MPS1 Inhibitor II, MPS1-IN-3

A cell permeable, non-toxic compound with a purine core scaffold that acts as a highly potent inhibitor of monopolar spindle1 kinase (MPS1; IC₅₀ = 50 nM). Displays good selectivity when screen against a panel of 450+ protein kinases. Reduces the levels of cyclin B that can be reversed by addition of proteasome inhibitor MG-132 (Cat. No. 474790). Inhibits SMAD2 phosphorylation and blocks the proliferation of U251 glioblastoma cells (IC₅₀ = 5 µM). Increasingly sensitizes U251 cells to the action of vincristine (~ 3 nM) in vitro and in orthotopic mouse model of glioblastoma (2 mg/kg) leading to their prolonged survival.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
MPS1

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Tannous, B.A., et al. 2013. J. Natl. Cancer Inst.105,1322.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)