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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
18 Citations for PDD 00017273
Citations are publications that use Tocris products. Selected citations for PDD 00017273 include:
Jian et al (2020) Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics 10 6530-6543 PMID: 32483468
Yanyuan et al (2020) Transcriptional Regulation of CCL2 by PARP1 Is a Driver for Invasiveness in Breast Cancer. Cancers (Basel) 12 PMID: 32455851
Keith W et al (2020) Pathological mutations in PNKP trigger defects in DNA single-strand break repair but not DNA double-strand break repair. Nucleic Acids Res 48 6672-6684 PMID: 32504494
Marco et al (2020) The Ubiquitin Ligase TRIP12 Limits PARP1 Trapping and Constrains PARP Inhibitor Efficiency. Cell Rep 32 107985 PMID: 32755579
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
Jiri et al (2021) Loss of nuclear DNA ligase III reverts PARP inhibitor resistance in BRCA1/53BP1 double-deficient cells by exposing ssDNA gaps. Mol Cell 81 4692-4708.e9 PMID: 34555355
Keith W et al (2021) XRCC1 prevents toxic PARP1 trapping during DNA base excision repair. Mol Cell 81 3018-3030.e5 PMID: 34102106
Amber et al (2021) Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents. Front Oncol 11 745981 PMID: 34778062
Rachel et al (2021) CDKL5 kinase controls transcription-coupled responses to DNA damage. EMBO J 40 e108271 PMID: 34605059
Mai et al (2021) NAD+ bioavailability mediates PARG inhibition-induced replication arrest, intra S-phase checkpoint and apoptosis in glioma stem cells. NAR Cancer 3 zcab044 PMID: 34806016
Mark T et al (2021) CARM1 regulates replication fork speed and stress response by stimulating PARP1. Mol Cell 81 784-800.e8 PMID: 33412112
Keuss et al (2019) Unanchored tri-NEDD8 inhibits PARP-1 to protect from oxidative stress-induced cell death. EMBO J 38 PMID: 30804002
Yoshinari et al (2019) ELTA: Enzymatic Labeling of Terminal ADP-Ribose. Mol Cell 73 845-856.e5 PMID: 30712989
Houl et al (2019) Selective Small Molecule PARG Inhibitor Causes Replication Fork Stalling and Cancer Cell Death. Nat Commun 10 5654 PMID: 31827085
Margarita et al (2022) PARP inhibition impedes the maturation of nascent DNA strands during DNA replication. Nat Struct Mol Biol 29 329-338 PMID: 35332322
Pierre-Olivier et al (2022) Poly ADP-ribosylation of SET8 leads to aberrant H4K20 methylation in mammalian nuclear genome. Commun Biol 5 1292 PMID: 36434141
Matthias et al (2022) MDM2 binds and ubiquitinates PARP1 to enhance DNA replication fork progression. Cell Rep 39 110879 PMID: 35649362
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Epigenetics in Cancer Poster
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.