DNA-PK inhibitor II, a cell-permeable compound, is shown to be a potent inhibitor of DNA repair enzymes. DNA-PK inhibition makes it potentially possible to make cell lines become more sensitive to ionizing radiation (IR) and a reduction of lethal damage r
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of protein kinase; DNA-activated; catalytic subunit
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 μM, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. An antiproliferative agent, and inhibitor of DNA-PK.
1.Veuger SJ, Curtin NJ, Richardson CJ, Smith GC, Durkacz BW. (2003) Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1.. Cancer Res, 63 (18):(6008-15). [PMID:14522929]
2.Willmore E, de Caux S, Sunter NJ, Tilby MJ, Jackson GH, Austin CA, Durkacz BW. (2004) A novel DNA-dependent protein kinase inhibitor, NU7026, potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia.. Blood, 103 (12):(4659-65). [PMID:15010369]
3.Leahy JJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GC. (2004) Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.. Bioorg Med Chem Lett, 14 (24):(6083-7). [PMID:15546735]
4.Smith GC, Jackson SP. (1999) The DNA-dependent protein kinase.. Genes Dev, 13 (8):(916-34). [PMID:10215620]
5.Kodama M, Murakami M, Kodama T. (1997) Differential implications of the oncogene-tumor suppressor gene complex in the geneses of 19 human neoplasias. Evidence in support of the steroid carcinogenesis hypothesis.. Anticancer Res, 17 (3C):(2285-92). [PMID:9216703]
6.Rosenzweig KE, Youmell MB, Palayoor ST, Price BD. (1997) Radiosensitization of human tumor cells by the phosphatidylinositol3-kinase inhibitors wortmannin and LY294002 correlates with inhibition of DNA-dependent protein kinase and prolonged G2-M delay.. Clin Cancer Res, 3 (7):(1149-56). [PMID:9815794]
7.Brustel J et al.. (2018) Large XPF-dependent deletions following misrepair of a DNA double strand break are prevented by the RNA:DNA helicase Senataxin.. Sci Rep, 8 (3850). [PMID:29497062]
8.Wakasugi M et al.. (2014) Nucleotide excision repair-dependent DNA double-strand break formation and ATM signaling activation in mammalian quiescent cells.. J Biol Chem, 289 (41):(28730-7). [PMID:25164823]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
G1524090