SKF-96365 hydrochloride

SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂，也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流，延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。

产品编号 T2170Cas号 130495-35-1

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SKF-96365 hydrochloride

产品编号 T2170别名 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑, SKF96365Cas号 130495-35-1

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规格	价格	库存
1 mg	¥ 218	现货
5 mg	¥ 498	现货
10 mg	¥ 713	现货
25 mg	¥ 1,470	现货
50 mg	¥ 2,890	现货
100 mg	¥ 4,330	现货
200 mg	¥ 6,180	现货
500 mg	¥ 9,180	现货
1 mL x 10 mM (in DMSO)	¥ 589	现货

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产品介绍

生物活性

产品描述	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.
体外活性	SKF-96365 在PC12细胞中对MPP+引起的损伤显示出保护作用，显著抑制了MPP+处理后PC12细胞的凋亡死亡，并且在PC12细胞中不影响MPP+诱导的坏死性死亡。由于其非选择性活性，SKF-96365已被证明对多种Ca2+通道有影响：它不仅能在常用测试浓度下阻断高电压激活（HVA）Ca2+通道，也能强效抑制在HEK293细胞中的低电压激活（LVA）T型Ca2+通道。SKF-96365对细胞内钙稳态的具体作用可能依赖于细胞类型和所使用的实验模型[2]。
体内活性	SKF-96365处理在体外和体内抑制了钙/钙调蛋白依赖性蛋白激酶IIγ（CaMKIIγ）/AKT信号通路[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	1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑, SKF96365

化学信息

分子量	402.91
分子式	C₂₂H₂₇ClN₂O₃
CAS No.	130495-35-1

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 60 mg/mL (148.92 mM)

H2O: 198.6 mM

溶液配制表

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.4819 mL	12.4097 mL	24.8194 mL	124.0972 mL
5 mM	0.4964 mL	2.4819 mL	4.9639 mL	24.8194 mL
10 mM	0.2482 mL	1.2410 mL	2.4819 mL	12.4097 mL
20 mM	0.1241 mL	0.6205 mL	1.2410 mL	6.2049 mL
50 mM	0.0496 mL	0.2482 mL	0.4964 mL	2.4819 mL
100 mM	0.0248 mL	0.1241 mL	0.2482 mL	1.2410 mL