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AdipoGen Life Sciences
PARG Inhibitor PDD00017273
80
CHF
CHF 80.00
In stock
AG-CR1-3646-M0011 mgCHF 80.00
AG-CR1-3646-M0055 mgCHF 225.00
| 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 (10mg/ml), methanol or acetonitrile (1mg/ml). |
| 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 |
Description
- 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
- 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)
- TRPM2 as a conserved gatekeeper determines the vulnerability of DA neurons by mediating ROS sensing and calcium dyshomeostasis: P. Ye, et al.; Prog. Neurobiol. ahead of print (2023)
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