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Mps1-IN-3 is an inhibitor of monopolar spindle 1 (Mps1; IC50 = 50 nM).1 It inhibits the proliferation of U251 glioblastoma cells (IC50 = ~5 µM). Mps1-IN-3 (2 µM) prevents checkpoint-mediated mitotic arrest induced by nocodazole (Item No. 13857) in U2OS osteosarcoma cells and, when used at a concentration of 5 µM in combination with the antimitotic agents vincristine (Item No. 11764) or paclitaxel (Item No. 10461), induces nuclear aberrancies and chromosome missegregation defects in U251-FM-H2B-GFP cells, which express firefly luciferase, mCherry, and a histone H2B-GFP fusion reporter. It sensitizes U251-FM cells to vincristine and increases survival in an orthotopic mouse model of glioblastoma when administered at a dose of 2 mg/kg.
WARNING This product is not for human or veterinary use.
1. Effects of the selective MPS1 inhibitor MPS1-