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Design and synthesis of AX4697, a bisindolylmaleimide exo-affinity probe that labels protein kinase C alpha and beta |
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| Authors: | 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 |
| Institution: | ActivX Biosciences, 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA. |
| Abstract: | The synthesis and biochemical characterization of AX4697, a fluorescent, bisindolylmaleimide-derived probe for PKCalpha and beta, is described. AX4697 was able to quantify changes in PKC expression in drug-treated Jurkat cells and was shown to covalently label PKCalpha on C619, a residue that sits just outside the active site. |
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