SGC-AAK1-1 | AAK1 Inhibitor | AmBeed-信号通路专用抑制剂

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SGC-AAK1-1 {[allProObj[0].p_purity_real_show]}

货号：A1189663

SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor.

SGC-AAK1-1 化学结构
CAS号：2247894-32-0

SGC-AAK1-1 3D分子结构
CAS号：2247894-32-0

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SGC-AAK1-1 纯度/质量文件产品仅供科研

货号：A1189663 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

SGC-AAK1-1 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].

SGC-AAK1-1 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.

SGC-AAK1-1 实验方案

计算器

存储液制备

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

SGC-AAK1-1 技术信息

CAS号	2247894-32-0
分子式	C₂₁H₂₅N₅O₃S
分子量	427.52

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

SGC-AAK1-1 {[allProObj[0].p_purity_real_show]}

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SGC-AAK1-1 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SGC-AAK1-1 质控信息

SGC-AAK1-1 生物活性

SGC-AAK1-1 参考文献

SGC-AAK1-1 实验方案

SGC-AAK1-1 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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