微管蛋白聚合抑制剂

微管蛋白聚合抑制剂用途

Tubulin polymetition-IN-24(化合物HMBA)是一种有效的微管蛋白聚合抑制剂。微管蛋白聚合-IN-24抑制MCF-7细胞增殖。微管蛋白聚合-IN-24在G2/M期诱导细胞凋亡和细胞周期阻滞。微管蛋白聚合-IN-24增加GTP水解速率并抑制微管组装[1]。

微管蛋白聚合抑制剂名称

[ CAS 号 ]:
564468-51-5

[ 中文名 ]:
微管蛋白聚合抑制剂

[ 英文名 ]:
tubulin polymerization inhibitor

[英文别名 ]:

微管蛋白聚合抑制剂生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白

信号通路 >> 细胞骨架 >> 微管/微管蛋白

[体外研究]

微管蛋白聚合-IN-24(化合物HMBA)以浓度依赖性方式抑制纯化微管蛋白(无MAPs)的组装[1]。24(0-100 nM)中的微管蛋白聚合以浓度依赖性方式抑制MCF-7增殖,IC50值为47 nM[1]。微管蛋白聚合-IN-24竞争性抑制秋水仙碱与微管蛋白的结合,Ki值为3.6μM[1]。微管蛋白聚合-IN-24在有丝分裂中抑制MCF-7细胞的进展,并诱导涉及p53途径的凋亡细胞死亡[1]。

[参考文献]

[1]. Chatterji BP, et al. HMBA depolymerizes microtubules, activates mitotic checkpoints and induces mitotic block in MCF-7 cells by binding at the colchicine site in tubulin. Biochem Pharmacol. 2010 Jul 1;80(1):50-61.

微管蛋白聚合抑制剂物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
524.7±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₂H₁₆O₃

[ 分子量 ]:
328.361

[ 闪点 ]:
188.8±23.6 °C

[ 精确质量 ]:
328.109955

[ LogP ]:
3.80

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.700

微管蛋白聚合抑制剂安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

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