For research use only. Not for therapeutic Use.
GW843682X (CAT: I004488) is a potent and selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3). It exhibits high inhibitory activity with IC50 values of 2.2 nM for PLK1 and 9.1 nM for PLK3. Importantly, it demonstrates over 100-fold selectivity against a panel of approximately 30 other kinases, including cyclin-dependent kinase 1 (cdk1) and cyclin-dependent kinase 2 (cdk2). GW843682X holds promise as a valuable tool compound for investigating the functions and signaling pathways associated with PLK1 and PLK3, which are involved in cell cycle regulation and other cellular processes.
Catalog Number | I004488 |
CAS Number | 660868-91-7 |
Synonyms | 5-(5,6-dimethoxybenzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]thiophene-2-carboxamide |
Molecular Formula | C22H18F3N3O4S |
Purity | ≥95% |
Target | Polo-like Kinase (PLK) |
Solubility | Soluble to 75 mM in DMSO and to 5 mM in ethanol |
Storage | Store at -20°C |
IC50 | 2.2/9.1 nM(PLK1/3) [1] |
Reference | </br>1:The cytotoxic effect of GW843682X on nasopharyngeal carcinoma. Hu Q, Chu Y, Hu W, Peng M, Song Q.Anticancer Agents Med Chem. 2016;16(12):1640-1645. PMID: 27198987 </br>2:An in-vitro evaluation of the polo-like kinase inhibitor GW843682X against paediatric malignancies. Spaniol K, Boos J, Lanvers-Kaminsky C.Anticancer Drugs. 2011 Jul;22(6):531-42. doi: 10.1097/CAD.0b013e3283454526. PMID: 21637161 |