Tubulin inhibitor 14 是一种有效的 NQO2(醌氧化还原酶 2)抑制剂,IC50 为 1.0 μM,也抑制微管蛋白聚合和内皮细胞毛细管样管的形成。Tubulin inhibitor 14 是一种微管去稳定剂,具有潜在的肿瘤选择性以及抗血管生成和血管破坏的功能[1]。
产品描述
Tubulin inhibitor 14 is a potent inhibitor of NQO2 (quinone oxidoreductase 2) with an IC50 of 1.0 μM which also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule destabilizer with potential tumor-selective as well as anti-angiogenic and vascular-destructive properties [1].
体外活性
Tubulin inhibitor 14 (compound 4) (0-20 μM, 96 h) inhibits the proliferation of cancer cells[1]. Tubulin inhibitor 14 (1-5 μM, 24 or 48 h) leads to G2/M cell cycle arrest [1]. Tubulin inhibitor 14 (0.5-1 μM, 24 h) activates SNU423 cell apoptosis [1]. Tubulin inhibitor 14 (0.5-1 μM, 24 h) disrupts the cytoskeleton network in endothelial cells which induces morphological alterations in endothelial cells [1]. Cell Proliferation Assay [1] Cell Line: MDA-MB-231, HepG2, SNU423, A549, HCT116 Concentration: 0 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, and 20 μM Incubation Time: 96 h Result: showed significant growth inhibition of cell proliferation with IC 50 values of 0.41 μM (MCF-7), 0.07 μM (MDA-MB-231), 1.44 μM (HepG2), 0.25 μM (SNU423), 0.27 μM (A549), and 0.13 μM (HCT116). Cell Cycle Analysis [1] Cell Line: HepG2 cells Concentration: 1, 2, 5 μM Incubation Time: 24 h, 48 h Result: Caused G2/M cell cycle arrest. Apoptosis Analysis [1] Cell Line: SNU423 cells Concentration: 0.5, 1 μM Incubation Time: 24 h Result: Induced SNU423 cell apoptosis. Immunofluorescence [1] Cell Line: HUVECs Concentration: 0.5, 1 μM Incubation Time: 24 h Result: Disrupted the cytoskeleton network in endothelial cells which induces morphological alterations in endothelial cells.
分子式
C15H9F2NO
分子量
257.23
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years