AAK1 inhibitor 1

Research use only, not for human use.

AAK1 inhibitor 1 (SGC-AAK1-1) is a potent, selective inhibitor of AAK1 and BMP2K/BIKE.

AAK1 inhibitor 1 (SGC-AAK1-1) is a potent, selective inhibitor of AAK1 and BMP2K/BIKE ((BMP-2 inducible kinase)) that potently targets the ATP-binding site (AAK1 Ki =9.1 nM, BIKE Ki= 17 nM); disaplays excellent kinase selectivity, only three kinases (RIOK1 KD=72 nM, RIOK3 KD=290 nM, and PIP5K1C KD=260 nM) were observed to bind SGC-AAK1-1 within 30-fold of the KD of AAK1 in a KINOMEscan assay; has potency for ectopically expressed full-length AAK1- and BIKE-Nluc fusion proteins (AAK1 IC50=230 nM; BIKE IC50=1.5 uM)in a live cell NanoBRET assay.

SGC-AAK1-1 (1.25 μM) significantly reduces phosphorylation of AP2M1 (T156) and activates WNT-driven BAR activity compared in a dose-dependent manner in HT1080 cells.SGC-AAK1-1 blocks AAK1 kinase activity, resulting in increased β-catenin protein stability and β-catenin-dependent transcription.

——

SGC-AAK1-1

Others

AAK1

AAK1

——

——

2247894-32-0

427.523

C21H25N5O3S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (116.95 mM)

CCN(CC)S(=O)(=O)NC1=CC=CC(=C1)C2=CC3=C(C=C2)C(=NN3)NC(=O)C4CC4

N-(6-(3-((N,N-diethylsulfamoyl)amino)phenyl)-1H-indazol-3-yl)cyclopropanecarboxamide

(-20℃)

With Ice Pack

≥ 2 years