化合物Sal003 T2417

Product Introduction
Bioactivity


英文名: Sal003

描述: Sal003 是 salubrinal 的衍生物，是一种高效特异性的细胞渗透性 eIF2α 磷酸酶抑制剂。

激酶实验: Catalytic assay: MEK5 protein isolated from the baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02189. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value.

体外活性: 在大鼠中,Sal003 损伤长时记忆的形成.

体内活性: 在小鼠胚胎成纤维细胞中,Sal003通过增加eIF2a的磷酸化,引起多核糖体的解聚。Sal003通过阻断eIF2a磷酸酯酶的活性,来增加eIF2a的磷酸化；Sal003通过引起的eIF2α的磷酸化,增强由细胞毒素诱导的凋亡信号通路。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 46.3 mg/mL (100 mM)


关键字: Sal-003 | Sal 003 | Sal003 | Apoptosis | Inhibitor | inhibit | Phosphatase

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途