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Monopolar spindle 1 (Mps1) inhibitors block a mitotic kinase that drives the spindle assembly checkpoint. In human cells the kinase is also known as threonine and tyrosine kinase (TTK). The MPS1 gene was first described in budding yeast, where it is needed to duplicate the spindle pole body. During mitosis Mps1 acts at unattached kinetochores and is required to recruit the checkpoint protein Mad2 to the Mad1-Mad2 core complex. Inhibition shortens mitosis and lets cells divide with misaligned chromosomes, which leads to aneuploidy. Representative compounds are AZ 3146, Mps1-IN-1, MPI-0479605 and the TTK inhibitor CFI-401870.
CFI-400936 is a potent inhibitor of the TTK protein kinase, demonstrating an IC50 of 3.6 nM. This compound exhibits significant antitumor activity, making it valuable for research focused on cancer treatment and cellular proliferation studies. Its ability to modulate TTK activity positions it as a useful tool for investigating therapeutic strategies in oncology.
ONCOII is a potent Mps1 inhibitor with an IC50 of 10.8 nM, primarily targeting the Mps1 kinase involved in cell division and checkpoint regulation. This reagent's efficacy is influenced by specific mutations in the Mps1 gene, as cells harboring such mutations show increased resistance to ONCOII. It is particularly useful in cancer research to study cell cycle dynamics and the effects of Mps1 modulation in tumorigenesis.
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Mps-BAY2b is a potent inhibitor of monopolar spindle 1 (MPS1) with an IC50 of 14 nM in human MPS1. This compound demonstrates significant anticancer activity, making it a valuable tool for cancer research. Mps-BAY2b can be utilized in studies to investigate cell cycle regulation and the mechanisms of tumor progression.
Mps1/TTK-IN-1 is a potent Mps1 kinase inhibitor that specifically binds to the ATP-binding pocket of the enzyme with an IC50 of 9.2 nM and a Kd of 1.6 nM. It effectively inhibits Mps1 activity, including in drug-resistant mutants (C604Y and C604W) with IC50 values of 170 nM and 19 nM, respectively. By blocking the phosphorylation of the kinetochore protein KNL1, Mps1/TTK-IN-1 disrupts spindle assembly checkpoint function and hinders proper chromosome separation, ultimately inhibiting mitosis and tumor cell proliferation, making it a valuable tool for cancer research.
