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SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride 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 hydrochloride 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 hydrochloride inhibited hERG current in a concentration-dependent manner.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $52 | In Stock | |
10 mg | $78 | In Stock | |
25 mg | $141 | In Stock | |
50 mg | $255 | In Stock | |
100 mg | $495 | In Stock | |
200 mg | $755 | In Stock | |
500 mg | $1,170 | In Stock | |
1 mL x 10 mM (in DMSO) | $57 | In Stock |
Description | SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride 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 hydrochloride 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 hydrochloride inhibited hERG current in a concentration-dependent manner. |
In vitro | 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]. |
In vivo | SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo[4]. |
Cell Research | 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) |
Alias | SKF96365 |
Molecular Weight | 402.91 |
Formula | C22H27ClN2O3 |
Cas No. | 130495-35-1 |
Smiles | Cl.COc1ccc(CCCOC(Cn2ccnc2)c2ccc(OC)cc2)cc1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (148.92 mM) H2O: 198.6 mM | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/H2O
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