PDD00017272 is a potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with an EC50 of 4.8 nM. By inhibiting PARG activity, this compound promotes the accumulation of poly(ADP-ribose) (pADPr) on chromatin, thereby disrupting DNA damage repair and replication processes, leading to PARP1/2-dependent cytotoxicity. PDD00017272 is particularly valuable for research applications involving cancer models with DNA repair deficiencies, such as those characterized by BRCA mutations, and demonstrates enhanced efficacy in tumor cells exhibiting lower PARG expression.
PDD00017272 is a potent inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with an EC50 of 4.8 nM. By inhibiting PARG activity, this compound promotes the accumulation of poly(ADP-ribose) (pADPr) on chromatin, thereby disrupting DNA damage repair and replication processes, leading to PARP1/2-dependent cytotoxicity. PDD00017272 is particularly valuable for research applications involving cancer models with DNA repair deficiencies, such as those characterized by BRCA mutations, and demonstrates enhanced efficacy in tumor cells exhibiting lower PARG expression.
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