Definition

A selective inhibitor of the serine/threonine-protein kinase monopolar spindle 1 (Mps1; TTK), with potential antineoplastic activity. Upon administration, MPS1 kinase inhibitor NMS-01940153E targets, binds to and inhibits the activity of Mps1, a core component of the spindle assembly checkpoint (SAC). Inhibition of Mps1 activity compromises the functioning of SAC, increases chromosome missegregation errors and decreases cancer cell viability. This inhibits tumor cell proliferation. Mps1, a dual-specificity protein kinase expressed in proliferating normal tissues and aberrantly overexpressed in certain tumor types, is activated during mitosis and is essential in proper SAC function, chromosomal alignment and segregation during cellular division.