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G2171

Sigma-Aldrich

GW843682X

≥98% (HPLC), solid

Synonym(s):

5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide, GW843682

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About This Item

Empirical Formula (Hill Notation):
C22H18F3N3O4S
CAS Number:
660868-91-7
Molecular Weight:
477.46
MDL number:
MFCD09971143
UNSPSC Code:
12352200
PubChem Substance ID:
329799898
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

solid

color

off-white

solubility

DMSO: >10 mg/mL

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC

InChI

1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)

InChI key

JSKUWFIZUALZLX-UHFFFAOYSA-N

Application

GW843682X has been used as a polo-like kinase-1 (PLK1) inhibitor:
  • to study the influence of PLK1 inhibition on Wee1 (G2 check point kinase), cyclin-dependent protein kinase 1 (Cdc2)–Yp15, expression in melanoma cells
  • to determine if PLK1 inhibition decreased the survival of hamartin and tuberin deficient cells
  • to investigate if inhibitors of PLK1 and aurora kinases have a synergistic antimitotic impact in HeLa cells

Biochem/physiol Actions

GW843682X is an anti-cancer compound. It can improve the ability of vincristine to promote growth arrest and apoptosis in leukemia cells. GW843682X is capable of disturbing the formation of spindles and terminate mitoses in lung adenocarcinoma cells.
GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor with nanomolar activity. It shows potent inhibition of proliferation of a wide variety of tumor cell lines.

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Timothy J Lansing et al.
Molecular cancer therapeutics, 6(2), 450-459 (2007-02-03)
Polo-like kinase 1 (PLK1) plays key roles in the regulation of mitotic progression, including mitotic entry, spindle formation, chromosome segregation, and cytokinesis. PLK1 expression and activity are strongly linked to proliferating cells. Many studies have shown that PLK1 expression is
Julio Vera et al.
Cellular signalling, 27(5), 951-960 (2015-02-17)
In the present report, the role of ATR-Chk1-Wee1 and ATM-Chk2-p53-p21 pathways in stress-induced cell cycle control is analysed in melanoma cells. Treatment of p53 wild-type melanoma cells with the genotoxic agent doxorubicin induces G2-M arrest, inhibitory phosphorylation of cell cycle
T Ikezoe et al.
Leukemia, 23(9), 1564-1576 (2009-05-08)
Polo-like kinase1 (PLK1) belongs to the family of serine/threonine kinases and plays an important role in centrosome maturation, bipolar spindle formation, and cytokinesis during mitosis. We found in this study that PLK1 was aberrantly highly expressed in a variety of
Jingjing Li et al.
Oncotarget, 6(11), 9327-9340 (2015-04-15)
Mitosis is choreographed by a number of protein kinases including polo-like kinases and Aurora kinases. As these kinases are frequently dysregulated in cancers, small-molecule inhibitors have been developed for targeted anticancer therapies. Given that PLK1 and Aurora kinases possess both
Matthildi Valianou et al.
Cell cycle (Georgetown, Tex.), 14(3), 399-407 (2015-01-08)
The mechanistic target of rapamycin complex 1 (mTORC1) increases translation, cell size and angiogenesis, and inhibits autophagy. mTORC1 is negatively regulated by hamartin and tuberin, the protein products of the tumor suppressors TSC1 and TSC2 that are mutated in Tuberous

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