Cat. No. 5261

Dimethylenastron C16H18N2O2S [863774-58-7]

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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

Soluble to 100 mM in DMSO and to 50 mM in ethanol
>99 %
Store at +4°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Sun et al (2011) Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta.Pharmacol Sin. 32 1543. PMID: 21986572.

Kaan et al (2010) Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J.Med.Chem. 53 5676. PMID: 20597485.

Liu et al (2006) Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells. J.Biol.Chem. 281 18090. PMID: 16627469.

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Keywords: Dimethylenastron, supplier, inhibitors, inhibits, of, mitotic, motor, kinesin, Eg5, mitosis, apoptosis, inducer, Hsp-70, expression, PI3K/Akt, pathway, myeloma, cell, migration, invasion, cytoprotective, antimitotic, antitumor, Tocris Bioscience, Kinesin Inhibitor products

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