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 | 281.31 |
| Formula | C17H15NO3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 154447-35-5 |
| PubChem ID | 9860529 |
| InChI Key | KKTZALUTXUZPSN-UHFFFAOYSA-N |
| Smiles | O=C2C1=CC=C3C(C=CC=C3)=C1OC(N4CCOCC4)=C2 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 2.81 | 10 |
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.55 mL | 17.77 mL | 35.55 mL |
| 5 mM | 0.71 mL | 3.55 mL | 7.11 mL |
| 10 mM | 0.36 mL | 1.78 mL | 3.55 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.71 mL |
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References
References are publications that support the products' biological activity.
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 PMID:
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