GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10?000-fold selective for RIP1 over 339 other kinases.
GSK'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4?nM in human and murine cells[1].
GSK'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2?mg/kg, GSK'963 would maintain blood concentrations above the concentration required for 90% inhibition of RIP1 activity for an extended period of time compared with Nec-1[1].
[1] Berger SB, et al. Cell Death Discov. 2015, 1:15009.