產品描述: | 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. |
靶點: |
Apoptosis;Autophagy;Calcium Channel;Potassium Channel;TRP/TRPV Channel;Apoptosis;PotassiumChannel;CalciumChannel;TRP/TRPVChannel;Autophagy |
體外研究: |
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. |
體內研究: |
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. |
細胞實驗: |
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 |
參考文獻: |
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 |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
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: |
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