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Small Molecules (Tool Compounds)

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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Chemical structure of PDD00017273
Increasing concentrations of novel PARG inhibitor PDD00017273 prevents breakdown of PAR chains (anti-PAR antibody, shown in green). Images courtesy of Allan Jordan, University of Manchester
IC<sup>50</sup> repeated sample (N=2)
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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

References: 4 entries

Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.

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Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase.

Europe PMC ID: 28254358

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James et al. 2016. ACS Chem Biol. :. PMID: 27689388.

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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: 4 entries

Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.

View  

Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase.

Europe PMC ID: 28254358

View  

James et al. 2016. ACS Chem Biol. :. PMID: 27689388.

View  

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

Europe PMC ID: 27689388

View  

Add a reference

References: 4 entries

Gravells et al. 2017. DNA Repair (Amst). :. PMID: 28254358.

View  

Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase.

View  

James et al. 2016. ACS Chem Biol. :. PMID: 27689388.

View  

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

View  

Add a reference

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