bpV(phen) trihydrate, an insulin mimetic, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor (antagonist) with IC50s of 38 nM, 343 nM and PTEN for PTEN, PTP-β and PTP-1B. 920 nM. bpV(phen) trihydrate suppresses the proliferation/growth 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 activates the Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also cause apoptosis and has anti-angiogenic and anti-tumor activities.

Physicochemical Properties

Molecular Formula	C12H14KN2O8V
Molecular Weight	404.29
Exact Mass	403.983
CAS #	171202-16-7
Related CAS #	bpV(phen);42494-73-5
Appearance	Yellow to orange solid powder
LogP	0.456
SMILES	[V]=O.[K+].[O-][O-].[O-][O-].O.O.O.N1C=CC=C2C=CC3=CC=CN=C3C=12
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Leishmania
ln Vitro	In H/R-damaged H9c2 cells, treatment with bpV (phen) (5 μM; 24.5 hours; H9c2 cells) further reduced cell viability [1]. H/R-damaged H9c2 cells undergo increased apoptosis upon treatment with bpV (phen) (5 μM; 24.5 hours) [1]. H/R-damaged H9c2 cells' cytoplasmic cytochrome c accumulation was markedly enhanced by bpV (phen) (5 μM; 24.5 hours; H9c2 cells) treatment [1]. Stimulation with bpV (phen) inhibits PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy [1]. The insulin receptor tyrosine kinase is hyperphosphorylated and activated, resulting in the insulin mimic bpV (phen) [4].
ln Vivo	The mean tumor volume was significantly reduced in male BALB/c nude (nu/nu) athymic mice treated with bpV (phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days) [1].
Cell Assay	Cell Viability Assay[1] Cell Types: Hypoxia/reoxygenation (H/R)-injured H9c2 cells Tested Concentrations: 5 μM Incubation Duration: 24.5 hrs (hours) (hypoxia for 24 h; reoxygenation for 30 minutes) Experimental Results: Caused a further decrease of cell viability. Apoptosis Analysis[1] Cell Types: Hypoxia/reoxygenation (H/R)-injured H9c2 cells Tested Concentrations: 5 μM Incubation Duration: 24.5 hrs (hours) (hypoxia for 24 h; reoxygenation for 30 minutes) Experimental Results: Increased the apoptosis of H/R-injured H9c2 cells. Western Blot Analysis[1] Cell Types: Hypoxia/reoxygenation (H/R)-injured H9c2 cells Tested Concentrations: 5 μM Incubation Duration: 24.5 hrs (hours) (hypoxia for 24 h; reoxygenation for 30 minutes) Experimental Results: demonstrated an increased release of Cytochrome C.
Animal Protocol	Animal/Disease Models: Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells[2] Doses: 5 mg/kg Route of Administration: intraperitoneal (ip)injection; daily; for 38 days Experimental Results: Caused a significant reduction in average tumor volume.
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.

Solubility Data

Solubility (In Vitro)	H2O : 18.18 mg/mL (44.97 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 25 mg/mL (61.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with heating and sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.