Name: Tubulin-IN-53
Brand: TargetMol
SKU: T212269
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述

Tubulin-IN-53 is a potent inhibitor of microtubulin (Tubulin) with an IC50 of 6.06 μM. By targeting the colchicine binding site on tubulin, Tubulin-IN-53 hinders tubulin polymerization, disrupting the microtubule network. It induces cell cycle arrest at the G2/M phase and apoptosis (apoptosis) in MCF-7 cells, while inhibiting cell migration. This compound also leads to a reduction in mitochondrial membrane potential and an increase in reactive oxygen species (ROS) accumulation. Additionally, Tubulin-IN-53 disrupts angiogenesis in human umbilical vein endothelial cells and is applicable in research on cancers such as breast and lung cancer.

体外活性

Tubulin-IN-53 (Compound A7)（72 h）在多种癌细胞中展现抗增殖效果，对 PC-3、MCF-7、MDA-MB-231、A549、HT-29 和 A549/TxR 细胞的 IC 50 分别是 6、4、5、6、4 和 10 nM，对正常细胞表现出轻微细胞毒性，L02 和 MCF-10A 细胞的 CC 50 分别为 112 和 220 nM。Tubulin-IN-53（5-20 nM, 14 d）持续阻止 MCF-7 细胞的集落形成。Tubulin-IN-53（5-20 nM, 6 h）以剂量依赖性方式阻碍 EBI 和 β-微管蛋白加合物的产生，并可完全破坏 MCF-7 细胞的微管网络。Tubulin-IN-53（5-20 nM, 24 h）可以诱导 MCF-7 细胞周期停滞在 G2/M 期并诱发细胞凋亡，同时显著提升细胞内 ROS 水平。Tubulin-IN-53（2.5-10 nM, 24 h）能抑制 A549 细胞的迁移，并有效抑制内皮细胞中血管网络的生成。