Dimethylenastron

An inhibitor of EG5

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5mg

￥687.00

550.00

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10mg

￥1087.00

870.00

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50mg

￥4312.00

3450.00

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100mg

￥7012.00

5610.00

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货号: ajce50180
CAS: 863774-58-7
别名: 2,3,4,6,7,8-六氢-4-(3-羟基苯基)-7,7-二甲基-2-硫代-5(1H)-喹唑啉酮
分子式: C16H18N2O2S
分子量: 302.39
纯度: >98%
溶解度: DMSO : ≥ 31 mg/mL (102.52 mM)
储存: Store at -20°C
库存: 现货

Background

Dimethylenastron is an inhibitor of the mitotic kinesin Eg5 (IC₅₀ = 200 nM in an ATPase assay).¹ It is selective for Eg5 over other kinesin subfamilies from four different organisms. Dimethylenastron induces accumulation of HeLa cells in the G₂/M phase (75% at a concentration of 1 μM). It inhibits spindle formation and induces radial arrangement of chromosomes in Xenopus oocytes. Dimethylenastron inhibits migration and growth of PANC-1 pancreatic cancer cells in a concentration-dependent manner.² Dimethylenastron also inhibits angiogenesis and induces severe circulation defects in zebrafish embryos.³

1.Gartner, M., Sunder-Plassmann, N., Seiler, J., et al.Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5Chembiochem6(7)1173-1177(2005) 2.Sun, X.-d., Shi, X.-j., Sun, X.-o., et al.Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5Acta Pharmacol. Sin.32(12)1543-1548(2011) 3.Exertier, P., Javerzat, S., Wang, B., et al.Impaired angiogenesis and tumor development by inhibition of the mitotic kinesin Eg5.Oncotarget4(12)2302-2316(2013)

Protocol

Cell experiment:

Cell invasion in response to Dimethylenastron is carried out by transwell assays. The upper surface of the transwell filters is coated with matrigel or fibronectin. Cells suspended in 200 μL serum-free media are added to the chamber, and the chamber is placed in a 24-well plate containing complete medium. After 24 h of incubation at 37°C, the filters are gently taken out and matrigel on the upper surface of the filters is removed by cotton swabs. Cells on the underside of transwell filters are fixed with 4% paraformaldehyde for 30 min, stained with 0.1% crystal violet for 10 min, and then photographed. For quantitative assessment, the number of invading cells is counted in five random fields per filter. The extent of cell invasion is quantified as the number of invading cells in the drug-treatment group divided by the number of invading cells in the control group[2].

Animal experiment:

Just after the conjunctival suture is closed, a metallic needle (30 G) is inserted into the subconjunctival space at the nasal margin of the superior rectus muscle and injection of one of the following agents is delivered: The rabbits receive either no adjuvant after the surgery in the control group, one unilateral subconjunctival injection of Dimethylenastron (1.0 μmol, 3.0 μmol) or of the vehicle (DMSO, 99.9%, 10 mg/mL) alone at baseline, which means an injection directly after surgery and in two further groups additionally at days 3 and 7 thereafter (1.0 μmol, 3.0 μmol)[3].

参考文献:

[1]. Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7.
[2]. Sun XD, et al. 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.
[3]. Lüke J, et al. The effect of adjuvant dimethylenastron, a mitotic Kinesin Eg5 inhibitor, in experimental glaucoma filtration surgery. Curr Eye Res. 2010 Dec;35(12):1090-8.