The present invention provides methods and compositions for inhibiting IKK, as well as methods and compositions for identifying compounds with activity as inhibitors of IKK, and methods and compositions for the treatment of diseases and/or conditions wherein IKK is implicated and inhibition of its activity is desired. In addition, the present invention provides methods and compositions for the improving the therapeutic activity of COX2 inhibitors, comprising administering the COX2 to a subject in combination with a compound that inhibits IKK activity. The present invention further provides compositions that comprise compounds that inhibit IKK and COX2.