Synonyms: N-(6-(3-(N,N-Diethylsulfamoylamino)phenyl)-1H-indazol-3-yl)cyclopropanecarboxamide
Molecular Formula: C21H25N5O3S
Molecular Weight: 427.52
Linear Structural Formula: C21H25N5O3S
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: SGC-AAK1-1 is an ATP-competitive kinase inhibitor against AP2-associated protein kinase 1/AAK1 and BMP-2-inducible protein kinase/BIKE/BMP2K (Ki = 9.1 & 17 nM, respectively, by ATP site fluorescent tracer displacement assay; AAK1 IC50 = 270 nM by coupled enzyme assay). SGC-AAK1-1 downregulates cellular AP2M1 Thr156 phosphorylation level in a dose-dependent manner (ECmax >=12.5 muM) without detectable cytotoxicity. Selectivity profiling identifies only 5 additional kinases among a panel of >=400 with >50% inhibition by 1 muM SGC-AAK1-1 (KD = 72 nM/RIOK1, 290 nM/RIOK3, 260 nM/PIP5K1C, 880 nM/CDKL1, 960 nM/MYLK2 by DiscoverX KINOMEscan). SGC-AAK1-1N is a structure analog and the recommended negative control (IC50 = 11 muM by AAK1 activity assay; KD = 8.8 muM/AAK1 & >10 muM/BIKE vs. KD = 26 nM/AAK1 & 930 nM/BIKE with SGC-AAK1-1 by DiscoverX). For characterization details of SGC-AAK1-1, please visit the SGC-AAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.SGC-AAK1-1N is the negative control for the active probe, SGC-AAK1-1. SGC-AAK1-1N is available from Sigma. To learn more about and purchase SGC-AAK1-1N, click here.To learn about other SGC chemical probes, visit sigma.com/sgc