SGC-AAK1-1
产品说明书
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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： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 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 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.70mL 2.34mL 1.17mL |
23.39mL 4.68mL 2.34mL |
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