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Submit ReviewGW 843682X
说明： Selective inhibitor of PLK1 and PLK3
化学名： 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide
纯度： ≥98% (HPLC)
生物活性 for GW 843682X
GW 843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively). Displays > 100-fold selectivity over ~30 other kinases tested including cdk1 and cdk2. Inhibits proliferation of most tumor cells in vitro and is selective over normal diploid fibroblasts.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
化合物库 for GW 843682X
GW 843682X is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for GW 843682X
| 分子量 | 477.46 |
| 公式 | C22H18F3N3O4S |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 660868-91-7 |
| PubChem ID | 9826308 |
| InChI Key | JSKUWFIZUALZLX-UHFFFAOYSA-N |
| Smiles | O=C(N)C(S3)=C(OCC4=CC=CC=C4C(F)(F)F)C=C3N2C1=CC(OC)=C(OC)C=C1N=C2 |
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 GW 843682X
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.81 | 75 | |
| ethanol | 2.39 | 5 |
制备储备液 for GW 843682X
以下数据基于产品分子量 477.46。 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 |
|---|---|---|---|
| 0.75 mM | 2.79 mL | 13.96 mL | 27.93 mL |
| 3.75 mM | 0.56 mL | 2.79 mL | 5.59 mL |
| 7.5 mM | 0.28 mL | 1.4 mL | 2.79 mL |
| 37.5 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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产品说明书 for GW 843682X
参考文献 for GW 843682X
参考文献是支持产品生物活性的出版物。
Lansing et al (2007) In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol.Cancer Ther. 6 450 PMID: 17267659
If you know of a relevant reference for GW 843682X, please let us know.
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关键词: GW 843682X, GW 843682X supplier, Selective, inhibitors, inhibits, PLK1, PLK3, Mitosis, Polo-like, Kinases, GW843682X, GlaxoSmithKline, GSK, Kinase, 2977, Tocris Bioscience
9 篇 GW 843682X 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GW 843682X 的部分引用包括：
Waxman (2011) Characterization of kinases involved in the phosphorylation of aggregated α-synuclein. J Neurosci Res 89 231 PMID: 21162130
Scutt et al (2009) Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks. J Biol Chem 284 15880 PMID: 19359241
Hu et al (2013) Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. PLoS One 8 e78832 PMID: 24205328
Colnaghi and Wheatley (2010) Liaisons between survivin and Plk1 during cell division and cell death. Exp Cell Res 285 22592 PMID: 20427271
Pal et al (2010) Role of a novel coiled-coil domain-containing protein CCDC69 in regulating central spindle assembly. J Biol Chem 9 4117 PMID: 20962590
O'Connor et al (2015) Requirement for PLK1 kinase activity in the maintenance of a robust spindle assembly checkpoint. Eukaryot Cell 5 42624 PMID: 26685311
Hu et al (2015) The Centriole Cartwheel Protein SAS-6 in Trypanosoma brucei Is Required for Probasal Body Biogenesis and Flagellum Assembly. Cell Cycle 14 898 PMID: 26116214
Barton et al (2014) Polo-like kinase 3 regulates CtIP during DNA double-strand break repair in G1. J Cell Biol 206 877 PMID: 25267294
Manchado et al (2010) Targeting mitotic exit leads to tumor regression in vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ phosphatase. Cancer Cell 18 641 PMID: 21156286
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.