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

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

Graphical abstractThe synthesis and biochemical characterization of AX4697, bisindolylmaleimide-derived, exo-affinity probe for PKCα and β, is described.Figure optionsDownload full-size imageDownload as PowerPoint slide