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Dimethylenastron

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Chemical Structure| 863774-58-7 同义名 : Eg5 Inhibitor III
CAS号 : 863774-58-7
货号 : A187476
分子式 : C16H18N2O2S
纯度 : 99%+
分子量 : 302.391
MDL号 : MFCD09264157
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(347.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Mitotic kinesins are exclusively involved in the formation and function of the mitotic spindle, and some kinesins are only expressed in proliferating cells. Mitotic kinesin Eg5, encoded by KIF11, is essential for cell division. Dimethylenastron is specific and reversible mitotic motor kinesin Eg5 inhibitor with IC50 value of 200 nM. Growth of HUVECs and lymphatic endothelial cells (LECs) was inhibited by dimethylenastron (DMN) in a dose- and time-dependent manner (0.1-1μM, 24-96 h). U87 gliomas grown on the chicken chorio-allantoic membrane showed reduced numbers of angiogenic capillaries after treatment with a single dose of 10 ug DMN per day[3]. Treatment of PANC1 pancreatic cancer cells with dimethylenastron (3 and 10 μM) for 24 h suppressed the migratory ability of the cancer cells in a concentration-dependent manner, but had no detectable effect on their proliferation[4].
作用机制 Dimethylenastron allosterically inhibits the motor domain ATPase of Eg5 by decreasing the rate of ADP release.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.53mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL
参考文献

[1]Aljaberi AM, Webster JR, Wheatley SP. Mitotic activity of survivin is regulated by acetylation at K129. Cell Cycle. 2015;14(11):1738-47.

[2]Exertier P, Javerzat S, et al. Impaired angiogenesis and tumor development by inhibition of the mitotic kinesin Eg5. Oncotarget. 2013 Dec;4(12):2302-16.

[3]Exertier P, Javerzat S, Wang B, Franco M, Herbert J, Platonova N, Winandy M, Pujol N, Nivelles O, Ormenese S, Godard V, Becker J, Bicknell R, Pineau R, Wilting J, Bikfalvi A, Hagedorn M. Impaired angiogenesis and tumor development by inhibition of the mitotic kinesin Eg5. Oncotarget. 2013 Dec;4(12):2302-16. doi: 10.18632/oncotarget.1490. PMID: 24327603; PMCID: PMC3926828.

[4]Sun XD, Shi XJ, Sun XO, Luo YG, Wu XJ, Yao CF, Yu HY, Li DW, Liu M, Zhou J. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta Pharmacol Sin. 2011 Dec;32(12):1543-8. doi: 10.1038/aps.2011.130. Epub 2011 Oct 10. PMID: 21986572; PMCID: PMC4010204.