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| | bpV(phen) (potassium hydrate) Basic information |
| | bpV(phen) (potassium hydrate) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 1 mg/ml; PBS (pH 7.2): 10 mg/ml | | form | A crystalline solid | | color | Yellow to orange |
| | bpV(phen) (potassium hydrate) Usage And Synthesis |
| Description | bpV(phen) is a bisperoxovanadium (bpV) compound which inhibits several different protein tyrosine phosphatases (PTPs), with selectivity for PTEN (IC50 = 38 nM). It also inhibits the vascular endothelial PTP, PTP-β (IC50 = 343 nM), and PTP-1β (IC50 = 920 nM). At 0.1 mM, bpV(phen) inhibits SH2 domain-containing inositol 5’-phosphatase-2. Presumably by inhibiting insulin receptor kinase-associated PTPs, bpV(phen) activates the insulin receptor tyrosine kinase and promotes downstream signaling, including activation of PI3-kinase. | | Uses | bpV(phen) (Potassium Hydrate) inhibits several different protein tyrosine phosphatases (PTPs). | | 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]. | 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. |
| | IC 50 | Leishmania | | References | [1] J-P LAI D L K J T Dalton. Phosphatase and tensin homologue deleted on chromosome ten (PTEN) as a molecular target in lung epithelial wound repair[J]. British Journal of Pharmacology, 2009, 152 8: 1172-1184. DOI: 10.1038/sj.bjp.0707501
[2] ANNETTE C. SCHMID. Bisperoxovanadium compounds are potent PTEN inhibitors[J]. FEBS Letters, 2004, 566 1-3: 35-38. DOI: 10.1016/j.febslet.2004.03.102
[3] AZUCENA KAKAZU H E P B Guru Sharma. Association of protein tyrosine phosphatases (PTPs)-1B with c-Met receptor and modulation of corneal epithelial wound healing.[J]. Investigative ophthalmology & visual science, 2008: 2927-2935. DOI: 10.1167/iovs.07-0709
[4] IAN H BATTY. The control of phosphatidylinositol 3,4-bisphosphate concentrations by activation of the Src homology 2 domain containing inositol polyphosphate 5-phosphatase 2, SHIP2.[J]. Biochemical Journal, 2007, 407 2: 255-266. DOI: 10.1042/bj20070558
[5] B I POSNER. Peroxovanadium compounds. A new class of potent phosphotyrosine phosphatase inhibitors which are insulin mimetics.[J]. The Journal of Biological Chemistry, 1994, 269 6: 4596-4604.
[6] A P BEVAN. Selective activation of the rat hepatic endosomal insulin receptor kinase. Role for the endosome in insulin signaling.[J]. The Journal of Biological Chemistry, 1995, 270 18: 10784-10791. DOI: 10.1074/jbc.270.18.10784
[7] C J BAND. 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).[J]. Molecular endocrinology, 1997, 11 13: 1899-1910. DOI: 10.1210/mend.11.13.0041 |
| | bpV(phen) (potassium hydrate) Preparation Products And Raw materials |
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