GSK-583 is a potent, selective and orally bioavailable RIPK2 kinase inhibitor with IC50 of 5 nM and 2 nM for human and rat RIP2, respectively.
GSK-583 displays robust selectivity against p38α and VEGFR2, and shows little or no inhibition of RIP3-dependent necroptotic cell death.
GSK-583 potently and dose dependently inhibits MDP-stimulated TNFα production in human monocytes and human whole bolld with IC50 of 8 nM and 237 nM, respectively.
GSK-583 inhibits MDP-induced inflammatory responses in vivo.
