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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

There are 4 reference entries for this reagent.

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References: 4 entries

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.


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References: 4 entries

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.


Add a reference