SKF-96365 hydrochloride
产品名称:SKF-96365 hydrochloride
产品描述:
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. |
体外活性 | 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[2]. |
体内活性 | SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo[4]. |
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) |
别名 | SKF96365, 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑 |
分子量 | 402.91 |
分子式 | C22H27ClN2O3 |
CAS No. | 130495-35-1 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 198.6 mM
H2O: 198.6 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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