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Description

A cell permeable alkylidene barbiturate analog that acts as a potent and specific inhibitor of tyrosyl-DNA phosphodiesterase 1 (Tdp1, IC50 = 710 nM) and increases the number of g-H2AX foci in MCF-7 cells. Shown to sensitize MCF-7 cells to camptothecin (CPT), increase DNA breaks, and reduce cell proliferation. However, it does not affect the viability of normal mammary epithelial cells up to 10 µ,M levels. Synergistically reduces cell proliferation and induces apoptosis in MCF-7 cells when combined with Rucaparib, a PARP-1 inhibitor.