A Chemical Probe Targeting AAK1 and BMP2K

04 September 2019, Version 1

Abstract

Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization of this 3-acylaminoindazole scaffold furnished a small molecule chemical probe (SGC-AAK1-1, 25) that is potent and selective for AAK1/BMP2K over other NAK family members, demonstrates narrow activity in a kinome-wide screen, and is functionally active in cells. This inhibitor represents one of the best available small molecule tools to study the functions of AAK1 and BMP2K.

Keywords

AAK1
BMP2K
NAK Family
Endocytosis
Protein kinase
acylaminoindazole

Supplementary materials

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ACS MCL experimental final
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