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ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK). Displays selectivity over other PIKK family enzymes (IC50 values are 0.23, 13.0, > 100 and > 100 μM for DNA-PK, PI3K, ATM and ATR respectively). Radiosensitizes both proliferating and quiescent mouse embryonic fibroblast cells to IR and inhibits DSB repair.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 281.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||35.55 mL||177.74 mL||355.48 mL|
|0.5 mM||7.11 mL||35.55 mL||71.1 mL|
|1 mM||3.55 mL||17.77 mL||35.55 mL|
|5 mM||0.71 mL||3.55 mL||7.11 mL|
References are publications that support the biological activity of the product.
Veuger et al (2003) Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-I. Cancer Res. 63 6008 PMID: 14522929
Amrein et al (2007) Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase. J.Pharmacol.Exp.Ther. 321 848 PMID: 17351105
Hollick et al (2003) 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase (DNA-PK). Bioorg.Med.Chem.Letts. 13 3083
If you know of a relevant reference for NU 7026, please let us know.
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Keywords: NU 7026, NU 7026 supplier, Selective, DNA-dependent, protein, kinases, inhibitors, inhibits, DNA-PK, NU7026, Protein, Kinase, Checkpoint, Control, Kinases, 2828, Tocris Bioscience
14 Citations for NU 7026
Citations are publications that use Tocris products. Selected citations for NU 7026 include:
Jaiswal et al (2017) ATM/Wip1 activities at chromatin control Plk1 re-activation to determine G2 checkpoint duration. EMBO J 36 2161 PMID: 28607002
Nakahara et al (2015) Activation of NF-κB by human papillomavirus 16 E1 limits E1-dependent viral replication through degradation of E1. Chembiochem 89 5040 PMID: 25717108
Yousefzadeh et al (2014) Mechanism of suppression of chromosomal instability by DNA polymerase POLQ. PLoS Genet 10 e1004654 PMID: 25275444
Tang et al (2012) Detection of early Abl kinase activation after ionizing radiation by using a peptide biosensor. J Neurosci 13 665 PMID: 22334513
Sultana et al (2013) Targeting XRCC1 deficiency in breast cancer for personalized therapy. Cancer Res 73 1621 PMID: 23253910
Petruccelli et al (2013) Expression of leukemia-associated fusion proteins increases sensitivity to histone deacetylase inhibitor-induced DNA damage and apoptosis. Mol Cancer Ther 12 1591 PMID: 23536727
Allen et al (2015) DNA Damage Response Proteins and Oxygen Modulate Prostaglandin E2 Growth Factor Release in Response to Low and High LET Ionizing Radiation. Front Oncol 5 260 PMID: 26697402
Rodgers et al (2015) Spatio-temporal regulation of RAG2 following genotoxic stress. DNA Repair (Amst) 27 19 PMID: 25625798
Fard et al (2013) The heterogenic final cell cycle of chicken retinal Lim1 horizontal cells is not regulated by the DNA damage response pathway. Cell Cycle 13 408 PMID: 24247150
Kanai et al (2012) Oncolytic virus-mediated manipulation of DNA damage responses: synergy with chemotherapy in killing glioblastoma stem cells. J Natl Cancer Inst 104 42 PMID: 22173583
Ando et al (2012) PIDD death-domain phosphorylation by ATM controls prodeath versus prosurvival PIDDosome signaling. Mol Cell 47 681 PMID: 22854598
You et al (2015) Nanoparticulate carbon black in cigarette smoke induces DNA cleavage and Th17-mediated emphysema. Elife 4 PMID: 26437452
Dolman et al (2015) DNA-Dependent Protein Kinase As Molecular Target for Radiosensitization of Neuroblastoma Cells. PLoS One 10 e0145744 PMID: 26716839
Bohgaki et al (2011) Genomic instability, defective spermatogenesis, immunodeficiency, and cancer in a mouse model of the RIDDLE syndrome. PLoS Genet 7 e1001381 PMID: 21552324
Do you know of a great paper that uses NU 7026 from Tocris? Please let us know.
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Literature in this Area
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.