Mps1-IN-2 |
| رقم الكتالوجGC15745 |
Mps1-IN-2 هو مثبط ثنائي Mps1 / Plk1 قوي وانتقائي وتنافسي ATP ، مع IC50 و Kd 145 nM و 12 nM لـ Mps1 و Kd 61 nM لـ Plk1
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1228817-38-6
Sample solution is provided at 25 µL, 10mM.
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Mps1-IN-2 is a potent and selective ATP-competitive inhibitor of Mps1 kinase with the IC50 value of 145nM [1].
Mps1-IN-2 has been reported to inhibit Mps1 kinase activity with the IC50 value of 145nM, when screened at 1μM ATP. In addition, Mps1-IN-2 has shown greater than 1000-fold selectivity to the Alk and Ltk enzyme. Moreover, Mps1-IN-2 has been revealed to bound to the ATP biding pocket of Mpa1 and formed a hydrogen bond with the hinge backbone (Glu603) at 2.74-Å resolution. Mps1-IN-2 has been noted to abrogate SAC function and override the checkpoint through direct inhibition of Mps1[1].
References:
[1] Kwiatkowski N1, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. doi: 10.1038/nchembio.345. Epub 2010 Apr 11.
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-2), 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]. |
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. | 1228817-38-6 | SDF | |
| Chemical Name | 9-cyclopentyl-2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5-methyl-7,8-dihydropyrimido[4,5-b][1,4]diazepin-6-one | ||
| Canonical SMILES | CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(CCC(=O)N4C)C5CCCC5 | ||
| Formula | C26H36N6O3 | M.Wt | 480.6 |
| الذوبان | DMF: 1 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml,DMSO: 1 mg/ml,Ethanol: slightly soluble | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0807 mL | 10.4037 mL | 20.8073 mL |
| 5 mM | 0.4161 mL | 2.0807 mL | 4.1615 mL |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0807 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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