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Description: Potent and selective PARG inhibitor; cell permeable
Chemical Name: 1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
Purity: ≥98% (HPLC)
Biological Activity for PDD 00017273
PDD 00017273 is a potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor (IC50 = 26 nM). Exhibits >350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3. Maintains PAR chains and induces DNA double-stranded breaks in cells following DNA damage. Decreases colony formation of ZR-75-1 BRCA1 WT cells and inhibits cancer cell survival. Cell permeable.
External Portal Information for PDD 00017273
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PDD 00017273 is reviewed on the chemical probes website.
Compound Libraries for PDD 00017273
PDD 00017273 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for PDD 00017273
| M. Wt | 514.62 |
| Formula | C23H26N6O4S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1945950-21-9 |
| PubChem ID | 121398766 |
| 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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PDD 00017273
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.46 | 100 |
Preparing Stock Solutions for PDD 00017273
The following data is based on the product molecular weight 514.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.94 mL | 9.72 mL | 19.43 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.89 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets for PDD 00017273
References for PDD 00017273
References are publications that support the biological activity of the product.
James et al (2016) First-in-class chemical probes against poly(ADP-ribose) glycohydrolase (PARG) inhibit DNA repair with differential pharmacology to Olaparib. ACS Chem.Biol. 11 3179 PMID: 27689388
Gravells et al (2017) Specific killing of DNA damage-response deficient cells with inhibitor of poly(ADP-ribose) glycohydrolase. DNA Repair 52 81 PMID: 28254358
Houl et al (2019) Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death. Nat.Commun. 10 5654 PMID: 31827085
Kliza (2021) Reading ADP-ribosylation signaling using chemical biology and interaction proteomics. Mol. Cell 81 4552 PMID: 34551281
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Keywords: PDD 00017273, PDD 00017273 supplier, PDD00017273, potent, selective, PARG, poly-(ADP-ribose)-glycohydrolase, inhibits, inhibitors, DNA, repair, Poly(ADP)-ribose, Glycohydrolase, 5952, Tocris Bioscience
4 Citations for PDD 00017273
Citations are publications that use Tocris products. Selected citations for PDD 00017273 include:
Houl et al (2019) Selective Small Molecule PARG Inhibitor Causes Replication Fork Stalling and Cancer Cell Death. Nat Commun 10 5654 PMID: 31827085
Keuss et al (2019) Unanchored tri-NEDD8 inhibits PARP-1 to protect from oxidative stress-induced cell death. EMBO J 38 PMID: 30804002
Moore et al (2019) The CHD6 chromatin remodeler is an oxidative DNA damage response factor. Nat Commun 10 241 PMID: 30651562
Hanzlikova et al (2018) The Importance of Poly(ADP-Ribose) Polymerase as a Sensor of Unligated Okazaki Fragments during DNA Replication. Mol Cell 71 319 PMID: 29983321
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.