PHA-408 (PHA-767408) is a potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.
PHA-408 inhibits LPS-induces TNF-α producton in PBMCs and HWB with IC50 of 20-30 nM, prevents IL-1β-induced IκBα phosphorylation in RASFs while sparing the JNK and p38 MAPK pathways and has no effect on IKK-2 phosphorylation.
PHA-408 demonstrates target-specific anti-inflammatory activities in in vivo model of airway inflammation.
