Biological Activity
PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective[1][2][3].
PB1 produces a robust activation of the BDNF effector ERK1/2. PB1 promotes RGC survival[1].
PB1 (150 μM; intraocular injection; 1 week) attenuates the loss of both RGC (retinal ganglion cells) soma and axons in experimental glaucoma[1].PB1 protects RGC soma in experimental glaucoma. PB1 single dose limits the biological activity in vivo. PB1 attenuates the loss of both RGC soma and axons in experimental glaucoma. PB1 (0.001~100 μM; 72 hours) is effective at rescuing acutely axotomized retinal ganglion cells[1][2].
References
[1]. Almasieh M, et al. A cell-permeable phosphine-borane complex delays retinal ganglion cell death after axonal injury through activation of the pro-survival extracellular signal-regulated kinases 1/2 pathway. J Neurochem. 2011;118(6):1075-1086. [2]. Schlieve CR, et al. Synthesis and characterization of a novel class of reducing agents that are highly neuroprotective for retinal ganglion cells. Exp Eye Res. 2006;83(5):1252-1259. [3]. Niemuth NJ, et al. Intracellular disulfide reduction by phosphine-borane complexes: Mechanism of action for neuroprotection. Neurochem Int. 2016;99:24-32.
