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Submit ReviewPDD 00017273
说明： Potent and selective PARG inhibitor; cell permeable
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for PDD 00017273
PDD 00017273 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PDD 00017273
| 分子量 | 514.62 |
| 公式 | C23H26N6O4S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PDD 00017273
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 51.46 | 100 |
制备储备液 for PDD 00017273
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for PDD 00017273
参考文献 for PDD 00017273
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for PDD 00017273, please let us know.
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关键词: 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 篇 PDD 00017273 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PDD 00017273 的部分引用包括：
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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