PARG Inhibitor PDD00017273
80 CHF CHF 80.00
AG-CR1-3646-M0011 mgCHF 80.00
AG-CR1-3646-M0055 mgCHF 225.00
|Synonyms||PARG Inhibitor Compound 4; 1-[(2,5-Dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(2-methylthiazol-5-yl)methyl]-2,4-dioxo-quinazoline-6-sulfonamide|
|Purity Chemicals||≥98% (HPLC)|
|Appearance||White to off-white solid.|
|Solubility||Soluble in DMSO (10mg/ml), methanol or acetonitrile (1mg/ml).|
|Identity||Determined by 1H-NMR|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Handling Advice||Keep cool and dry.|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Human poly(ADP-ribose) glycohydrolase (PARG) inhibitor for in vitro studies.
- Inhibits human recombinant PARG enzymes (IC50=26nM) and PARG in cell assays (IC50=37nM). Inactive against related glycohydrolases ARH3 and PARP1s (IC50>30µM). Showed no cytotoxicity (IC50>30µM).
- Poly(ADP ribose) glycohydrolase (PARG) is a critical component in the repair of single strand DNA breaks and therefore a target in cancer cells. PARG counteracts the function of the ARTD family of poly(ADP ribose) polymerases (known as PARPs) by efficiently catalysing the hydrolysis of O-glycosidic linkages of ADP-ribose polymer, thereby reversing the effects of PARPs.
- First-in-class chemical probes against poly(ADP-ribose) glycohydrolase (PARG) inhibit DNA repair with differential pharmacology to Olaparib: D.I. James, et al.; ACS Chem. Biol. 11, 3179 (2016)
- Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase: P. Gravells, et al.; DNA Repair 52, 81 (2017)