SGC-AAK1-1

SGC-AAK1-1

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 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

Features and Benefits

SGC-AAK1-1 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575980 SGC-AAK1-1 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£626.79 (exc VAT) per 25MG
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3575981 SGC-AAK1-1 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£156.00 (exc VAT) per 5MG
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