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SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K

Carrow Wells, Rafael M Couñago, Juanita C Limas, Tuanny L Almeida, Jeanette Gowen Cook, David H Drewry, Jonathan M Elkins, Opher Gileadi, Nirav R Kapadia, Alvaro Lorente-Macias, Julie E Pickett, Alexander Riemen, etc.

ACS Med Chem Lett. 2019 Oct 23;11(3):340-345.

PMID: 32184967

Abstract:

Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization 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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR4245233 SGC-AAK1-1 SGC-AAK1-1 Price
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