Mps1-IN-1 (Synonyms: Monopolar Spindle 1 Kinase Inhibitor 1, Mps1 Kinase Inhibitor 1) |
| رقم الكتالوجGC11292 |
Mps1-IN-1 هو مثبط كيناز قوي وانتقائي وتنافسي ATP ، مع IC50 و Kd من 367 نانومتر و 27 نانومتر
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Cas No.: 1125593-20-5
Sample solution is provided at 25 µL, 10mM.
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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:
[1].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.
Kinase experiment: | The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-1), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay[1]. |
Cell experiment: | U2OS cells expressing doxycycline-inducible PLK4 are plated in 96 well plates. A double thymidine block is performed using the following treatment regimen: thymidine for 18-20 hrs., release for 10 hrs. with doxycycline induction of PLK4 during this time, then a second thymidine block, followed by release. Six hours after the 2nd thymidine release, Mps1-IN-1 (or DMSO vehicle) is added and the proliferation of the cell populations is monitored with Cell Titer GLO assay[1]. |
References: [1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. | |
| Cas No. | 1125593-20-5 | SDF | |
| المرادفات | Monopolar Spindle 1 Kinase Inhibitor 1, Mps1 Kinase Inhibitor 1 | ||
| Chemical Name | 1-(4-((4-((2-(isopropylsulfonyl)phenyl)amino)-1H-pyrrolo[2,3-b]pyridin-6-yl)amino)-3-methoxyphenyl)piperidin-4-ol | ||
| Canonical SMILES | OC1CCN(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 | ||
| Formula | C28H33N5O4S | M.Wt | 535.66 |
| الذوبان | ≥ 16.05mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8669 mL | 9.3343 mL | 18.6686 mL |
| 5 mM | 0.3734 mL | 1.8669 mL | 3.7337 mL |
| 10 mM | 0.1867 mL | 0.9334 mL | 1.8669 mL |
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- Purity: >99.50%
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