Mps1-IN-1 dihydrochloride

Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells[1].

Mps1: 367 nM (IC₅₀); Mps1: 27 nM (Kd); ALK: 21 nM (Kd); LTK: 29 nM (Kd); PYK2: 280 nM (Kd); FAK: 440 nM (Kd); IGF1R: 750 nM (Kd); INSR: 470 μM (Kd); CLK1: 1900 nM (Kd); ERK2: 2900 nM (Kd); INSRR: 1200 nM (Kd); TNK1: 2600 nM (Kd); TNK2: 3100 nM (Kd); GAK: 1100 nM (Kd)

Desiccate at RT

[1] Nicholas Kwiatkowski, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. DOI:10.1038/nchembio.345