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GSK-461364, GSK461364, GSK 461364, GSK-461364A, GSK 461364A, GSK461364A, 929095-18-1
Solubility: Soluble in DMSO
Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months)
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM). It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases. GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis. It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier. GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.