产品说明书
KY1220
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同义名 : | - |
| CAS号 : | 292168-79-7 | |
| 货号 : | A217096 | |
| 分子式 : | C14H10N4O3S | |
| 纯度 : | 98% | |
| 分子量 : | 314.319 | |
| MDL号 : | MFCD00609073 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(159.07 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Axin is a cytoplasmic protein which contains a regulation of G-protein signaling (RGS) domain and a dishevelled and axin (DIX) domain. Axin is a component of the β-catenin destruction complex required for regulating CTNNB1 levels through phosphorylation and ubiquitination, and modulating Wnt-signaling. In Wnt signaling, axin probably facilitates the phosphorylation of CTNNB1 and APC by GSK3B[3]. KY1220 specifically binds to the RGS domain of Axin, activates GSK3β via a conformational change enhancing β-catenin complex assembly, and subsequently degrade both β-catenin and Ras via proteasomal degradation[4]. The inhibitory IC50 of KY1220 on the Wnt/β-catenin pathway was 2.1 μM, and in HEK293 cells, both β-catenin and pan-Ras protein levels were reduced in a dose-dependent manner after treatment with KY1220 at the concentration of 5~50 μM[5]. The proliferation and transformation of HCT15, SW480, D-WT and D-MT colon cancer cells were efficiently inhibited after treatment with KY1220[5]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.91mL 3.18mL 1.59mL |
31.81mL 6.36mL 3.18mL |
| 参考文献 |
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