Catalog Number: 3712
Alternate Names: KU 57788
Chemical Name: 8-(4-Dibenzothienyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one
Biological Activity
Potent and selective DNA-PK inhibitor (IC50 = 14 nM). Selective for DNA-PK over a range of kinases including mTOR, PI 3-K, ATM and ATR. Potentiates the effects of doxorubicin (Cat. No. 2252) and etoposide (Cat. No. 1226) in vitro and etoposide in vivo. Also enhances CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency 2 to 3-fold, and decreases nonhomologous end-joining (NHEJ) frequency ~40%.
Technical Data
  • M.Wt:
    413.49
  • Formula:
    C25H19NO3S
  • Solubility:
    Soluble to 5 mM in DMSO with gentle warming
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    503468-95-9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia.
    Willmore et al.
    Clin.Cancer Res., 2008;14:3984
  2. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441.
    Zhao et al.
    Cancer Res., 2006;66:5354
  3. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
    Leahy et al.
    Bioorg.Med.Chem.Lett., 2004;14:6083
  4. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing.
    Robert et al.
    Genome Med., 2015;7:93
Citations:

The citations listed below are publications that use Tocris products. Selected citations for NU 7441 include:

23 Citations: Showing 1 - 10
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  1. Activation of DNA Damage Response Pathways during Lytic Replication of KSHV.
    Authors: Hollingworth Et al.
    Nucleic Acids Res 2015;7:2908
  2. Dendritic cells induce Th2-mediated airway inflammatory responses to house dust mite via DNA-dependent protein kinase.
    Authors: Mishra Et al.
    Mol Cancer Ther 2015;6:6224
  3. NSCLC cells demonstrate differential mode of cell death in response to the combined treatment of radiation and a DNA-PKcs inhibitor.
    Authors: Yu Et al.
    Oncotarget 2015;6:3848
  4. Transcriptional elongation requires DNA break-induced signalling.
    Authors: Bunch Et al.
    Invest Ophthalmol Vis Sci 2015;6:10191
  5. Cellular responses to a prolonged delay in mitosis are determined by a DNA damage response controlled by Bcl-2 family proteins.
    Authors: Colin Et al.
    Viruses 2015;5:140156
  6. Pioglitazone restores IGFBP-3 levels through DNA PK in retinal endothelial cells cultured in hyperglycemic conditions.
    Authors: Thakran Et al.
    Open Biol 2015;56:177
  7. EXO1 is critical for embryogenesis and the DNA damage response in mice with a hypomorphic Nbs1 allele.
    Authors: Rein Et al.
    Nat Commun 2015;43:7371
  8. The scaffold protein WRAP53β orchestrates the ubiquitin response critical for DNA double-strand break repair.
    Authors: Henriksson Et al.
    Genes Dev 2014;28:2726
  9. Identification of synthetic lethality of PRKDC in MYC-dependent human cancers by pooled shRNA screening.
    Authors: Zhou Et al.
    BMC Cancer 2014;14:944
  10. BRCA2 and RAD51 promote double-strand break formation and cell death in response to gemcitabine.
    Authors: Jones Et al.
    J Cell Biol 2014;13:2412
  11. Human papillomavirus episome stability is reduced by aphidicolin and controlled by DNA damage response pathways.
    Authors: Edwards Et al.
    J Virol 2013;87:3979
  12. DNA-PK phosphorylation of IGFBP-3 is required to prevent apoptosis in retinal endothelial cells cultured in high glucose.
    Authors: Zhang and Steinle
    Neurobiol Dis 2013;54:3052
  13. Senataxin, defective in the neurodegenerative disorder ataxia with oculomotor apraxia 2, lies at the interface of transcription and the DNA damage response.
    Authors: Yüce and West
    Mol Cell Biol 2013;33:406
  14. Functional intersection of ATM and DNA-dependent protein kinase catalytic subunit in coding end joining during V(D)J recombination.
    Authors: Lee Et al.
    PLoS One 2013;33:3568
  15. Ataxia telangiectasia mutated (ATM) is dispensable for endonuclease I-SceI-induced homologous recombination in mouse embryonic stem cells.
    Authors: Rass Et al.
    J Biol Chem 2013;288:7086
  16. DNA-dependent protein kinase regulates DNA end resection in concert with Mre11-Rad50-Nbs1 (MRN) and ataxia telangiectasia-mutated (ATM).
    Authors: Zhou and Paull
    J Biol Chem 2013;288:37112
  17. A new method for high-resolution imaging of Ku foci to decipher mechanisms of DNA double-strand break repair.
    Authors: Britton Et al.
    J Cell Biol 2013;202:579
  18. Targeting aberrant DNA double-strand break repair in triple-negative breast cancer with alpha-particle emitter radiolabeled anti-EGFR antibody.
    Authors: Song Et al.
    Mol Cancer Ther 2013;12:2043
  19. Functional redundancy between the XLF and DNA-PKcs DNA repair factors in V(D)J recombination and nonhomologous DNA end joining.
    Authors: Oksenych Et al.
    Nat Commun 2013;110:2234
  20. Kinase-dead ATM protein causes genomic instability and early embryonic lethality in mice.
    Authors: Yamamoto Et al.
    J Virol 2012;198:305
  21. Genomic instability, defective spermatogenesis, immunodeficiency, and cancer in a mouse model of the RIDDLE syndrome.
    Authors: Bohgaki Et al.
    PLoS Genet 2011;7:e1001381
  22. γ-Radiation promotes immunological recognition of cancer cells through increased expression of cancer-testis antigens in vitro and in vivo.
    Authors: Sharma Et al.
    Invest Ophthalmol Vis Sci 2011;6:e28217
  23. Differential effects of DNA double-strand break repair pathways on single-strand and self-complementary adeno-associated virus vector genomes.
    Authors: Cataldi and McCarty
    Mol Cell Biol 2010;84:8673
Expand to show all 23 Citations

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