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Description: Inhibitor of mitotic motor kinesin Eg5
Chemical Name: 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone
Purity: ≥99% (HPLC)
Citations (1)
Literature (1)

Biological Activity for Dimethylenastron

Dimethylenastron 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.

Technical Data for Dimethylenastron

M. Wt 302.39
Formula C16H18N2O2S
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 863774-58-7
PubChem ID 11609157
Smiles O=C1CC(C)(C)CC2=C1C(C3=CC=CC(O)=C3)NC(N2)=S

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Dimethylenastron

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 30.24 100
ethanol 15.12 50

Preparing Stock Solutions for Dimethylenastron

The following data is based on the product molecular weight 302.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.31 mL 16.53 mL 33.07 mL
5 mM 0.66 mL 3.31 mL 6.61 mL
10 mM 0.33 mL 1.65 mL 3.31 mL
50 mM 0.07 mL 0.33 mL 0.66 mL

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Product Datasheets for Dimethylenastron

References for Dimethylenastron

References are publications that support the biological activity of the product.

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

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

If you know of a relevant reference for Dimethylenastron, please let us know.

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Keywords: Dimethylenastron, 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, Kinesin, Mitosis, 5261, Tocris Bioscience

1 Citation for Dimethylenastron

Citations are publications that use Tocris products. Selected citations for Dimethylenastron include:

Simon P et al (2021) Intestinal goblet cells sample and deliver lumenal antigens by regulated endocytic uptake and transcytosis. Elife 10 PMID: 34677124

Do you know of a great paper that uses Dimethylenastron from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:

  • Cell Cycle and Mitosis
  • DNA Damage Repair
  • Targeted Protein Degradation
  • Ubiquitin Proteasome Pathway
  • Chemotherapy Targets