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Names | |
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IUPAC name
ethyl 4-(3-hydroxyphenyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxylate
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Other names
Monastrol
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Identifiers | |
3D model (JSmol)
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ChEBI | |
ChEMBL | |
ChemSpider | |
PubChem CID
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CompTox Dashboard (EPA)
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Properties | |
C14H16N2O3S | |
Molar mass | 292.35344 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa).
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Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab of Tim Mitchison. Monastrol was shown to inhibit the kinesin-5 (also known as KIF11, Kinesin Eg5), a motor protein important for spindle bipolarity.[1]
Mechanism of action
Monastrol binds to a long loop that is specific to the Eg5 (also known as KIF11 or kinesin-5) kinesin family, and allosterically inhibits ATPase activity of the kinesin [2]
References
- ^ Thomas U. Mayer; Tarun M. Kapoor; Stephen J. Haggarty; Randall W. King; Stuart L. Schreiber; Timothy J. Mitchison (1999). "Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen". Science. 286 (5441): 971–974. doi:10.1126/science.286.5441.971. PMID 10542155. S2CID 15348455.
- ^ Maliga Z, Kapoor TM, Mitchison TJ (September 2002). "Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5". Chem. Biol. 9 (9): 989–96. doi:10.1016/S1074-5521(02)00212-0. PMID 12323373.
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