Monopolar spindle 1 (Mps1), also known as TTK, is a serine threonine kinase, which ensures proper biorientation of sister chromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC). Mps1 has been shown to function as the key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughter cells.Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disruption of Mps1 function induces aneuploidy and cell death.
||BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
||CFI-402257 is a highly selective and orally bioavailable TTK and Mps1 inhibitor with Kis of 0.1 and 0.09 nM, respectively.
||AZ3146 is a reasonably potent and selective Mps1 inhibitor with IC50 of 35 nM for Mps1Cat.
||Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
||NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
||NMS-P715 analog is an inhibitor of MPS1, with an IC50 of 84 nM.
||Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
||Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
||A potent, selective, orally active Mps1 (TTK) inhibitor with IC50 of 3.1 nM