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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 Cancer Research Technology

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
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
Relevance NU7441 is a highly potent and selective DNA-PK inhibitor.

References: 2 entries

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

Leahy et al. 2004. Bioorg Med Chem Lett. 14(24):6083-7. PMID: 15546735.


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References: 2 entries

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

Leahy et al. 2004. Bioorg Med Chem Lett. 14(24):6083-7. PMID: 15546735.


Add a reference

References: 2 entries

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

Leahy et al. 2004. Bioorg Med Chem Lett. 14(24):6083-7. PMID: 15546735.


Add a reference


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