GW843682X
GW843682X 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). GW843682X inhibited the proliferation and induced apoptosis of 5-8F cells in a dose-dependent manner (IC50=62.5-125nmol/L). GW843682X exhibited remarkable cytotoxic effects on nasopharyngeal carcinoma 5-8F cells by down-regulating IAP gene expression, suggesting that GW843682X may become a novel therapeutic agent for nasopharyngeal carcinoma.
1: Hu Q, Chu Y, Hu W, Peng M, Song Q. The cytotoxic effect of GW843682X on nasopharyngeal carcinoma. Anticancer Agents Med Chem. 2016 May 20. [Epub ahead of print] PubMed PMID: 27198987.
2: Hu J, Wang G, Liu X, Zhou L, Jiang M, Yang L. Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. PLoS One. 2013 Oct 18;8(10):e78832. doi: 10.1371/journal.pone.0078832. eCollection 2013. PubMed PMID: 24205328; PubMed Central PMCID: PMC3799749.
3: Pezuk JA, Brassesco MS, Morales AG, de Oliveira JC, de Paula Queiroz RG, Machado HR, Carlotti CG Jr, Neder L, Scrideli CA, Tone LG. Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma. Cancer Gene Ther. 2013 Sep;20(9):499-506. doi: 10.1038/cgt.2013.46. Epub 2013 Jul 26. PubMed PMID: 23887645.
4: Brassesco MS, Pezuk JA, Morales AG, de Oliveira JC, Roberto GM, da Silva GN, Francisco de Oliveira H, Scrideli CA, Tone LG. In vitro targeting of Polo-like kinase 1 in bladder carcinoma: comparative effects of four potent inhibitors. Cancer Biol Ther. 2013 Jul;14(7):648-57. doi: 10.4161/cbt.25087. Epub 2013 May 31. PubMed PMID: 23792639; PubMed Central PMCID: PMC3742494.
5: Vazquez-Martin A, Corominas-Faja B, Oliveras-Ferraros C, Cufí S, Dalla Venezia N, Menendez JA. Serine79-phosphorylated acetyl-CoA carboxylase, a downstream target of AMPK, localizes to the mitotic spindle poles and the cytokinesis furrow. Cell Cycle. 2013 May 15;12(10):1639-41. doi: 10.4161/cc.24700. Epub 2013 Apr 19. PubMed PMID: 23603990; PubMed Central PMCID: PMC3680544.
6: Vazquez-Martin A, Cufí S, Oliveras-Ferraros C, Menendez JA. Raptor, a positive regulatory subunit of mTOR complex 1, is a novel phosphoprotein of the rDNA transcription machinery in nucleoli and chromosomal nucleolus organizer regions (NORs). Cell Cycle. 2011 Sep 15;10(18):3140-52. Epub 2011 Sep 15. PubMed PMID: 21900751.
7: Spaniol K, Boos J, Lanvers-Kaminsky C. An in-vitro evaluation of the polo-like kinase inhibitor GW843682X against paediatric malignancies. Anticancer Drugs. 2011 Jul;22(6):531-42. doi: 10.1097/CAD.0b013e3283454526. PubMed PMID: 21637161.
8: Liu XS, Liu X. Targeting Plk1 in cutaneous T-cell lymphomas (CTCLs). Cell Cycle. 2011 May 15;10(10):1523. Epub 2011 May 15. PubMed PMID: 21478668.
9: Vazquez-Martin A, Oliveras-Ferraros C, Cufí S, Menendez JA. Polo-like kinase 1 regulates activation of AMP-activated protein kinase (AMPK) at the mitotic apparatus. Cell Cycle. 2011 Apr 15;10(8):1295-302. Epub 2011 Apr 15. PubMed PMID: 21474997.
10: Nihal M, Stutz N, Schmit T, Ahmad N, Wood GS. Polo-like kinase 1 (Plk1) is expressed by cutaneous T-cell lymphomas (CTCLs), and its downregulation promotes cell cycle arrest and apoptosis. Cell Cycle. 2011 Apr 15;10(8):1303-11. Epub 2011 Apr 15. PubMed PMID: 21436619.
11: Li Z, Umeyama T, Li Z, Wang CC. Polo-like kinase guides cytokinesis in Trypanosoma brucei through an indirect means. Eukaryot Cell. 2010 May;9(5):705-16. doi: 10.1128/EC.00330-09. Epub 2010 Mar 12. PubMed PMID: 20228202; PubMed Central PMCID: PMC2863957.
12: Ikezoe T, Yang J, Nishioka C, Takezaki Y, Tasaka T, Togitani K, Koeffler HP, Yokoyama A. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. doi: 10.1038/leu.2009.94. Epub 2009 May 7. PubMed PMID: 19421227.
13: Didier C, Cavelier C, Quaranta M, Demur C, Ducommun B. Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia. Eur J Pharmacol. 2008 Sep 4;591(1-3):102-5. doi: 10.1016/j.ejphar.2008.06.062. Epub 2008 Jun 19. PubMed PMID: 18616938.
14: Lansing TJ, McConnell RT, Duckett DR, Spehar GM, Knick VB, Hassler DF, Noro N, Furuta M, Emmitte KA, Gilmer TM, Mook RA Jr, Cheung M. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol Cancer Ther. 2007 Feb;6(2):450-9. Epub 2007 Jan 31. PubMed PMID: 17267659.
2: Hu J, Wang G, Liu X, Zhou L, Jiang M, Yang L. Polo-like kinase 1 (PLK1) is involved in toll-like receptor (TLR)-mediated TNF-α production in monocytic THP-1 cells. PLoS One. 2013 Oct 18;8(10):e78832. doi: 10.1371/journal.pone.0078832. eCollection 2013. PubMed PMID: 24205328; PubMed Central PMCID: PMC3799749.
3: Pezuk JA, Brassesco MS, Morales AG, de Oliveira JC, de Paula Queiroz RG, Machado HR, Carlotti CG Jr, Neder L, Scrideli CA, Tone LG. Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma. Cancer Gene Ther. 2013 Sep;20(9):499-506. doi: 10.1038/cgt.2013.46. Epub 2013 Jul 26. PubMed PMID: 23887645.
4: Brassesco MS, Pezuk JA, Morales AG, de Oliveira JC, Roberto GM, da Silva GN, Francisco de Oliveira H, Scrideli CA, Tone LG. In vitro targeting of Polo-like kinase 1 in bladder carcinoma: comparative effects of four potent inhibitors. Cancer Biol Ther. 2013 Jul;14(7):648-57. doi: 10.4161/cbt.25087. Epub 2013 May 31. PubMed PMID: 23792639; PubMed Central PMCID: PMC3742494.
5: Vazquez-Martin A, Corominas-Faja B, Oliveras-Ferraros C, Cufí S, Dalla Venezia N, Menendez JA. Serine79-phosphorylated acetyl-CoA carboxylase, a downstream target of AMPK, localizes to the mitotic spindle poles and the cytokinesis furrow. Cell Cycle. 2013 May 15;12(10):1639-41. doi: 10.4161/cc.24700. Epub 2013 Apr 19. PubMed PMID: 23603990; PubMed Central PMCID: PMC3680544.
6: Vazquez-Martin A, Cufí S, Oliveras-Ferraros C, Menendez JA. Raptor, a positive regulatory subunit of mTOR complex 1, is a novel phosphoprotein of the rDNA transcription machinery in nucleoli and chromosomal nucleolus organizer regions (NORs). Cell Cycle. 2011 Sep 15;10(18):3140-52. Epub 2011 Sep 15. PubMed PMID: 21900751.
7: Spaniol K, Boos J, Lanvers-Kaminsky C. An in-vitro evaluation of the polo-like kinase inhibitor GW843682X against paediatric malignancies. Anticancer Drugs. 2011 Jul;22(6):531-42. doi: 10.1097/CAD.0b013e3283454526. PubMed PMID: 21637161.
8: Liu XS, Liu X. Targeting Plk1 in cutaneous T-cell lymphomas (CTCLs). Cell Cycle. 2011 May 15;10(10):1523. Epub 2011 May 15. PubMed PMID: 21478668.
9: Vazquez-Martin A, Oliveras-Ferraros C, Cufí S, Menendez JA. Polo-like kinase 1 regulates activation of AMP-activated protein kinase (AMPK) at the mitotic apparatus. Cell Cycle. 2011 Apr 15;10(8):1295-302. Epub 2011 Apr 15. PubMed PMID: 21474997.
10: Nihal M, Stutz N, Schmit T, Ahmad N, Wood GS. Polo-like kinase 1 (Plk1) is expressed by cutaneous T-cell lymphomas (CTCLs), and its downregulation promotes cell cycle arrest and apoptosis. Cell Cycle. 2011 Apr 15;10(8):1303-11. Epub 2011 Apr 15. PubMed PMID: 21436619.
11: Li Z, Umeyama T, Li Z, Wang CC. Polo-like kinase guides cytokinesis in Trypanosoma brucei through an indirect means. Eukaryot Cell. 2010 May;9(5):705-16. doi: 10.1128/EC.00330-09. Epub 2010 Mar 12. PubMed PMID: 20228202; PubMed Central PMCID: PMC2863957.
12: Ikezoe T, Yang J, Nishioka C, Takezaki Y, Tasaka T, Togitani K, Koeffler HP, Yokoyama A. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76. doi: 10.1038/leu.2009.94. Epub 2009 May 7. PubMed PMID: 19421227.
13: Didier C, Cavelier C, Quaranta M, Demur C, Ducommun B. Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia. Eur J Pharmacol. 2008 Sep 4;591(1-3):102-5. doi: 10.1016/j.ejphar.2008.06.062. Epub 2008 Jun 19. PubMed PMID: 18616938.
14: Lansing TJ, McConnell RT, Duckett DR, Spehar GM, Knick VB, Hassler DF, Noro N, Furuta M, Emmitte KA, Gilmer TM, Mook RA Jr, Cheung M. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol Cancer Ther. 2007 Feb;6(2):450-9. Epub 2007 Jan 31. PubMed PMID: 17267659.
| Chemical | |
|---|---|
| CAS Num | 660868-91-7 |
| Chemical Formula | C22H18F3N3O4S |
| Molecular Weight | 477.4582 |
| IUPAC Chemical Name | 5-(5,6-dimethoxybenzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]thiophene-2-carboxamide |
| Exact Mass | 477.097 |
| Elemental Analysis | C, 55.34; H, 3.80; F, 11.94; N, 8.80; O, 13.40; S, 6.71 |
| Synonym | GW843682X; GW 843682X; GW-843682X. |
| Solubility | Soluble in DMSO |
| SMILES Code | O=C(C1=C(OCC2=CC=CC=C2C(F)(F)F)C=C(N3C4=CC(OC)=C(OC)C=C4N=C3)S1)N |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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