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PARG inhibitor PDD00031704 Inactive Small Molecule (Tool Compound)

Invented by Dr Allan Jordan at Cancer Research UK Manchester Institute, Dr Kate Smith at Cancer Research UK Manchester Institute

Info

Catalogue Number 153580
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.

Methylation of the sulphonamide moiety of the PARG Inhibitor PDD00017273 was found to disrupt PARG-binding interactions, rendering the compound inactive and providing useful controls to demonstrate on-target pharmacology of the active compound.
On Target IC50 >100┬ÁM (PARG)
Molecular Formula C24H28N6O4S2
Molecular Weight (g/mol) 528.16
Research Area Cancer, Epigenetics & Nuclear Signalling
Storage Ambient
Notes N-methylated analogs of the PARG tool compounds are inactive.

References

There are 2 reference entries for this reagent.

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References: 2 entries

James et al. 2016. ACS Chem Biol. 11(11):3179-3190. PMID: 27689388.

First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.

Europe PMC ID: 27689388


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References: 2 entries

James et al. 2016. ACS Chem Biol. 11(11):3179-3190. PMID: 27689388.

First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.


Add a reference