PARG inhibitor PDD00017273 Small Molecule (Tool Compound)
- Name Allan Jordan ; Kate Smith
- Institute Cancer Research UK, Manchester Institute
Tool name: PARG inhibitor PDD00017273 Small Molecule (Tool Compound)
Alternate names: Poly(ADP-ribose) glycohydrolase
Molecular formula: C23H26N6O4S2
Tool type: Small molecules
Tool sub-type: Inhibitor
Molecular weight of the target: 514.62
Description: Poly(ADP ribose) glycohydrolase (PARG) has been shown to be a critical component in the repair of single strand DNA breaks. PARG counteracts the function of the ARTD family of poly(ADP ribose) polymerases, commonly known as PARPS, by efficiently catalysing the hydrolysis of O-glycosidic linkages of ADP-ribose polymer, thereby reversing the effects of PARPs. As PARG exists as a single protein, it presents an attractive target for therapeutic intervention in cancer cells with enhanced dependence upon DNA repair.
Research area: Cancer
Additional notes: PARG Biochem EC50 = 26 nM
PARG Cell EC50 = 37 nM
PARP1 Biochem EC50 > 30 uM
ARH3 Biochem EC50 > 30 uM
72h Cytotoxicity (HeLa) > 30uM
Solubility > 100 uM
- For Research Use Only
- • James et al. 2016. ACS Chem Biol. :. PMID: 27689388.
Gravells et al., 2017. Specific killing of DNA damage-response deficient cells
with inhibitors of poly(ADP-ribose) glycohydrolase. DNA Repair.