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SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)
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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.
Title: SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)
Description:
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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