Merck, 262015-25MG, DNA Base Excision Repair Pathway Inhibitor

General description
A cell-permeable, potent, specific, and nontoxic inhibitor of the DNA repair enzyme, APE1 (human apurinic/apyrimidinic endonuclease; IC₅₀ = ~3 µM). Shown to target the APE1 active site and inhibit its 3′-phosphodiesterase and 3′-phosphatase activities. Exhibits minimal effects on endonuclease IV, BamH1 restriction endonuclease, or topoisomerase I even at concentration as high as 100 µM. Also shown to potentiate the cytotoxicity of several DNA damaging agents, such as MMS, temozolomide, Zeocin, and H₂O₂ in HeLa, HT1080, and MDA-MB-231 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
APE 1
Product does not compete with ATP.
Reversible: no
Target IC₅₀: ~3 µM against APE1 (human apurinic/apyrimidinic endonuclease
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Madhusudan, S., et al. 2005. Nucl. Acids Res.33, 4711.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)