A cell-permeable naphthyridine N-oxide compound that acts as a potent, reversible p38α MAP kinase inhibitor (IC 50 = 68nM) and exhibits excellent selectivity among 54-kinases
It acts on the ATP-binding site plus an adjacent hydrophobic pocket
Exhibits desirable ADME (Absorption, Distribution, Metabolism, and Excretion) profile with good microsomal stability, low toxicity, and low reactivity towards cytochrome P450 isozymes
Shown to inhibit lipopolysaccharide-induced TNFα production in a dose-dependent manner (ED 50 of 0.5mg/kg).