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| MONASTROL Basic information |
| Product Name: | MONASTROL | | Synonyms: | 4-(3-HYDROXYPHENYL)-6-METHYL-2-THIOXO-1,2,3,4-TETRAHYDRO-4H-PYRIMIDIN-5-CARBOXYLIC ACID ETHYL ESTER;6-METHYL-4-(3-HYDROXYPHENYL)-2-THIOXO-1,2,3,4-TETRAHYDROPYRIMIDINE-5-CARBOXYLATE;1,2,3,4-TETRAHYDRO-4-(3-HYDROXYPHENYL)-6-METHYL-2-THIOXO-5-PYRIMIDINECARBOXYLIC ACID, ETHYL ESTER;Monastrol - CAS 254753-54-3 - Calbiochem;CS-2432;5-Pyrimidinecarboxylic acid, 1,2,3,4-tetrahydro-4-(3-hydroxyphenyl)-6-methyl-2-thioxo-, ethyl ester, (4S)-;O-(4-Hydroxy-3-iodophenyl)-3 | | CAS: | 254753-54-3 | | MF: | C14H16N2O3S | | MW: | 292.35 | | EINECS: | | Product Categories: | All Inhibitors;Inhibitors | | Mol File: | 254753-54-3.mol |
| MONASTROL Chemical Properties |
| Melting point | 185-185.9 °C(lit.) | | Boiling point | 441.3±55.0 °C(Predicted) | | density | 1.34±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 100 mg/mL | | pka | 9.63±0.10(Predicted) | | form | White solid | | color | white to off-white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. | | CAS DataBase Reference | 254753-54-3(CAS DataBase Reference) |
| MONASTROL Usage And Synthesis |
| Description | Monastrol (254753-54-3) is a potent, cell-permeable, small molecule inhibitor of mitosis. Monastrol-arrested cells are characterized by monopolar spindles.1?Does not affect other motor proteins or tubulin. Specifically inhibits the mitotic molecular motor kinesin Eg5, a motor protein required for spindle formation (IC50?= 14 μM).2?Mimics the effect of amyloid β on long term potentiation in a cellular model of learning and memory.3?Enhances regeneration of adult axons.4 | | Chemical Properties | Crystalline Solid | | Uses | Inhibitor of mammalian cell mitosis. | | Uses | Monastrol has been used:- to treat MDA-MB-231 cells as a non-microtubule-targeting agent
- as a antineoplastic agent, to treat mouse myeloma cell line SP 2/0, to induce apoptosis and to elucidate the role of metabotropic glutamate receptor 3 (Grm3) in apoptosis
- as an inhibitor of pteridine reductase in GFP-transfected promastigotes infected macrophages for flow cytometer-based growth inhibition assay and to evaluate anti-leishmanial activity of Leishmania donovani hamster model in vivo
| | Uses | A cell-permeablesmall molecule inhibitor of the mitotic kinesin, Eg5, arrests cells in mitosis with monoastral spindles | | Biological Activity | Potent, cell-permeable, small molecule mitosis inhibitor that does not interact with tubulin. Arrests cells in mitosis and specifically inhibits the motility of the mitotic kinesin Eg5, a motor protein required for mitotic spindle formation and maintenance (IC 50 = 14 μ M). | | Biochem/physiol Actions | Monastrol is a potent, cell-permeant inhibitor of mitosis. Monastrol arrested cells are characterized by monopolar spindles. This phenotype is induced through specific disruption of mitotic molecular motor kinesin Eg5 with IC50 at 14 μM. No effect on other motor proteins and tubulin. | | References | 1) Mayer?et al. (1999), Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen; Science,?286?971
2) Kapoor?et al.?(2000),?Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of mitotic kinesin, Eg5; J. Cell Biol.,?150?975
3) Ari?et al.?(2014),?Alzheimer amyloid beta inhibition of Eg5/kinesin 5 reduces neurotrophin and/or transmitter receptor function; Neurobiol. Aging,?35?1839
4) Lin?et al. (2011),?Inhibition of Kinesin-5, a microtubule-based motor protein, as a strategy for enhancing regeneration of adult axons; Traffic,?12?269 |
| MONASTROL Preparation Products And Raw materials |
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