| References: |
Polo-like Kinase Inhibitor III (GW843682X) is a cell-permeable thiophene-benzimidazole compound that acts as a potent and reversible inhibitor against Plk (polo-like kinases) (Ki against Plk1/2/3/4 = 4.8, 3.8, 8.0, and 163 nM , respectively), while exhibiting little or much reduced activity against 39 other commonly studied kinases. Polo-like Kinase Inhibitor III preferentially inhibits the proliferation of a panel of 11 tumor cell lines (IC50 ≤0.7 μM) over normal human diploid fibroblasts (IC50 = 6.14 μM) in culture and is equally potent against the mdr-1-expressing MES-SA/DX5 and its parent non-drug resistant MES-SA uterine sarcoma cell line. |
