Chemical Name: 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone
Biological ActivityDimethylenastron is an 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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
Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.
Kaan et al.
Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells.
Liu et al.
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