Home / Polo-like Kinase Inhibitors / GW 843682X

GW 843682X

Catalog #: 2977
9 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
2977/1
2977/10
2977/50
GW 843682X | CAS No. 660868-91-7 | Polo-like Kinase Inhibitors
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Description: Selective inhibitor of PLK1 and PLK3

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

Purity: ≥98%

Product Details
Citations (9)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1.
    Lansing et al.
    Mol.Cancer Ther., 2007;6:450

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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

  1. Requirement for PLK1 kinase activity in the maintenance of a robust spindle assembly checkpoint.
    Authors: O'Connor Et al.
    Eukaryot Cell  2015;5:42624
  2. 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
  3. Polo-like kinase 3 regulates CtIP during DNA double-strand break repair in G1.
    Authors: Barton Et al.
    J Cell Biol  2014;206:877
  4. 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
  5. Characterization of kinases involved in the phosphorylation of aggregated α-synuclein.
    Authors: Waxman
    J Neurosci Res  2011;89:231
  6. 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
  7. Liaisons between survivin and Plk1 during cell division and cell death.
    Authors: Colnaghi and Wheatley
    Exp Cell Res  2010;285:22592
  8. 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
  9. 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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