Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetDNA-PK activity

Target IC₅₀: 15 µM against DNA-PK (DNA-dependent protein kinase) activity

Cell permeable: yes

General description

A cell-permeable vanillin derivative that acts as a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK) activity (IC₅₀ = 15 µM) and DNA-PK-mediated double strand break (DSB) DNA repair by non-homologous DNA-end-joining (NHEJ). Reported to effectively sensitize cells to Cisplatin (Cat. No. 232120). Does not affect the activities of PKC or Chk2.

A cell-permeable vanillin derivative that acts as a potent and selective inhibitor of DNA-PK (DNA-dependent protein kinase) activity (IC₅₀ = 15 µM) and DNA-PK-mediated DSB (double strand break) DNA repair by NHEJ (non-homologous DNA-end-joining). Shown to effectively sensitize cells to killing by Cisplatin (Cat. No. 232120). Does not affect PKC or Chk2 kinase activities.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Willmore, E., et al. 2004. Blood,103, 4659.Durant, S., and Karran, P. 2003. Nucleic Acids Res.31, 5501.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)