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SGC-AAK1-1

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Chemical Structure| 2247894-32-0 同义名 : -
CAS号 : 2247894-32-0
货号 : A1189663
分子式 : C21H25N5O3S
纯度 : 97%
分子量 : 427.52
MDL号 : MFCD31689256
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(116.95 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Adaptor-associated kinase 1 (AAK1) has been proposed as being a promising drug target for the treatment of a variety of neurological and psychiatric disorders, such as schizophrenia, cognitive deficits in schizophrenia, Parkinson's disease, bipolar disorder, Alzheimer's disease and neuropathic pain[1].SGC-AAK1-1 is a potent and selective inhibitor of AAK1 (AP2 associated kinase 1) (IC50 of 270 nM and a Ki of 9 nM),and is a chemical probe. phosphorylation of AP2M1 (T156)significantly reduced by SGC-AAK1-1 (1.25 μM) and activates WNT-driven BAR activity compared in a dose-dependent manner in HT1080 cells. SGC-AAK1-1 blocks AAK1 kinase activity, resulting in increased β-catenin protein stability and β-catenin-dependent transcription.Following KINOMEscan of compounds 25 (SGCAAK-1) and 26, the binding affinities (KD) of all kinases inhibited >80% at 1 μM plus AAK1 and a few kinases inhibited by structurally related analogs were determined .Only three kinases were bound by 25 within 30-fold of the potency of 25 for AAK1: RIOK1 (KD = 72), RIOK3 (KD =290), and PIP5K1C (KD = 260) [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.39mL

4.68mL

2.34mL
参考文献

[1] Belén Martinez-Gualda, Dominique Schols, Steven De Jonghe. A patent review of adaptor associated kinase 1 (AAK1) inhibitors (2013-present). Expert Opin Ther Pat. 2021 Oct;31(10):911-936.

[2]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.