GSK-481 (GSK481) is a highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase (RIPK1) with biochemical IC50 of 10 nM.
GSK-481 displays complete specificity for RIP1 kinase over a panel of 456 kinases.
GSK-481 exhibits excellent translation in the U937 cellular assay with IC50 of 10 nM, demonstrates significant blockage of the induced RIP1 autophosphorylation at Ser166 in HT29 cells.
GSK-481 possesses good pharmacokinetic profiles in rodents.
