Biochemical and cellular characterization of VRX0466617, a novel and selective inhibitor for the checkpoint kinase Chk2.

@article{Carlessi2007BiochemicalAC,
  title={Biochemical and cellular characterization of VRX0466617, a novel and selective inhibitor for the checkpoint kinase Chk2.},
  author={Luigi Carlessi and Giacomo Buscemi and Gary Larson and Zhi Hong and Jim Zhen Wu and Domenico Delia},
  journal={Molecular cancer therapeutics},
  year={2007},
  volume={6 3},
  pages={935-44}
}
VRX0466617 is a novel selective small-molecule inhibitor for Chk2 discovered through a protein kinase screening program. In this study, we provide a detailed biochemical and cellular characterization of VRX0466617. We show that VRX0466617 blocks the enzymatic activity of recombinant Chk2, as well as the ionizing radiation (IR)-induced activation of Chk2 from cells pretreated with the compound, at doses between 5 and 10 micromol/L. These doses of VRX0466617 inhibited, to some extent, the… CONTINUE READING

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