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Contributor Information

  • Name Michelle Garrett
  • Institute The Institute of Cancer Research

Tool Details

  • Tool name: Chk2 inhibitor CCT241533 Small Molecule (Tool Compound)
  • Molecular formula: C23H27FN4O4
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Description: The Chk2 inhibitor CCT241533 was shown to produce a mechanistic inhibition of CHK2 in HT29 human colon cancer cells as well as a radioprotective effect in mouse thymocytes. In normal cells, p53 is activated by CHK2 and other kinases in response to double-strand DNA damage resulting in G1 cell cycle arrest and apoptosis. Inhibition of CHK2 may provide an antitumor effect in cancer cells, and therefore a therapeutic approach.
  • Research area: Cell Signaling & Signal Transduction ; Neurobiology

  • For Research Use Only

Target Details

  • Target: DNA damage response signaling enzyme checkpoint kinase 2 (CHK2)

Application Details

Handling

  • Purity: 442.48 g/mol
  • Shipping conditions: Dry Ice

Documentation

  • Available on request

References

  •   Caldwell et al. 2011. J Med Chem. 54(2):580-90. PMID: 21186793.
  •   Anderson et al. 2011. Cancer Res. 71(2):463-72. PMID: 21239475.
  •   CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.
  •   Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.