SKF-96365是有效的 TRP Channel 抑制剂, 能够在结直肠癌细胞里通过引起细胞周期阻滞和凋亡,表现抗肿瘤活性。
Description | SKF-96365 hydrochloride, a potent TRP Channel blocker, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells. | ||||||||||||||||
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IC50 & Target | TRP Channel[1] | ||||||||||||||||
In Vitro | 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[1]. 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[2]. | ||||||||||||||||
In Vivo | 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[2]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : ≥ 30 mg/mL (74.46 mM) * "≥" means soluble, but saturation unknown. Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References | |
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