A cell-permeable benzothiazolyltetrahydrothienopyridine compound that acts as a potent, competitive, and active site targeting inhibitor of APE1 (IC50=2.0uM in a fluorescence based HTS assay; and 12uM in a radiotracer incision assay). Shown to block APE1 activity in HEK293T and HeLa cells extract (IC50=600nM) 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=80min).
Formula:C19H21N3OS2
Molecular Weight:371.5
Solubility:DMSO (2.5mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.