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

Christopher R M AsquithBenedict-Tilman BergerJing WanJames M BennettStephen J CapuzziDaniel J CronaDavid Harold DrewryMichael P EastJonathan M ElkinsOleg FedorovPaulo H GodoiDebra M HunterStefan KnappSusanne MüllerChad D TorriceCarrow I WellsH Shelton EarpTimothy M WillsonWilliam J Zuercher
Published in: Journal of medicinal chemistry (2019)
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.
Keyphrases
  • cell cycle
  • high throughput
  • single cell
  • living cells
  • social media
  • tyrosine kinase
  • anti inflammatory
  • cell death
  • signaling pathway