GW 843682X

Cat. No. 2977

GW 843682X C22H18F3N3O4S [660868-91-7]

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Chemical Name: 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
477.46
Formula:
C22H18F3N3O4S
Solubility:
Soluble to 75 mM in DMSO and to 5 mM in ethanol
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
660868-91-7

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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 this product please let us know.

Citations are publications that use Tocris products. Selected citations for GW 843682X include:

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.

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.

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.

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.

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.

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.

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.

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Keywords: GW 843682X, supplier, Selective, inhibitors, inhibits, PLK1, PLK3, Mitosis, Polo-like, Kinases, GW843682X, GlaxoSmithKline, GSK, Tocris Bioscience, Polo-like Kinase Inhibitor products

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