PARG inhibitor PDD00017273 Small Molecule (Tool Compound)
Invented by Dr Allan Jordan at Cancer Research UK Manchester Institute, Dr Kate Smith at Cancer Research UK Manchester Institute
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| Catalogue Number | 152787 |
| Antigen/Gene or Protein Targets | Poly(ADP-ribose) glycohydrolase (PARG) |
| Synonyms | Poly(ADP-ribose) glycohydrolase |
| 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 |
| 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. |
| 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 |
References: 2 entries
Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.
James et al. 2016. ACS Chem Biol. :. PMID: 27689388.
Add a reference
References: 2 entries
Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.
James et al. 2016. ACS Chem Biol. :. PMID: 27689388.
Add a reference
References: 2 entries
Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.
James et al. 2016. ACS Chem Biol. :. PMID: 27689388.
Add a reference
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