Chemical Name: 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide
Biological ActivitySelective 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1.
Lansing et al.
Mol.Cancer Ther., 2007;6:450
Citations for GW 843682X
The citations listed below are publications that use Tocris products. Selected citations for GW 843682X include:
9 Citations: Showing 1 - 9
Requirement for PLK1 kinase activity in the maintenance of a robust spindle assembly checkpoint.
Authors: O'Connor Et al.
Eukaryot Cell 2015;5:42624
The Centriole Cartwheel Protein SAS-6 in Trypanosoma brucei Is Required for Probasal Body Biogenesis and Flagellum Assembly.
Authors: Hu Et al.
Cell Cycle 2015;14:898
Polo-like kinase 3 regulates CtIP during DNA double-strand break repair in G1.
Authors: Barton Et al.
J Cell Biol 2014;206:877
Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells.
Authors: Hu Et al.
PLoS One 2013;8:e78832
Characterization of kinases involved in the phosphorylation of aggregated α-synuclein.
J Neurosci Res 2011;89:231
Role of a novel coiled-coil domain-containing protein CCDC69 in regulating central spindle assembly.
Authors: Pal Et al.
J Biol Chem 2010;9:4117
Liaisons between survivin and Plk1 during cell division and cell death.
Authors: Colnaghi and Wheatley
Exp Cell Res 2010;285:22592
Targeting mitotic exit leads to tumor regression in vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ phosphatase.
Authors: Manchado Et al.
Cancer Cell 2010;18:641
Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.
Authors: Scutt Et al.
J Biol Chem 2009;284:15880
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