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 | 302.39 |
| Formula | C16H18N2O2S |
| Storage | Store at +4°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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.24 | 100 | |
| ethanol | 15.12 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 302.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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
References
References are publications that support the products' biological activity.
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
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, Kinesin, Mitosis, Kinesin, Tocris Bioscience
