Neuroinflammatory-IN-3

Neuroinflammatory-IN-3, a tubulin inhibitor, is an anti-neuroinflammatory agent. Neuroinflammatory-IN-3 is a potent antitumor agent that functions by the inhibition of tubulin polymerization[1][2].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Research Areas >> Neurological Disease

Neuroinflammatory-IN-3（compound 1）在 10μM 浓度下抑制 BV-2 小胶质细胞中 LPS 介导的 NO 释放至 70%，IC50 为 5.22μM。Neuroinflammatory-IN-3 与微管蛋白的秋水仙碱结合域结合[1]。 Neuroinflammatory-IN-3（compound 1；72 小时）对 HeLa、U266、A549 和 MCF7 细胞系具有抗增殖作用，IC50 分别值为 450 nM、416 nM、381 nM 和 744 nM[2]。 Neuroinflammatory-IN-3（compound 1；1 μM；3-12 小时）以时间依赖性方式触发细胞周期停滞[2]。 Neuroinflammatory-IN-3（compound 1）以剂量依赖性方式抑制微管蛋白聚合[2]。 Cell Cycle Analysis[2] Cell Line: HeLa cells Concentration: 1 μM Incubation Time: 3 h, 6 h, 12 h Result: Triggered cell-cycle arrest.

[1]. Junhyeong Yim, et al. Phenotype-based screening rediscovered benzopyran-embedded microtubule inhibitors as anti-neuroinflammatory agents by modulating the tubulin-p65 interaction. Exp Mol Med. 2022 Dec 12;1-10  

[2]. Jongmin Park, et al. Discovery and target identification of an antiproliferative agent in live cells using fluorescence difference in two-dimensional gel electrophoresis. Angew Chem Int Ed Engl. 2012 May 29;51(22):5447-51.