Catalog Number: 5261
Chemical Name: 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone
Biological Activity
Inhibitor of mitotic motor kinesin Eg5 (IC50 = 200 nM). Arrests mitosis, triggers apoptosis and up-regulates Hsp-70 expression in multiple human myeloma cell lines. Also inhibits the growth of several types of cancer cell lines (EC50 values are 330, 603, 743 and 881 nM in HCT116, Htert-HME1, BxPC3, K562 and NCI-H1299 cancer cells, respectively). Suppresses the migration and invasion of PANC1 cells in vitro. Cytoprotective.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Background References
  1. Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
    Kaan et al.
    J.Med.Chem., 2010;53:5676
  2. Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells.
    Liu et al.
    J.Biol.Chem., 2006;281:18090
  3. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5.
    Sun et al.
    Acta.Pharmacol Sin., 2011;32:1543
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