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DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)

Invented by Prof Bernard Golding at University of Newcastle upon Tyne Dr Laurent Rigoreau at University of Newcastle upon Tyne

Info

Catalogue Number 151889
Antigen/Gene or Protein Targets DNA-dependent protein kinase (DNA-PK)
Synonyms DNA-dependent protein kinase (DNA-PK) inhibitor NU7441
Type Inhibitor
Relevance NU7441 is a highly potent and selective DNA-PK inhibitor.
On Target IC50 14 nM
Selectivity Also inhibits PI3K with IC50 of 5 μM in cell-free assays.
Molecular Formula C25H19NO3S
Molecular Weight (g/mol) 413.49 g/mol
In vivo applications 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.
In vitro applications NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 μM or 1 μM) 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 η. NU7441 increases levels of fludarabine-induced γH2AX 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.
Research Area DNA Damage and Repair, Epigenetics & Nuclear Signalling

References

There are 4 reference entries for this reagent.

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References: 4 entries

Zhao et al. 2006. Cancer Res. 66(10):5354-62. PMID: 16707462.

Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441.

Europe PMC ID: 16707462

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.

Europe PMC ID: 15546735


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References: 4 entries

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.


Add a reference