bpV(phen) trihydrate

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 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. bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells. bpV(phen) (5 μM; 24.5 hours; H9c2 cells) 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. bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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 AnalysisCell 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 . 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 cellsDosage: 5 mg/kg Administration: Intraperitoneal injection; daily; for 38 days Result: Caused a significant reduction in average tumor volume. Form:Solid IC50& Target:IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B),Parasite Leishmania,Apoptosis

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