GW 843682X

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Cat.No. 2977 - GW 843682X | C22H18F3N3O4S | CAS No. 660868-91-7
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)
Datasheet
Citations (8)
Reviews
Literature

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

Compound Libraries

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

Technical Data

M. Wt 477.46
Formula C22H18F3N3O4S
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 660868-91-7
PubChem ID 9826308
InChI Key JSKUWFIZUALZLX-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.09 mL 10.47 mL 20.94 mL
5 mM 0.42 mL 2.09 mL 4.19 mL
10 mM 0.21 mL 1.05 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Selective, inhibitors, inhibits, PLK1, PLK3, Mitosis, Polo-like, Kinases, GW843682X, GlaxoSmithKline, GSK, Polo-like, Kinase, Mitosis, Polo-like, Kinase, Tocris Bioscience

8 Citations for GW 843682X

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

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

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

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

Colnaghi and Wheatley (2010) Liaisons between survivin and Plk1 during cell division and cell death. Exp Cell Res 285 22592 PMID: 20427271

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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Cell Cycle & DNA Damage Repair

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.