SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)
Asquith C., Berger B-T., Wan J., Bennett J., East M., Elkins J., Fedorov O., Godoi P., Hunter D., Knapp S., Mueller S., Wells C., Earp S., Willson T., Zuercher W.
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.