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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.
Sold for research purposes under agreement from GlaxoSmithKline
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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
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Keywords: GW 843682X, GW 843682X supplier, Selective, inhibitors, inhibits, PLK1, PLK3, Mitosis, Polo-like, Kinases, GW843682X, GlaxoSmithKline, GSK, Kinase, 2977, Tocris Bioscience
9 Citations for GW 843682X
Citations are publications that use Tocris products. Selected citations for GW 843682X include:
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
Colnaghi and Wheatley (2010) Liaisons between survivin and Plk1 during cell division and cell death. Exp Cell Res 285 22592 PMID: 20427271
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
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
Waxman (2011) Characterization of kinases involved in the phosphorylation of aggregated α-synuclein. J Neurosci Res 89 231 PMID: 21162130
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
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
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Literature in this Area
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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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.