On July 31, 2012, Hutti, Jessica E.; Porter, Melissa A.; Cheely, Adam W.; Cantley, Lewis C.; Wang, Xiaodong; Kireev, Dmitri; Baldwin, Albert S.; Janzen, William P. published an article.COA of Formula: C20H24N2O4 The title of the article was Development of a high-throughput assay for identifying inhibitors of TBK1 and IKKε. And the article contained the following:
IKKε and TBK1 are noncanonical IKK family members which regulate inflammatory signaling pathways and also play important roles in oncogenesis. However, few inhibitors of these kinases have been identified. While the substrate specificity of IKKε has recently been described, the substrate specificity of TBK1 is unknown, hindering the development of high-throughput screening technologies for inhibitor identification. Here, we describe the optimal substrate phosphorylation motif for TBK1, and show that it is identical to the phosphorylation motif previously described for IKKε. This information enabled the design of an optimal TBK1/IKKε substrate peptide amenable to high-throughput screening and we assayed a 6,006 compound library that included 4,727 kinase-focused compounds to discover in vitro inhibitors of TBK1 and IKKε. 227 Compounds in this library inhibited TBK1 at a concentration of 10 μM, while 57 compounds inhibited IKKε. Together, these data describe a new high-throughput screening assay which will facilitate the discovery of small mol. TBK1/IKKε inhibitors possessing therapeutic potential for both inflammatory diseases and cancer. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).COA of Formula: C20H24N2O4
The Article related to high throughput screening tbk1 ikk inhibitor, Pharmacology: Methods and other aspects.COA of Formula: C20H24N2O4