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Description: GW843682X is a novel, potent, selective, ATP-competitive inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) with IC50s of 2.2 nM and 9.1 nM, respectively. It is more than 100-fold selective against ?30 other kinases. 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.
References: Mol Cancer Ther. 2007 Feb; 6(2):450-9. Epub 2007 Jan 31.; Eur J Pharmacol. 2008 Sep 4; 591(1-3):102-5.; Leukemia. 2009 Sep; 23(9):1564-76.
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