PARG Inhibitor PDD00017273

CHF 80.00
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Product Details
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
Product Type Chemical
Properties
Formula

C23H26N6O4S2

MW 514.6
CAS 1945950-21-9
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO, methanol or acetonitrile.
Identity Determined by 1H-NMR
InChi Key IFWUBRBMMNTBRZ-UHFFFAOYSA-N
Smiles O=C(C1=CC(S(NC2(CC2)C)(=O)=O)=CC=C1N3CC4=CC(C)=NN4C)N(CC5=CN=C(C)S5)C3=O
Shipping and Handling
Shipping AMBIENT
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.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • 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.
Product References
  1. 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)
  2. Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase: P. Gravells, et al.; DNA Repair 52, 81 (2017)
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