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Submit ReviewDimethylenastron
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)
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 |
| InChI Key | RUOOPLOUUAYNPY-UHFFFAOYSA-N |
| 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.
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
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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
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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