SIS3
产品说明书
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同义名 : | SIS3 HCl |
| CAS号 : | 521984-48-5 | |
| 货号 : | A170854 | |
| 分子式 : | C28H28ClN3O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 489.993 | |
| MDL号 : | MFCD09265258 | |
| 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 : |
DMSO: 120 mg/mL(244.9 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： |
IP 2% DMSO+2% Tween80+30% PEG300+water 7 mg/mL clear PO 0.5% CMC-Na 28 mg/mL suspension |
| 生物活性 | |||
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| 描述 | Smads are a family of proteins with similar structure that mediates the numerous effects of the transforming growth factor beta (TGF-β) superfamily, which are critically important for tissue regeneration and homeostasis[1]. The specific inhibitor of Smad3 (SIS3) is a synthesized chemical that specifically inhibits Smad3 with IC50 value of 3 μM[2]. A549 cells were treated with 3 μM of SIS3 for 4h prior to 5 ng/mL TGF-β1 exposure for 48 hours. SIS3 markedly decreased the expression of p-Smad3 that was induced by TGF-β1 but did not affect total Smad3 expression as examined by western blotting assay. The results from immunofluorescence assay also indicated that the A549 cells had an obvious nuclear expression of p-Smad3 with a spindle-shaped-like morphology when treated with TGF-β1 only. However, after the pre-treatment with SIS3, the TGF-β1-induced morphological changes were not significant and the fluorescence intensity of p-Smad3 was weakened mainly in the nucleus[3]. In ureteral obstruction (UUO) BALB/c mouse model, 0.2 and 2 mg/kg of SIS3 was intraperitoneally injected to the mice daily for 1 week, and on the 8th post-operation day, the kidney was harvested. The phosphorylation levels of Smad3 were remarkably decreased after treating with SIS3 and the signal ligand TGF-β1 also showed suppression in a dose dependent level measured by western blotting assay[4]. |
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| 作用机制 | SIS3 can specifically inhibits Smad3 phosphorylation and its binding to Smad4 [4] . | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.20mL 2.04mL 1.02mL |
20.41mL 4.08mL 2.04mL |
| 参考文献 |
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