GSK583

Description: GSK583 is a highly potent and selective RIP2 kinase inhibitor with an IC50 value of 5 nM. RIP2 kinase is a critical component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines. GSK583 exhibits comparable binding affinity for RIP3 kinase in an in-house FP binding assay configured similarly to the RIP2 FP assay (RIP2 FP IC50 = 5 nM; RIP3 FP IC50 = 16 nM). Despite the potent biochemical activity against RIP3 kinase, GSK583 shows little or no inhibition of RIP3-dependent necroptotic cell death in a cellular assay up to 10 uM concentration.

References: J Med Chem. 2016 May 26; 59(10):4867-80.