/kg; i.p.; daily; for 38 days; male BALB/c nude (nu/nu) athymic mice) treatment causes a significant reduction in average tumor volume [1].
Target activity PTP1B:920 nM , PTEN:38 nM , PTP-β:343 nM
molecular weight 350.24
Molecular formula C12H8KN2O5V
CAS 42494-73-5
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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. 2015 Oct 23;290(43):26051-8.