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Description

A cell-permeable, potent, specific, and nontoxic inhibitor of the DNA repair enzyme, APE1 (human apurinic/apyrimidinic endonuclease, IC50 = ~3 µ,M). 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 µ,M. 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 µ,M). 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 µ,M. 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.