Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: ~3 µM against APE1 (human apurinic/apyrimidinic endonuclease

Primary TargetAPE 1

Cell permeable: yes

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.

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.

Legal Information

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

Other Notes

Madhusudan, S., et al. 2005. Nucl. Acids Res.33, 4711.

Packaging

Packaged under inert gas

25 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: Irritant (B)