bpV(HOpic)

BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity[1][2].

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> PTEN

Research Areas >> Neurological Disease

IC50: 14 nM (PTEN)[1]

BpV(HOpic) (1 µM) treatment increases cell proliferation and decreases apoptotic rate in MG63 cells received Cisplatin treatment[3]. Bpv(HOpic) (1 µM) enhances migration of C2C12 myoblasts and is associated with activation of PI3K/AKT and MAPK/ERK signalling pathways[4]. BpV(HOpic) (1 µM; 48 hours) promotes the initiation of swine follicle growth and development, similar as in rodent species and humans[5]. Nanocarrier-BpV(HOpic) enhances axonal outgrowth of neurons[2].

BpV(HOpic) (0.05 mg/kg; i.p.) at reperfusion ameliorates liver ischemia/reperfusion (I/R) injury in vivo[6]. BpV(HOpic) (200 μg/kg; i.p.) exacerbates renal dysfunction and promotes tubular damage in mice with ischemia/reperfusion injury (IRI)[7]. Animal Model: Male Wistar rats are subjected to partial hepatic ischemia[6] Dosage: 0.05 mg/kg Administration: I.p. injections at the start of reperfusion Result: Ameliorated reoxygenation injury and reproduced the hepatoprotective effects obtained by adenosine A2A receptor stimulation. Animal Model: Male C57BL/6 mice (8-12 weeks old; 20-30 g ) are subjected to renal ischemia[7] Dosage: 200 μg/kg Administration: I.p. injections 1 h before ischemia and then administers every 6 h after ischemia for 24 hr Result: Raised the level of serum creatinine and blood serum urea nitrogen.

[1]. Schmid AC, et, al. Bisperoxovanadium compounds are potent PTEN inhibitors. FEBS Lett. 2004 May 21; 566(1-3): 35-8.

[2]. Kim MS, et, al. Nanotherapeutics of PTEN Inhibitor with Mesoporous Silica Nanocarrier Effective for Axonal Outgrowth of Adult Neurons. ACS Appl Mater Interfaces. 2016 Jul 27; 8(29): 18741-53.

[3]. Zhang B, et, al. Silencing of miR-19a-3p enhances osteosarcoma cells chemosensitivity by elevating the expression of tumor suppressor PTEN. Oncol Lett. 2019 Jan; 17(1): 414-421.

[4]. Dimchev GA, et, al. Phospho-tyrosine phosphatase inhibitor Bpv(Hopic) enhances C2C12 myoblast migration in vitro. Requirement of PI3K/AKT and MAPK/ERK pathways. J Muscle Res Cell Motil. 2013 May; 34(2): 125-36.

[5]. Raffel N, et, al. The effect of bpV(HOpic) on in vitro activation of primordial follicles in cultured swine ovarian cortical strips. Reprod Domest Anim. 2019 Aug; 54(8): 1057-1063.

[6]. Ponte CD, et, al. Pharmacological postconditioning protects against hepatic ischemia/reperfusion injury. Liver Transpl. 2011 Apr; 17(4): 474-82.

[7]. Zhou J,et, al. Pharmacological Inhibition of PTEN Aggravates Acute Kidney Injury. Sci Rep. 2017 Aug 25; 7(1): 9503.