| Bioactivity | Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity[1]. |
| Invitro | Tubulin/HDAC-IN-4 (compound 9n) (0-10 µM; 72 h) 对 MDA-MB-231、A549 表现出细胞毒性，IC50s 为 0.34、0.29、0.016、0.15、0.16 µM 分别为 PC-3、U251、MCF-7 细胞[1]。Tubulin/HDAC-IN-4（2.5、5、10、20、40 nM；24 小时）以剂量依赖性方式抑制 PC-3 细胞集落形成[1]。Tubulin/HDAC-IN-4 (0.2、1、5、25 µM) 抑制微管蛋白聚合，IC50值为 4.82 µM[1]。Tubulin/HDAC-IN-4（0.08、0.16、0.32；24 h）可增加 PC-3 细胞中 Ac-α-tubulin 和 Ac-Histone H3 的表达[1]。Tubulin/HDAC-IN-4（0.08、0.16、0.32 µM；24 小时）诱导细胞凋亡和 G2/M 期细胞周期停滞[1]。Tubulin/HDAC-IN-4（0.08、0.16、0.32 µM；24 小时）可诱导细胞内 ROS 水平显着升高[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tubulin/HDAC-IN-4 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | Tubulin/HDAC-IN-4 (10, 20 mg/kg; i.v.; every two days for 21 days) 显示出抗癌活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C24H26N2O6 |
| Molar Mass | 438.47 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Shanshan Xie, et al. Design and biological evaluation of dual tubulin/HDAC inhibitors based on millepachine for treatment of prostate cancer. European Journal of Medicinal Chemistry. 2024, 268(15): 116301. |