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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Kinesin-K858
K858

Chemical Structure : K858

CAS No.: 72926-24-0

K858 (K-858, K 858)

货号: PC-45767Not For Human Use, Lab Use Only.

K858 is a potent, selective inhibitor of mitotic kinesin Eg5 ATPase activity with IC50 of 1.3 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

K858 is a potent, selective inhibitor of mitotic kinesin Eg5 ATPase activity with IC50 of 1.3 uM.
K858 displays >150-fold more selective for Eg5 than other members of the kinesin superfamily.
K858 induces mitotic arrest, apoptosis, and cell growth inhibition through the activation of the Mad2-mediated spindle checkpoint, and has no effect on microtubule polymerization.
K858 exhibits potent antitumor activity in xenograft models of cancer, and induces the accumulation of mitotic cells with monopolar spindles in tumor tissues.

物理化学性质&存储条件

分子量 277.3421
分子式 C13H15N3O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Acetamide, N-(4-acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)-

参考文献

1. Nakai R, et al. Cancer Res. 2009 May 1;69(9):3901-9.

2. De Iuliis F, et al. Invest New Drugs. 2016 Aug;34(4):399-406.

3. De Monte C, et al. Eur J Med Chem. 2015 Nov 13;105:245-62.

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