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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 185 | 现货 | |
5 mg | ¥ 413 | 现货 | |
10 mg | ¥ 662 | 现货 | |
25 mg | ¥ 1,320 | 现货 | |
50 mg | ¥ 2,150 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner. |
靶点活性 | EG5:1.3 μM |
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. |
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] |
别名 | K858 Racemic, K858 |
分子量 | 277.34 |
分子式 | C13H15N3O2S |
CAS No. | 72926-24-0 |
Smiles | CC(=O)NC1=NN(C(C)=O)C(C)(S1)c1ccccc1 |
密度 | 1.27 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 27.7 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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