GW843682X

GW843682X is a potent, ATP-competitive small molecule inhibitor of Polo-like kinase 1 (PLK1) and Polo-like kinase 3 (PLK3). Originally developed by GlaxoSmithKline, it is primarily utilized as a high-quality chemical probe in preclinical oncology research. PLK1 is a critical serine/threonine kinase that regulates multiple stages of mitosis, including centrosome maturation, spindle assembly, and cytokinesis. By inhibiting PLK1, GW843682X induces a characteristic polo phenotype with monopolar spindles, resulting in G2/M phase arrest and subsequent apoptosis. Research has demonstrated that sensitivity to GW843682X is particularly high in cancer cell lines, such as small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC), that exhibit mesenchymal features or specific microRNA profiles, including low expression of the miR-200 family.