Selective inhibitor of c-Jun N-terminal kinase (JNK) (IC50
= 0.7 μ
M). Inhibits the protein-protein interaction between JNK and JIP (IC50
= 239 nM). Displays selectivity over p38 MAPK and Akt. Restores insulin sensitivity in a mouse model of type-2 diabetes.
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Design, synthesis and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-jun N-terminal kinase.
De et al.
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