| 产品描述： | SKF-96365, a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ/AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 inhibited hERG current in a concentration-dependent manner. |
| 靶点： |
Apoptosis;Autophagy;Calcium Channel;Potassium Channel;TRP/TRPV Channel;Apoptosis;PotassiumChannel;CalciumChannel;TRP/TRPVChannel;Autophagy |
| 体外研究： |
SKF-96365 exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells. SKF-96365 inhibits hERG current in a concentration-dependent manner. SKF-96365 can induces cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 treatment inhibits the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade. Overexpression of CaMKIIγ or AKT abolishes the effects of SKF-96365 on cancer cells, suggesting a critical role of the CaMKIIγ/AKT signaling pathway in SFK-96365-induced biological effects. |
| 体内研究： |
SKF-96365 inhibits CRC cell growth in vivo. SKF-96365 treatment results in a decrease of p-CaMKII and p-AKT as well as an increase in LC3-II, cleaved PARP, caspase-3, and caspase-9 in mice. |
| 细胞实验： |
To investigate whether SKF-96365 could protect PC12 cells from injury induced by MPP+ insult, cultured PC12 cells are pretreated with SKF-96365 in different concentrations (1 µM, 10 µM or 50 µM) 30 min before MPP+ addition. The cells viability is measured 24 h after MPP+ insult by using the cell proliferation reagent WST-1. (Only for Reference) Cell lines: PC12 cells |
| 参考文献： |
1. Chen T, et al. PLoS One. 2013, 8(1):e55601. 2. Yao H, et al. Cell Death Differ. 2009, 16(12):1681-1693. 3. Singh A, et al. Br J Pharmacol. 2010, 160(6):1464-1475. 4. Jing Z, et al. Cancer Lett. 2016, 372(2):226-38. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.482 ml |
12.41 ml |
24.819 ml |
| 5 mM |
0.496 ml |
2.482 ml |
4.964 ml |
| 10 mM |
0.248 ml |
1.241 ml |
2.482 ml |
| 50 mM |
0.05 ml |
0.248 ml |
0.496 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京