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抑制剂描述:

产品名称:Salubrinal

产品别名:见爱必信官网

英文别名:Salubrinal

靶点:Phosphatase;Autophagy

CAS:405060-95-9

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Salubrinal是一种选择性的eIF2α 脱磷酸作用抑制剂,可以抑制ER应激介导的细胞凋亡,EC50约为15 μM。

溶解性:DMSO : 48 mg/mL (100 mM)

体外研究:

Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Salubrinal inhibited ER stress-mediated apoptosis induced by the protein glycosylation inhibitor tunicamycin (Tm) in a dose-dependent manner, with a median effective concentration (EC50) ～ 15 μM. Salubrinal also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress. However, Salubrinal is not a general apoptosis inhibitor. Salubrinal induced rapid and robust eIF2α phosphorylation and its downstream effects in PC12 cells, including down-regulation of cyclin D1 and up-regulation of GADD34 and CHOP, two proteins whose expression is induced by eIF2α phosphorylation. Salubrinal inhibits eIF2α dephosphorylation by inhibiting the PP1/GADD34 complex. Salubrinal inhibits HSV replication with IC50 of ~ 3μM by inhibiting eIF2α dephosphorylation. Salubrinal increased non-rapid eye movement (NREM) sleep.

体内研究:Salubrinal inhibits HSV replication in a mouse cornea infection model. Compared to vehicle control, topical Salubrinal treatment significantly reduced the viral titer recovered from eye swabs of infected animals. I.C.V. administration of Salubrinal significantly modified the homeostatic sleep response.

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