General description
Cell-permeable, selective and potent inhibitor of the FEN-1 and a chemopotentiator.
Fen1-IN-1 is a cell-permeable N-hydroxyimide compound that potently and selectively inhibits FEN-1 (Flap endonuclease 1) (IC50 = 11 nM), a divalent metal-dependent nuclear enzyme with the ability to cleave the 5′ overhang of branched dsDNA. FEN1-IN-1 minimally affects the activity of a related endonuclease xeroderma pigmentosum G (XPG; IC50 = 292 nM). Dose-dependently potentiates methyl methanesulfonate (MMS) and temozolomide-induced DNA damages in T24 bladder carcinoma cells. 20 µM of Fen1i is shown to suppress the proliferation, migration, and invasion of tumor cells.