Monopolar spindle 1 (Mps1/TTK) is a serine/threonine kinase conserved from yeast to human.It has been demonstrated that it serves as the essential kinase that triggers the spindle assembly checkpoint (SAC) to ensure that chromosomes are distributed properly to daughter cells.
One of the key elements of the SAC is MPS1, a dual specificity protein kinase that prevents cells from transitioning from metaphase to anaphase until the kinetochores are correctly attached to the microtubules and under the proper tension at the metaphase plate. In order to handle aneuploidy, which is brought on by abnormally high or low chromosome numbers, cancer cells heavily rely on MPS1. Numerous tumor types have been found to have the kinase upregulated. Due to Mps1's high level of expression in cancer cells and the relationship between these levels and the histological grades of cancers, it is a desirable oncology target.
|BAY 1217389 (BAY-1217389) is a novel, potent, orally bioavailable and selective inhibitor of the serine/threonine kinase monopolar spindle 1 (MPS1) (IC50< 10 nM) with potential cancer activity by selectively binding to and inhibiting the activity of Mps1.
|Empesertib (also known as BAY 1161909) is a novel, potent, orally bioavailable, and selective inhibitor of serine/threonine kinase Mps1 (monopolar spindle 1)with an IC50 of < 1 nM.
|Mps1-IN-1 is a novel, ATP-competitive, selective and potent Mps1 kinase inhibitor with antitumor activity.
|Mps1-IN-2 is a novel,ATP-competitive and potent Mps1 (monopolar spindle)/Plk1(Polo Like Kinase 1) inhibitor with potential anticancer activity.
|TC-Mps1-12 is a novel, selective and potent monopolar spindle 1 (Mps1) inhibitor with anticancer activity.