GW 843682X

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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% (HPLC)
Citations (9)
Literature (4)

Biological Activity 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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries for GW 843682X

GW 843682X is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GW 843682X

M. Wt 477.46
Formula C22H18F3N3O4S
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 660868-91-7
PubChem ID 9826308
Smiles O=C(N)C(S3)=C(OCC4=CC=CC=C4C(F)(F)F)C=C3N2C1=CC(OC)=C(OC)C=C1N=C2

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.

Solubility Data for GW 843682X

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 35.81 75
ethanol 2.39 5

Preparing Stock Solutions for GW 843682X

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for GW 843682X

Certificate of Analysis / Product Datasheet
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References for GW 843682X

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

If you know of a relevant reference for GW 843682X, please let us know.

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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:

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

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

Do you know of a great paper that uses GW 843682X from Tocris? Please let us know.

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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.