GSK669 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor, inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling (IC50=0.5 uM), has an IC50 of 3.2 uM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.GSK669 specifically inhibits MDP-induced NOD2 activation, has no effect on IL-8 secretion induced by over-expression of NOD1.GSK669 significantly inhibits platelet proinflammatory cytokine release induced by muramyl dipeptide, platelet aggregation, ATP release, and ROS generation induced by collagen and collagen related peptide (CRP). GSK669 inhibits thrombosis and oxidative stress via targeting platelet glycoprotein VI (GPVI), decreases malonaldehyde (MDA) and increases superoxide dismutase (SOD) levels in mouse plasma
