Catalog Number: 2828
Chemical Name: 2-(4-Morpholinyl)-4H-naphthol[1,2-b]pyran-4-one
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 10 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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. Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-I.
    Veuger et al.
    Cancer Res., 2003;63:6008
  2. 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.
    Amrein et al.
    J.Pharmacol.Exp.Ther., 2007;321:848
  3. 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase (DNA-PK).
    Hollick et al.
    Bioorg.Med.Chem.Letts., 2003;13:3083
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