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SGC-AAK1-1

Chemical Structure : SGC-AAK1-1

CAS No.: 2247894-32-0

SGC-AAK1-1 (AAK1 inhibitor 1)

Catalog No.: PC-35853Not For Human Use, Lab Use Only.

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).

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Biological Activity

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).
SGC-AAK1-1 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.
SGC-AAK1-1 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.

Physicochemical Properties

M.Wt 427.523
Formula C21H25N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Agajanian MJ, et al. Cell Rep. 2019 Jan 2;26(1):79-93.e8.

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