Description
InformationGSK'963 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.TargetsRIP1 kinase (Cell-free assay) 29 nMIn vitroGSK\'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4\u2009nM in human and murine cells.In vivoGSK\'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2\u2009mg/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.Cell Research(from reference)Cell lines：BMDM Concentrations：100\u2009nM Incubation Time：30 min