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Beschreibung

A cell-permeable indole compound that acts as a potent, ATP-competitive, and isozyme-selective p38alpha MAP kinase inhibitor (IC50 = 3.2 nM). It inhibits p38beta only at much higher concentrations (IC50 = 122 nM) and exhibits little activity against p38gamma, ERK2, JNK-1, or MAPKAPK-2 even at concentrations as high as 50 µ,M. When administered to NOD mice via food intake in vivo, SD-169 is shown to prevent the development of type 1 diabetes in prediabetic mice and display therapeutic efficacy in treating animals already in mild and moderate hyperglycemic states.