1883549-35-6

Icerguastat (Sephin1) Carbonate, a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat Carbonate inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect[1][2][3].

Sephin 1 is an inhibitor of the regulatory subunit PPP1R15A of protein phosphatase 1. Does not bind PPP1R15B or have α2 adrenergic agonist activity. Cytoprotective in endoplasmic reticulum stressed cells in vitro. Prevents defects associated with protein misfolding in a mouse Charcot-Marie Tooth-1B model. Orally available.

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[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. DOI:10.1093/brain/awy322
[2] Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Science. 2015;348(6231):239-242. DOI:10.1126/science.aaa4484
[3] Thapa S, et al. Sephin1 Reduces Prion Infection in Prion-Infected Cells and Animal Model. Mol Neurobiol. 2020;57(5):2206-2219. DOI:10.1007/s12035-020-01880-y