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SGC-AAK1-1,≥98% (HPLC)

别名:N-(6-(3-(N,N-二乙基氨磺酰氨基)苯基)-1H-吲唑-3-基)环丙烷甲酰胺;N-(6-(3-(N,N-Diethylsulfamoylamino)phenyl)-1H-indazol-3-yl)cyclopropanecarboxamide

Empirical Formula (Hill Notation): C21H25N5O3S 分子量: 427.52
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML2219
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$340.36

说明

生化/生理作用

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-AAK1-1 是一种化学探针,可通过与结构基因组学联盟 (SGC) 合作获得。
 

特点和优势

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.
 

属性

测定

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES string

CCN(CC)S(NC1=CC=CC(C2=CC(NN=C3NC(C4CC4)=O)=C3C=C2)=C1)(=O)=O

 

安全信息

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16