BAY-985 is a novel, potent, orally bioavailable and highly specific ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. It has antitumor activity. The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its
homologue IKKε are noncanonical members of the inhibitor of the nuclear
factor κB (IκB) kinase family. These kinases play important roles in
multiple cellular pathways and, in particular, in inflammation. BAY-985 inhibits the cellular phosphorylation of interferon regulatory
factor 3 and displays antiproliferative efficacy in the melanoma cell
line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2
human melanoma xenograft model.