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CAS No.: 72926-24-0

K858 (Racemic) Catalog No. CSN18408

Synonyms: K858

K858 is a selective and ATP-uncompetitive mitotic kinesin Eg5 inhibitor with IC50 value of 1.3 μM.

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技术信息

生物活性

描述Kinesins are widely expressed, microtubule-dependent motors that play vital roles in microtubule-associated cellular activities, such as cell division and intracellular transport. Eg5, also known as kinesin-5 or kinesin spindle protein, is a member of the kinesin family that contributes to the formation and maintenance of the bipolar mitotic spindle during cell division^[3]. K858 was selected in a phenotype-based forward chemical genetics screen as an antimitotic agent, and subsequently characterized as an inhibitor of Eg5. K858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. Long-term continuous treatment of cancer cells with K858 resulted in antiproliferative effects through the induction of mitotic cell death, and polyploidization followed by senescence. In contrast, treatment of nontransformed cells with K858 resulted in mitotic slippage without cell death, and cell cycle arrest in G(1) phase in a tetraploid state^[4]. K858 is a potent inhibitor of replication and induces apoptosis in breast tumor cells, independently from the tumor phenotype. This anti-proliferative response of tumor cells to K858 can be limited by the contemporaneous over-expression of survivin; the reduction of survivin levels by AKT inhibitors can sensitize tumor cells to K858-induced apoptosis^[5]. Glioblastoma cells usually express high levels of kinesin Eg5, K858 inhibited cell growth, induced apoptosis, reversed epithelial-mesenchymal transition and inhibited migration in both cell lines. At the same time, K858 increased the expression of survivin, an anti-apoptotic molecule, and that the forced down-regulation of survivin, obtained with the specific inhibitor YM155, boosted K858-dependent apoptosis^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6057 mL
- 18.0283 mL
- 36.0566 mL
- 5 mM
- 0.7211 mL
- 3.6057 mL
- 7.2113 mL
- 10 mM
- 0.3606 mL
- 1.8028 mL
- 3.6057 mL

技术信息

CAS号

72926-24-0

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H15N3O2S

运输

蓝冰

分子量

277.34

别名

K858

溶解度

DMSO	95.0 mg/mL (342.5 mM)
Water	insoluble

动物实验配方

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