GSK2983559-AM is the acitve form of GSK2983559, a potent, selective RIPK2 with IC50 of 5 nM.
GSK2983559-AM potently and dose dependently inhibited MDP-stimulated IL-8 production in HEK293 cells and TNFα production in monocytes with IC50 of 4 nM and 13 nM, respectively.
GSK2983559-AM displays little to no effect against a panel of other innate immune receptors, including TNFR, IL1R and TLR2/4/7/9 (IC50>10 uM).
The prodrug GSK2983559 reduced inflammation, edema, and goblet cell depletion in a murine TNBS colitis model.
