bioRxivCell Biology
SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)
C. R. M. Asquith, B.-T. Berger, J. Wan, J. M. Bennett, M. P. East, J. M. Elkins, O. Fedorov, P. H. Godoi, D. M. Hunter, S. Knapp, S. Mueller, C. I. Wells, H. S. Earp, T. M. Willson, W. J. Zuercher
Abstract
We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G associated kinase (GAK), together with a structurally-related negative control SGC-GAK-1N (14). SGC-GAK-1 is highly selective in a kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent inhibitor of RIPK2 lacking GAK activity. Together, the chemical probe set of 11, 14, and 18 can be used to interrogate the cellular biology of GAK inhibition.
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