GW 843682X

Name: GW 843682X
Brand: Tocris Bioscience
SKU: 2977

Catalog # 2977 | Tocris Bioscience a Bio-Techne Brand

Citations (9)

COA / SDS

Selective inhibitor of PLK1 and PLK3

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Key Product Details

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)
Molecular Weight:	477.46

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Technical Data
Citations (9) / Reviews

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
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.

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

Solubility for GW 843682X

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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	1.40 mL	2.79 mL
37.5 mM	0.06 mL	0.28 mL	0.56 mL

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References for GW 843682X

References are publications that support the biological activity of the product.

Lansing In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol.Cancer Ther. 2007 PMID: 17267659

Citations for GW 843682X (9)

Showing 1 - 9 of 9 citations Showing All

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Citations are publications that use Bio-Techne 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
Waxman (2011) Characterization of kinases involved in the phosphorylation of aggregated α-synuclein. J Neurosci Res. 89:231
PMID: 21162130
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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