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. The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKKε are non-canonical members of the inhibitor of nuclear factor κB (IκB) kinase family. These kinases play important roles… Click to show full abstract
. The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKKε are non-canonical members of the inhibitor of nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKKε inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2, but showed only weak to moderate antitumor activity in the SK-MEL-2 human melanoma xenograft model.
Journal Title: Journal of medicinal chemistry
Year Published: 2019
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