Home / DNA-dependent Protein Kinase Inhibitors / NU 7441

NU 7441

Catalog #: 3712
54 Citations Datasheet
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3712/50
NU 7441 | CAS No. 503468-95-9 | DNA-dependent Protein Kinase Inhibitors
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Description: Potent and selective DNA-PK inhibitor
Alternative Names: KU 57788

Chemical Name: 8-(4-Dibenzothienyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one

Purity: ≥99%

Product Details
Citations (54)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

NU 7441 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Replication of an Autonomous Human Parvovirus in Non-dividing Human Airway Epithelium Is Facilitated through the DNA Damage and Repair Pathways.
    Deng X, Yan Z, Cheng F, Engelhardt J, Qiu J
    PLoS Pathog, 2016;12(1):e1005399.
  2. Dendritic cells induce Th2-mediated airway inflammatory responses to house dust mite via DNA-dependent protein kinase.
    Mishra, Amarjit, Brown, Alexandr, Yao, Xianglan, Yang, Shutong, Park, Sung-Jun, Liu, Chengyu, Dagur, Pradeep, McCoy, J Philip, Keeran, Karen J, Nugent, Gayle Z, Jeffries, Kenneth, Qu, Xuan, Yu, Zu-Xi, Levine, Stewart, Chung, Jay H
    Nat Commun, 2015;6(0):6224.
  3. Chloroquine or Chloroquine-PI3K/Akt Pathway Inhibitor Combinations Strongly Promote gamma-Irradiation-Induced Cell Death in Primary Stem-Like Glioma Cells.
    Firat E, Weyerbrock A, Gaedicke S, Grosu A, Niedermann G
    PLoS ONE, 2012;7(10):e47357.
  4. Mitotic progression following DNA damage enables pattern recognition within micronuclei
    SM Harding, JL Benci, J Irianto, DE Discher, AJ Minn, RA Greenberg
    Nature, 2017;0(0):.
  5. DNA-dependent protein kinase regulates DNA end resection in concert with Mre11-Rad50-Nbs1 (MRN) and ataxia telangiectasia-mutated (ATM).
    Zhou, Yi, Paull, Tanya T
    J Biol Chem, 2013;288(52):37112-25.
  6. The scaffold protein WRAP53beta orchestrates the ubiquitin response critical for DNA double-strand break repair.
    Henriksson S, Rassoolzadeh H, Hedstrom E, Coucoravas C, Julner A, Goldstein M, Imreh G, Zhivotovsky B, Kastan M, Helleday T, Farnebo M
    Genes Dev, 2014;28(24):2726-38.
  7. DEK is required for homologous recombination repair of DNA breaks
    EA Smith, B Gole, NA Willis, R Soria, LM Starnes, EF Krumpelbec, AG Jegga, AM Ali, H Guo, AR Meetei, PR Andreassen, F Kappes, LM Vinnedge, JA Daniel, R Scully, L Wiesmüller, SI Wells
    Sci Rep, 2017;7(0):44662.
  8. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing.
    Robert et al.
    Genome Med., 2015;7:93
  9. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441.
    Zhao et al.
    Cancer Res., 2006;66:5354
  10. 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
  11. 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

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Citations for NU 7441

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

54 Citations: Showing 1 - 10

  1. Ku-DNA binding inhibitors modulate the DNA damage response in response to DNA double-strand breaks.
    Authors: Joseph R Et al.
    NAR Cancer  2023;5:zcad003
  2. DNA damage repair kinase DNA-PK and cGAS synergize to induce cancer-related inflammation in glioblastoma.
    Authors: Min Sup Et al.
    EMBO J  2023;42:e111961
  3. Dynamics and competition of CRISPR-Cas9 ribonucleoproteins and AAV donor-mediated NHEJ, MMEJ and HDR editing.
    Authors: Lei Et al.
    Nucleic Acids Res  2021;49:969-985
  4. Pathological mutations in PNKP trigger defects in DNA single-strand break repair but not DNA double-strand break repair.
    Authors: Keith W Et al.
    Nucleic Acids Res  2020;48:6672-6684
  5. Oxidative DNA damage is concurrently repaired by base excision repair (BER) and apyrimidinic endonuclease 1 (APE1)-initiated nonhomologous end joining (NHEJ) in cortical neurons.
    Authors: S-D Et al.
    Neuropathol Appl Neurobiol  2020;46:375-390
  6. Synergistic gene editing in human iPS cells via cell cycle and DNA repair modulation.
    Authors: Thomas L Et al.
    Nat Commun  2020;11:2876
  7. Combining PARP and DNA-PK Inhibitors With Irradiation Inhibits HPV-Negative Head and Neck Cancer Squamous Carcinoma Growth.
    Authors: Markus Et al.
    Front Genet  2020;11:1036
  8. Oocytes can efficiently repair DNA double-strand breaks to restore genetic integrity and protect offspring health.
    Authors: Jessica M Et al.
    Proc Natl Acad Sci U S A  2020;117:11513-11522
  9. TOP2β-Dependent Nuclear DNA Damage Shapes Extracellular Growth Factor Responses via Dynamic AKT Phosphorylation to Control Virus Latency.
    Authors: Lora A Et al.
    Mol Cell  2019;74:466-480.e4
  10. FUS (fused in sarcoma) is a component of the cellular response to topoisomerase I-induced DNA breakage and transcriptional stress.
    Authors: Martínez-Macías Et al.
    Life Sci Alliance  2019;2
  11. mEAK-7 Forms an Alternative mTOR Complex with DNA-PKcs in Human Cancer.
    Authors: Nguyen Et al.
    iScience  2019;17:190
  12. ATM orchestrates the DNA-damage response to counter toxic non-homologous end-joining at broken replication forks.
    Authors: Balmus Et al.
    Nat Commun  2019;10:87
  13. Impaired DNA damage response signaling by FUS-NLS mutations leads to neurodegeneration and FUS aggregate formation.
    Authors: Naumann Et al.
    Nat Commun  2018;9:335
  14. The ATM and Rad3-Related (ATR) Protein Kinase Pathway Is Activated by Herpes Simplex Virus 1 and Required for Efficient Viral Replication.
    Authors: Edwards Et al.
    J Virol  2018;92
  15. In cellulo phosphorylation of DNA double-strand break repair protein XRCC4 on Ser260 by DNA-PK.
    Authors: Moghani Et al.
    J Radiat Res  2018;59:700
  16. Tissue-selective effects of nucleolar stress and rDNA damage in developmental disorders.
    Authors: Calo Et al.
    Nature  2018;554:112
  17. DNA Double-Strand Break Resection Occurs during Non-homologous End Joining in G1 but Is Distinct from Resection during Homologous Recombination.
    Authors: Biehs Et al.
    Mol Cell  2017;65:671
  18. Regulation of human polλ by ATM-mediated phosphorylation during non-homologous end joining.
    Authors: Dale A Et al.
    DNA Repair (Amst)  2017;51:31-45
  19. Ionizing radiation response of primary normal human lens epithelial cells.
    Authors: Hamada
    PLoS One  2017;12:e0181530
  20. DNA-PK triggers histone ubiquitination and signaling in response to DNA double-strand breaks produced during the repair of transcription-blocking topoisomerase I lesions.
    Authors: Cristini Et al.
    Nucleic Acids Res  2016;44:1161
  21. A novel cytoprotective function for the DNA repair protein Ku in regulating p53 mRNA translation and function.
    Authors: Lamaa Et al.
    EMBO Rep  2016;17:508
  22. Replication of an Autonomous Human Parvovirus in Non-dividing Human Airway Epithelium Is Facilitated through the DNA Damage and Repair Pathways.
    Authors: Deng Et al.
    PLoS Pathog  2016;12:e1005399
  23. Activation of DNA Damage Response Pathways during Lytic Replication of KSHV.
    Authors: Hollingworth Et al.
    Nucleic Acids Res  2015;7:2908
  24. 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
  25. 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
  26. Transcriptional elongation requires DNA break-induced signalling.
    Authors: Bunch Et al.
    Invest Ophthalmol Vis Sci  2015;6:10191
  27. 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
  28. 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
  29. 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
  30. Requirement for Parp-1 and DNA ligases 1 or 3 but not of Xrcc1 in chromosomal translocation formation by backup end joining.
    Authors: Soni Et al.
    Nucleic Acids Res  2014;42:6380
  31. The scaffold protein WRAP53β orchestrates the ubiquitin response critical for DNA double-strand break repair.
    Authors: Henriksson Et al.
    Genes Dev  2014;28:2726
  32. Identification of synthetic lethality of PRKDC in MYC-dependent human cancers by pooled shRNA screening.
    Authors: Zhou Et al.
    BMC Cancer  2014;14:944
  33. BRCA2 and RAD51 promote double-strand break formation and cell death in response to gemcit.
    Authors: Jones Et al.
    J Cell Biol  2014;13:2412
  34. Hypoxic stress facilitates acute activation and chronic downregulation of fanconi anemia proteins.
    Authors: Scanlon and Glazer
    Mol Cancer Res  2014;12:1016
  35. Repair of DNA strand breaks in a minichromosome in vivo: kinetics, modeling, and effects of inhibitors.
    Authors: Ronald Et al.
    PLoS One  2013;8:e52966
  36. Human papillomavirus episome stability is reduced by aphidicolin and controlled by DNA damage response pathways.
    Authors: Edwards Et al.
    J Virol  2013;87:3979
  37. Targeting XRCC1 deficiency in breast cancer for personalized therapy.
    Authors: Sultana Et al.
    Cancer Res  2013;73:1621
  38. Stathmin regulates mutant p53 stability and transcriptional activity in ovarian cancer.
    Authors: Sonego Et al.
    EMBO Mol Med  2013;5:707
  39. 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
  40. 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
  41. 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
  42. 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
  43. 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
  44. 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
  45. 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
  46. 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
  47. Unmodified histone H3K4 and DNA-dependent protein kinase recruit autoimmune regulator to target genes.
    Authors: B Matija Et al.
    Mol Cell Biol  2012;32:1354-62
  48. Targeting protein for xenopus kinesin-like protein 2 (TPX2) regulates γ-histone 2AX (γ-H2AX) levels upon ionizing radiation.
    Authors: Neumayer Et al.
    J Biol Chem  2012;287:42206
  49. Kinase-dead ATM protein causes genomic instability and early embryonic lethality in mice.
    Authors: Yamamoto Et al.
    J Virol  2012;198:305
  50. Synthetic lethal targeting of DNA double-strand break repair deficient cells by human apurinic/apyrimidinic endonuclease inhibitors.
    Authors: Sultana Et al.
    Int J Cancer  2012;131:2433
  51. Parvovirus B19 infection of human primary erythroid progenitor cells triggers ATR-Chk1 signaling, which promotes B19 virus replication.
    Authors: Luo Et al.
    J Virol  2011;85:8046
  52. Genomic instability, defective spermatogenesis, immunodeficiency, and cancer in a mouse model of the RIDDLE syndrome.
    Authors: Bohgaki Et al.
    PLoS Genet  2011;7:e1001381
  53. 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
  54. 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

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