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Contributor Information

  • Name Bernard Golding ; Laurent Rigoreau
  • Institute Newcastle University

Tool Details

  • Tool name: DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)
  • Alternate names: DNA-dependent protein kinase (DNA-PK) inhibitor NU7441
  • Molecular formula: C25H19NO3S
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Molecular weight of the target: 413.49 g/mol
  • Application: NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. NU7441 increases the persistence of ÎłH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 ÎźM or 1 ÎźM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase Ρ. NU7441 increases levels of fludarabine-induced ÎłH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells.
  • Description: NU7441 is a highly potent and selective DNA-PK inhibitor.
  • Research area: Cell Signaling & Signal Transduction; DNA Damage and Repair; Epigenetics & Nuclear Signalling
  • Selectivity: Also inhibits PI3K with IC50 of 5 ÎźM in cell-free assays.
  • IC50: 14 nM

  • For Research Use Only

Target Details

  • Target molecular weight: 413.49 g/mol
  • Primary target: DNA-dependent protein kinase (DNA-PK)

Application Details

  • Application: NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. NU7441 increases the persistence of ÎłH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 ÎźM or 1 ÎźM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase Ρ. NU7441 increases levels of fludarabine-induced ÎłH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells.

Handling

  • Purity: 413.49 g/mol
  • Shipping conditions: Dry Ice

Documentation

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References

  • •  Zhao et al. 2006. Cancer Res. 66(10):5354-62. PMID: 16707462.
  • •  Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441.
  • •  Leahy et al. 2004. Bioorg Med Chem Lett. 14(24):6083-7. PMID: 15546735.
  • •  Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.