Design and synthesis of AX4697, a bisindolylmaleimide exo-affinity probe that labels protein kinase C alpha and beta

作者：Liu Yongsheng; Wu Jiangyue; Weissig Helge; Betancort Juan M; Gai Wen Zhi; Leventhal Phillip S; Patricelli Matthew P; Samii Babak; Szardenings Anna K; Shreder Kevin R^*; Kozarich John W

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(22): 5955-5958.

DOI：10.1016/j.bmcl.2008.08.045

• AX4697
• Kinase probe
• PKC alpha
• PKC beta
• Exo-affinity label
• Bisindolylmaleimide

The synthesis and biochemical characterization of AX4697, a fluorescent, bisindolylmaleimide-derived probe for PKC alpha and beta, is described. AX4697 was able to quantify changes in PKC expression in drug-treated Jurkat cells and was shown to covalently label PKC alpha on C619, a residue that sits just outside the active site.

• 出版日期2008-11-15