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]. In Vitro: Mps1-IN-1 dihydrochloride (2-10 μM; 96 hours) inhibits the proliferative capacity of HCT116 cells to 33% that of DMSO control^[1].
Mps1-IN-1 dihydrochloride (0.3-10 μM; 4 hours) induces bypass of a checkpoint-mediated mitotic arrest in a dose-dependent manner. Mps1-IN-1 dihydrochloride (10 µM) administration results in a dose-dependent decrease in the time spent in mitosis with nearly 100% U2OS cells initiating anaphase within 20 minutes^[1].
Mps1-IN-1 dihydrochloride (0.5, 2, 10 μM) causes a dose-dependent reduction in hyper-phosphorylated Mps1 as demonstrated by a decrease in phosphorylation-induced mobility shift in UTRM10 LAP-Mps1 WT cells^[1].
Mps1-IN-1 (5, 10 μM) arrested in mitosis using Nocodazole, results in a dose-dependent accumulation of 4c pHistone H3 negative cells in U2OS cells^[1].
Acceleration of mitosis kinetics in Mps1-IN-1-treated cells had direct consequences on genomic stability with cells exhibiting significant signs of chromosome mis-alignment and chromosome mis-segregation^[1].
Mps1-IN-1 dihydrochloride demonstrates greater than 1000-fold selectivity relative to the 352 member kinase panel with the major exceptions of Alk and Ltk^[1].