626604-26-0Relevant academic research and scientific papers
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3
Zhang, Han-Cheng,Ye, Hong,Conway, Bruce R.,Derian, Claudia K.,Addo, Michael F.,Kuo, Gee-Hong,Hecker, Leonard R.,Croll, Diane R.,Li, Jian,Westover, Lori,Xu, Jun Z.,Look, Richard,Demarest, Keith T.,Andrade-Gordon, Patricia,Damiano, Bruce P.,Maryanoff, Bruce E.
, p. 3245 - 3250 (2004)
A novel series of acyclic 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides was synthesized and evaluated for activity against GSK-3β and selectivity versus PKC-βII, as well as a broad panel of protein kinases. Compounds 14 and 17c potently inhibited GSK-3β (IC50=7 and 26nM, respectively) and exhibited excellent selectivity over PKC-βII (325 and >385-fold, respectively). Compound 17c was also highly selective against 68 other protein kinases. In a cell-based functional assay, both 14 and 17c effectively increased glycogen synthase activity by inhibiting GSK-3β.
