Poly(ADP-ribose) polymerases (PARPs) have diverse roles in cellular processes, including DNA repair and apoptosis. ABT-888 is an orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively). It enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation. ABT-888 is an orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively). It enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation. ABT-888 also acts synergistically with chemotherapies to increase the lethal effects of radiation in cancer cells.