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SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK)

Christopher R M Asquith, Benedict-Tilman Berger, Jing Wan, James M Bennett, Stephen J Capuzzi, Daniel J Crona, David H Drewry, Michael P East, Jonathan M Elkins, Oleg Fedorov, Paulo H Godoi, Debra M Hunter, etc.

J Med Chem. 2019 Mar 14;62(5):2830-2836.

PMID: 30768268

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). 11 was highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent RIPK2 inhibitor lacking GAK activity. Together, this chemical probe set can be used to interrogate GAK cellular biology.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR4245230 SGC-GAK-1 SGC-GAK-1 Price
IAR4245231 SGC-GAK-1N SGC-GAK-1N Price
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