In vitro study | BMS-582949 inhibition of p38 activation in the cell, reducing the level of phosphorylation of p38. When p38 is activated by LPS, BMS-582949 treatment rapidly reverses this activation, whereby p38 phosphorylation is reduced. BMS-582949 is a double-acting inhibitor of p38, which inhibits both the activity of p38 kinase itself and the activation of p38 itself in cells. BMS-582949 binds to p38a, causing a conformational change in the p38a activation loop (which can be phosphorylated by an upstream kinase), thereby inhibiting its phosphorylation. |