KINASE PROFILING Kinase Selectivity Profiling Easy-to-Use Strip Tube Format W hen profiling compounds against a broad panel of kinases, researchers desire technology that is universal and consistent for assessing selectivity and potency of inhibitors against multiple classes of kinases. Although several platforms for kinase inhibitor profiling exist, most have limitations, including confidentiality issues if profiling is outsourced, immediate accessibility to generated data, and costly, time-consuming assay development required for each kinase when profiling in-house. The Kinase Selectivity Profiling Systems for kinase inhibitor profiling studies are based on the luminescent ADP-Glo™ Kinase Assay, a universal kinase detection system, and offer several advantages. • Sets of kinases organized by kinase families, presented in easy-to-use multiwell strips and standardized for optimal kinase activity. • Flexible kinase inhibitor profiling by assessing compounds at a single dose or testing a dose response against eight kinases at once. • Fast, simple reaction assembly that can be easily automated. Using the kinase profiling strips in the Kinase Selectivity Profiling Systems (Figure 1), we have generated selectivity profiles using small or large kinase panels, as well as identifying compound promiscuity towards members of a single kinase subfamily or different subfamilies of the kinome. Figure 1 is an overview of the Kinase Profiling System protocol. Figure 2 shows a dose response profile with the TK-3 family of kinases using a selective and nonselective inhibitor. With these benefits to the user, the bioluminescent kinase platform offers routine performance of inhibitor profiles in a quick and flexible manner using one assay format for all classes of kinases when evaluating compounds during drug discovery. Learn More enews | April 2015 Pagina 5

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Promega Benelux - Monthly online Magazine - April 2015 edition Lees publicatie 100Home


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