BAY-985 is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase ε (IKKε; IC50 = 2 nM for both).1 It is selective for TBK1 and IKKε over FLT3, RSK4, DRAK1, and ULK1 (IC50s = 123, 276, 311, and 7,390 nM, respectively). BAY-985 inhibits phosphorylation of interferon regulatory factor 3 (IRF3) in MDA-MB-231 cells expressing mouse IRF3 (IC50 = 74 nM). It inhibits the proliferation of SK-MEL-2 cells in vitro (IC50 = 900 nM) and reduces tumor weight in an SK-MEL-2 mouse xenograft model when administered at a dose of 200 mg/kg.
1.Lefranc, J., Schulze, V.K., Hillig, R.C., et al.Discovery of BAY-985, a highly selective TBK1/IKKε inhibitorJ. Med. Chem.63(2)601-612(2020)