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Description

A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1, IC50 = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes., A cell permeable purinone derivative that acts as a highly potent and selective inhibitor of monopolar spindle 1 kinase (MPS1, IC50 = ~35 nM). Inhibits the phosphorylation of full-length immunoprecipitated human MPS1 and exhibits minimal activity against a panel of 49 other protein kinases. Has much reduced activity against FAK, JNK1, JNK2, and KIT and does not affect the activity of mitotic-specific phosphoforms of Aurora B and BubR1. Induces a significant reduction in time to complete mitosis (from 90 min to 32 min) and causes abnormal mitosis where over 50% of cells enter anaphase without aligning their chromosomes.Please note that the molecular weight for this compound is batch-specific due to variable water content.