BpV(phen) (trihydrate)

BpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC₅₀s 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:IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)^[3]
Parasite Leishmania^[2]
Apoptosis^[1] 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]. 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].