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.
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.
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