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[1][2].
Molekulargewicht:
531.67
Reinheit:
99.47
CAS Nummer:
[1945950-20-8]
Formel:
C23H25N5O4S3
Target-Kategorie:
Poly(ADP-ribose) Glycohydrolase (PARG)
Anwendungsbeschreibung:
MCE Product type: Reference compound
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
