货号 | 5261/50 |
别名 | 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyp |
供应商 | Tocris |
生物活性 | 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. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 302.39 |
分子式 | C16H18N2O2 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
参考文献 | Sunet 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. Kaanet 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. Liuet 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. |