bpV(HOpic) (potassium salt, technical grade)

• 纯度 = 98.00%

IC50: 14 nM for PTEN; 4.9 μM for PTP-β; 25.3 μM for PTP-1βB

bpV(HOpic) is a protein tyrosine phosphatases inhibitor.

The tumour suppressor phosphatase and tensin homologue deleted on chromosome 10 (PTEN) shares homology with protein tyrosine phosphatases (PTPases).

In vitro: Previous study showd that T bpVs with polar N,O ligands (bpV(HOpic) and bpV(pic) had a strong preference towards PTEN, while bpVs with the neutral N,N ligands seemed to be more promiscuous targeting both PTPases and PTEN. bpV(HOpic) could induce the phosphorylation of PKB in a dose-dependent manner. For cytotoxicity, it was found that bpV(HOpic) showed cytoxicity significantly killing cells at concentrations equal or higher than 100 μM, indicating nanomolar doses that coud inhibit in-vitro and in-vivo PTEN phosphatase activity might not affect cell viability [1].

In vivo: The purpose of a previous study was to test the optimal neuroprotective dose of bpV(HOpic) when administrated after focal ischemia/reperfusion (I/R) injury in rats. bpV(HOpic) at 0.25, 0.50 and 1.0 mg/kg were intraperitoneally injected just after reperfusion. Results showed that the maximal reduction in brain injury was observed with 1.0 mg/kg. This dose could also significantly block apoptosis in the penumbral cortex of rats. Such beneficial effect was probably due to the increasing levels of Akt phosphorylation in the penumbral cortex [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Schmid, A. C.,Byrne, R.D.,Vilar, R., et al. Bisperoxovanadium compounds are potent PTEN inhibitors. FEBS Letters 566(1-3), 35-38 (2004).
[2] Guo JY, Ding J, Yuan F, Chen H, Chen SW, Tian HL. Dose-dependent protective effect of bisperoxovanadium against acute cerebral ischemia in a rat model of ischemia/reperfusion injury. Int J Mol Sci. 2013 Jun 5;14(6):12013-22.