PARG inhibitor PDD00031704 Inactive Small Molecule (Tool Compound)
Invented by Dr Allan Jordan at Cancer Research UK Manchester Institute
Catalogue Number | 152787 |
Antigen/Gene or Protein Targets | Poly(ADP-ribose) glycohydrolase (PARG) |
Synonyms | Poly(ADP-ribose) glycohydrolase |
Relevance | 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. |
Molecular Formula | C23H26N6O4S2 |
lUPAC | 1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(2-methylthiazol-5-yl)methyl]-2,4-dioxo-quinazoline-6-sulfonamide |
Molecular Weight (g/mol) | 514.62 |
Solubility | DMSO, MeCN, MeOH |
Research Area | Epigenetics & Nuclear Signalling |
Storage | Ambient |
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 |
Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.
Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase.
Europe PMC ID: 28254358
First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.
Europe PMC ID: 27689388
James et al. 2016. ACS Chem Biol. :. PMID: 27689388.
Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.
Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase.
First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.
James et al. 2016. ACS Chem Biol. :. PMID: 27689388.