生物活性 | |||
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描述 | Icerguastat, also known as Sephin1, is a Guanabenz derivative that lacks α2-adrenergic activity and is a selective inhibitor of PPP1R15A (R15A). Icerguastat inhibits the dephosphorylation of eIF2α, thereby prolonging the protective response. Icerguastat has antiphospholipid effects[1][2][3].At a concentration of 5 μM, Icerguastat prolongs eIF2α phosphorylation in oligodendrocytes under stress[1].Icerguastat selectively binds and inhibits stress-induced PPP1R15A, but not the associated constitutive PPP1R15B, thereby prolonging the action of the adaptive phosphorylation signalling pathway and protecting cells from lethal protein misfolding stress[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
5.09mL 1.02mL 0.51mL |
25.43mL 5.09mL 2.54mL |
50.85mL 10.17mL 5.09mL |