Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor.

PLK1:61 nM (Kd), GAK:140 nM (Kd), PLK4:3100 nM (Kd), Mps1:145 nM, STK33:5000 nM (Kd), PLK3:1600 nM (Kd)

mTOR activity is assayed using LanthaScreen Kinase kit reagents. PI(3)K α, β, γ and δ activity are assayed using the PI(3)K HTRF assay kit. The concentration of INK128 necessary to achieve inhibition of enzyme activity by 50% (IC50) is calculated using concentrations ranging from 20 μM to 0.1 nM (12-point curve). IC50?values are determined using a nonlinear regression model.