Product Image

Contributor Information

  • Name Allan Jordan ; Kate Smith
  • Institute Cancer Research UK, Manchester Institute

Tool Details

  • Tool name: PARG inhibitor PDD00017273 Small Molecule (Tool Compound)
  • Alternate names: Poly(ADP-ribose) glycohydrolase
  • Molecular formula: C23H26N6O4S2
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Molecular weight of the target: 514.62
  • Description: 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.
  • Research area: Cancer
  • IUPAC: 1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(2-methylthiazol-5-yl)methyl]-2,4-dioxo-quinazoline-6-sulfonamide
  • Additional 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

  • For Research Use Only

Target Details

  • Target molecular weight: 514.62
  • Primary target: Poly(ADP-ribose) glycohydrolase (PARG)

Application Details

Handling

  • Purity: 514.62 g/mol
  • Solubility: DMSO, MeCN, MeOH
  • Storage conditions: Ambient
  • Shipping conditions: Dry Ice

Documentation

Related Tools

Product Image

Phenyl(2,4,6-trimethoxyphenyl)iodonium p-Toluenesulfonate small molecule (tool compound)

#157895
Product Image

Tetrahydrobenzodiazepine - YY3 small molecule (tool compound)

#154222
Product Image

Mitochondrial Luminophore Small Molecule (Tool Compound)

#152785

References

  • •  James et al. 2016. ACS Chem Biol. :. PMID: 27689388. Gravells et al., 2017. Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase. DNA Repair.