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Mps1-IN-1

Catalog No.
B4907
Mps1 kinase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$99.00
In stock
5mg
$89.00
In stock
10mg
$163.00
In stock
50mg
$575.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Reference:
Kwiatkowski N, Jelluma N, Filippakopoulos P et al.  Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt535.66
Cas No.1125593-20-5
FormulaC28H33N5O4S
Solubilityinsoluble in H2O; ≥16.05 mg/mL in DMSO; ≥9.26 mg/mL in EtOH
Chemical Name1-(4-((4-((2-(isopropylsulfonyl)phenyl)amino)-1H-pyrrolo[2,3-b]pyridin-6-yl)amino)-3-methoxyphenyl)piperidin-4-ol
SDFDownload SDF
Canonical SMILESOC1CCN(C2=CC(OC)=C(NC3=NC4=C(C=CN4)C(NC5=C(S(=O)(C(C)C)=O)C=CC=C5)=C3)C=C2)CC1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

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