AAK1 inhibitor 1

SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1[1].

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 μM) without detectable cytotoxicity. Selectivity profiling identifies only 5 additional kinases among a panel of ∼400 with >50% inhibition by 1 μM 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 μM by AAK1 activity assay; KD = 8.8 μM/AAK1 & >10 μM/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

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[1] Agajanian MJ, et al. WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop. Cell Rep. 2019 Jan 2;26(1):79-93.e8. DOI:10.1016/j.celrep.2018.12.023