5-[(5-Nitro-2-thiazolyl)thio]-1,3,4-thiadiazol-2-amine (SU 3327)
• Selective inhibitor of c-Jun N-terminal kinase (JNK) (IC50 = 0.7 μM). 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
OTAVAchemicals Catalogue Number: 7070707069
CAS Registry Number: 40045-50-9
Purity: 95%+ (HPLC)
Ref.: Pellecchia et al. 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. Journal of Medicinal Chemistry (2009), 52, 1943-1952
Abstract: Comprehensive structure-activity relationship studies on a novel series of c-Jun N-terminal kinase(JNK) inhibitors is reported. The compounds are substrate competitive inhibitors that bind to the docking site of the kinase. The reported medicinal chemistry and structure-based optimizations studies resulted in the discovery of selective and potent thiadiazole JNK inhibitors that display promising in vivo activity in mouse models of insulin insensitivity.