Icerguastat (Synonyms: Sephin1; IFB-088) |
| Katalog-Nr.GC62677 |
Icerguastat (Sephin1), ein Derivat von Guanabenz, dem die α2-adrenerge AktivitÄt fehlt, ist ein selektiver Inhibitor der regulatorischen Phosphatase-Untereinheit PPP1R15A (R15A).
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Cas No.: 951441-04-6
Sample solution is provided at 25 µL, 10mM.
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Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect[1][2][3].
Icerguastat (5 µM) prolongs eIF2α phosphorylation in oligodendrocytes under stress[1].Icerguastat (Sephin1) (selective inhibitor of a holophosphatase), safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin1 selectively binds and inhibits the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress[2].
Icerguastat (4-8 mg/kg; i.p.; daily for 35 days) delays the onset of EAE (experimental autoimmune encephalomyelitis)[1].Icerguastat (100 μg; i.p.) prolongs the survival of prion-infected mice[3].
[1]. Chen Y, et al. Sephin1, which prolongs the integrated stress response, is a promising therapeutic for multiple sclerosis. Brain. 2019;142(2):344-361.
[2]. Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Science. 2015;348(6231):239-242.
[3]. Thapa S, et al. Sephin1 Reduces Prion Infection in Prion-Infected Cells and Animal Model. Mol Neurobiol. 2020;57(5):2206-2219.
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