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Dimethylenastron
- Eg5 inhibitor III
- Soluble in DMSO
- MF: C16H18N2O2S
- MW: 302.39
Description
Dimethylenastron is a potent, cell-permeable inhibitor of the mitotic motor Eg5/KIF11. It disrupts bipolar spindle formation, induces mitotic arrest and blocks proliferation in dividing cells.
Eg5/KSP is required for centrosome separation and mitotic spindle assembly. Dimethylenastron provides an antimitotic tool for studying kinesin motor pharmacology, mitotic catastrophe and cell-cycle checkpoint responses.
Key Features
- Eg5/KIF11 mitotic kinesin inhibitor
- Reported IC50: 200 nM
- More potent than monastrol in reported comparative assays
- Induces spindle defects and mitotic arrest
Applications
- Kinesin spindle protein pharmacology
- Mitotic arrest and spindle assembly studies
- Cancer cell proliferation assays
- Cell-cycle checkpoint research
More Information
| Parent CAS No. | 863774-58-7 |
|---|---|
| Chemical Name | 4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-1,2,3,4,7,8-hexahydroquinazolin-5(6H)-one |
| SMILES | N1C2=C(C(=O)CC(C)(C)C2)C(C2=CC=CC(O)=C2)NC1=S |
| MFCD | N.A. |
| InChi | InChI=1S/C16H18N2O2S/c1-16(2)7-11-13(12(20)8-16)14(18-15(21)17-11)9-4-3-5-10(19)6-9/h3-6,14,19H,7-8H2,1-2H3,(H2,17,18,21) |
| InChiKey | RUOOPLOUUAYNPY-UHFFFAOYSA-N |
| CID | 11609157 |
| Short Description | Eg5 inhibitor |
References
- M. Gartner et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7.
- M. Liu et al. Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells. J Biol Chem. 2006 Jun 30;281(26):18090-7.
- M. Liu et al. Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor. Biochem Pharmacol. 2008 Jul 15;76(2):169-78.
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