中文名:Salubrinal
英文名:Salubrinal
英文別名:2-Propenamide, 3-phenyl-N-[2,2,2-trichloro-1-[[(8-quinolinylamino)thioxomethyl]amino]ethyl]-, (2E)-
純度:10mM in DMSO
貨號:S408834
包裝:1ml
Cas號:405060-95-9
存儲溫度:-80℃儲存
產(chǎn)品介紹:
Information
Salubrinal Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
In?vitro
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.
In?vivo
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.
Cell?Data
cell?lines:HCT-116 and WSU-DLCL2 cells
Concentrations:0-100 μM
Incubation?Time:48 hours
Powder?Purity:≥98%
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關鍵字: 2-Propenamide, 3-phenyl-N-[2,2,2-trichloro-1-[[(8-quinolinylamino)thioxomethyl]amino]ethyl]-, (2E)-
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