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Beschreibung

A cell-permeable benzothiazolyltetrahydrothienopyridine compound that acts as a potent, competitive, and active site targeting inhibitor of APE1 (IC50 = 2.0 microM in a fluorescence based HTS assay, and 12 .0 microM in a radiotracer incision assay). Shown to block APE1 activity in HEK293T and HeLa cells extract (IC50 = 600 nM) and increase genomic AP site accumulation. Potentiates the cytotoxicity of DNA-damaging alkylating agents in HeLa cells by ~3-fold. Exhibits favorable pharmacokinetic properties and desirable ADME attributes. Due to its lipophilic nature, it crosses the blood-brain barrier rather easily and shows desirable stability (t1/2 = 80 min).