PDD00017272

Description

PDD00017272 is an inhibitor of poly ADP-ribose glycohydrolase PARG EC50=4.8 nM and an activator of PARP1/2. PDD00017272 inhibits its activity of hydrolyzing poly ADP-ribose pADPr , resulting in the accumulation of pADPr on chromatin, interfering with DNA damage repair and replication processes, and inducing PARP1/2-dependent cytotoxicity. PDD00017272 can be used in cancer models with DNA repair defects such as BRCA mutations or resistance to PARP inhibitors. PDD00017272 has a PARG expression level-correlated inhibitory potency with EC50 of 9.2 nM PARG cells , the tumor cells with lower PARG expression are more sensitive.