Mps1-IN-1

Mps1-IN-1

Catalog Number:
L002370713APE
Mfr. No.:
APE-B4907
Price:
$292
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      • Overview
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          Background

          Mps1-IN-1 is a selective Mps1 (monopolar spindle 1) kinase inhibitor with IC50 value of 367 nM.MPS1 (monopolar spindle 1 kinase) is a crucial part of the spindle assembly checkpoint. It facilitates the formation of C-MAD2 (closed MAD2) conformer and the MCC (mitotic checkpoint complex) assembly, involved in the maintenance of chromosomal stability and tumor growth. Mps1-IN-1 abolishes the SAC (spindle assembly checkpoint) function. In U2OS cells, dose-dependent treatment of Mps1-IN-1 decreases the time spent in mitosis with almost 100% cells starting anaphase in 20 minutes. In contrast, just 10% of DMSO-treated cells starting anaphase in the same period. Acceleration of mitosis kinetics in Mps1-IN-1 treated cells affects genomic stability and causes aneuploidy. In addition, Mps1-IN-1 treated cells shows decrease in kinetochore-bound Mad2 by 80%. Mps1-IN-1–treated cells spent roughly 40% less time in mitosis as compared to DMSO-treated cells. Moreover, Mps1-IN-1 disrupts the kinase activity of Aurora B. Mps1-IN-1 treatment lead to decrease in the phosphorylation status of Aurora B at Thr232 in a dose-dependent manner. Furthermore, Mps1-IN-1 increases multipolar cell divisions and decreases cell viability.

      • Properties
        • Alternative Name
          1-(4-((4-((2-(isopropylsulfonyl)phenyl)amino)-1H-pyrrolo[2,3-b]pyridin-6-yl)amino)-3-methoxyphenyl)piperidin-4-ol
          CAS Number
          1125593-20-5
          Molecular Formula
          C28H33N5O4S
          Molecular Weight
          535.66
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥16.05 mg/mL in DMSO; ≥9.26 mg/mL in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

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