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K858 (Racemic)

K858 Racemic (K858) 是一种选择性有丝分裂驱动蛋白 Eg5 抑制剂，以 ATP 非竞争性方式起作用，IC50值为 1.3 μM。

CAS号

72926-24-0

分子式

C13H15N3O2S

主要靶点

Kinesin|Apoptosis

仅限科研使用

Cat No : CM04933

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Synonyms

K858|K858 Racemic

验证数据展示

  • CAS No.: 72926-24-0

    K858 (Racemic)
    CAS#: 72926-24-0

产品信息

K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.

CAS号 72926-24-0
分子式 C13H15N3O2S
主要靶点 Kinesin|Apoptosis
主要通路 凋亡|细胞骨架
分子量 277.34
纯度 100.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 K858|K858 Racemic

靶点活性

Eg5:1.3 μM

体内活性

K858 exhibits antitumor activity and induces mitotic arrest in a human tumor xenograft mouse model. K858 exhibits antitumor activity and induces mitotic arrest in human xenograft tumor models. [1]

体外活性

K858 is an ATP-uncompetitive inhibitor of Eg5 that is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K858 induces mitotic arrest and growth inhibition through the activation of the Mad2-mediated spindle checkpoint. K858 induces mitotic cell death in Y cells but not in normal cells. K858 induces mitotic arrest, apoptosis, and cell growth inhibition and has no effect on microtubule polymerization.

溶解度

DMSO:27.7 mg/mL(100 mM)

参考文献

1.Nakai R, et al. Y Res. 2009 May 1;69(9):3901-9.
2.Indorato RL, et al. Biochem Pharmacol. 2013 Nov 15;86(10):1441-51.

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