SML2219
SGC-AAK1-1
≥98% (HPLC)
Synonym(s):
N-(6-(3-(N,N-Diethylsulfamoylamino)phenyl)-1H-indazol-3-yl)cyclopropanecarboxamide
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About This Item
Empirical Formula (Hill Notation):
C21H25N5O3S
CAS Number:
Molecular Weight:
427.52
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
CCN(CC)S(NC1=CC=CC(C2=CC(NN=C3NC(C4CC4)=O)=C3C=C2)=C1)(=O)=O
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
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.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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