SKF-96365 hydrochlorideCAS号: 130495-35-1分子式: C22H26N2O3.HCl分子量: 402.91描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
产品描述 | |
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.
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纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
SKF 96365 hydrochloride
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外观 |
白色固体
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可溶性/溶解性 |
Water : 100 mM
Ethanol : 80 mg/mL (198.56 mM) |
生物活性 | |
靶点 |
TRPC
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In vitro(体外研究) |
SKF-96365 exhibits protective activity against MPP+ injury in PC12 cells and significantly inhibits apoptotic cell death in PC12 cells after MPP+ administration. SKF-96365 does not exert effects on necrotic cell death induced by MPP+ insult in PC12 cells. Because of its non-selective activity, SKF-96365 has been demonstrated to have effects on multiple other Ca2+ channels: it not only blocks high-voltage-activated (HVA) Ca2+ channels at typically utilized test concentrations, but also potently inhibits low-voltage -activated (LVA) T-type Ca2+ channels in HEK293 cells. The exact effect of SKF-96365 on intracellular calcium homeostasis might dependent on cell types and experimental models used.
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In vivo(体内研究) |
SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo.
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参考文献 | |
参考文献 |
[1] Singh A, et al. Br J Pharmacol. 2010, 160(6):1464-1475. [2] Chen T, et al. PLoS One. 2013, 8(1):e55601. [3] Yao H, et al. Cell Death Differ. 2009, 16(12):1681-1693. [4] Jing Z, et al. Cancer Lett. 2016, 372(2):226-38. |
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