PDD 00017273
PDD00017273 is a potent and selective inhibitor of Poly(ADP-ribose) glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM. It catalyses hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, reversing the effects of poly(ADP-ribose) polymerases (PARPs). PDD 00017273 suppresses the ZR-75-1 cells carring BRCA1 and BRCA2 wild type, and exhibits less potent activities against MDA-MB-436 cells carry the 5396 + 1G>A mutation in BRCA1. It is used for specific killing of cells defective in certain homologous recombination (HR) proteins such as breast cancer gene 1/2 (BRCA1/2).