DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)
Invented by Prof Bernard Golding from University of Newcastle upon Tyne , Dr Laurent Rigoreau from Cancer Research Horizons
Invented at University of Newcastle upon Tyne
- Datasheet
- References (4)
- Inventor Info
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: 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
Add a reference
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
