TPCA-1

A potent and selective inhibitor of IκB kinase-2 (IKK-2) (IC₅₀ = 17.9 nM). Displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. TPCA-1 inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF-κB nuclear localization. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.