Biological Activity
Selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 367 nM); exhibits >1000 fold-selectivity against a panel of 352 kinases with the exceptions of ALK and Ltk. Disrupts the recruitment of Mad2 to kinetochores. Increases frequency of multipolar mitosis in U2OS cells.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of Mps1-IN-1 is reviewed on the chemical probes website.
Compound Libraries
Mps1-IN-1 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 608.58 |
| Formula | C28H33N5O4S.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 91691119 |
| InChI Key | HFJLUXGXTPNYTQ-UHFFFAOYSA-N |
| Smiles | CC(C)S(C(C=CC=C3)=C3NC1=CC(NC4=C(OC)C=C(N5CCC(O)CC5)C=C4)=NC2=C1C=CN2)(=O)=O.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 60.86 | 100 | |
| water | 60.86 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 608.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.64 mL | 8.22 mL | 16.43 mL |
| 5 mM | 0.33 mL | 1.64 mL | 3.29 mL |
| 10 mM | 0.16 mL | 0.82 mL | 1.64 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.33 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kwiatkowski et al (2010) Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat.Chem.Biol. 6 359 PMID: 20383151
Miduturu et al (2011) High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chem.Biol. 18 868 PMID: 21802008
Lan and Cleveland (2010) A chemical tool box defines mitotic and interphase roles for Mps1 kinase. J.Cell Biol. 190 21 PMID: 20624898
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