BAY-985，5MG，SML3843-5MG，Sigma

Biochem/physiol Actions

ATP-competitive, potent and selective inhibitor against TANK-binding kinase 1 (TBK1) and IKKe.

BAY-985 is an ATP-competitive, potent and selective inhibitor against IκB kinase members TANK-binding kinase 1 (TBK1 IC50 = 2/30 nM with 10 μM/1 mM ATP) and IKK-epsilon (IKKε IC50 = 2 nM with 10 μM ATP) with 60-, 138-, 155, and ~4000-fold lower potency toward FLT3, RSK4, DRAK1, and ULK1, respectively. BAY-985 potently inhibits cellular interferon regulatory factor 3 phosphorylation (pIRF3 IC50 = 74 nM) and displays antiproliferation efficacy in human melanoma SK-MEL-2 cultures (IC50 = 900 nM). When administered orally (200 mg/kg bid. po.), BAY-985 suppresses SK-MEL-2 xengraft-derived tumor growth in mice in vivo (T/C tumor weight ratio = 0.6).