| Description | Tunicamycin is a mixture of antibiotics that inhibit N-linked glycosylation by blocking GlcNAc phosphotransferase (GPT). Tunicamycin has antitumor activity, as well as anti-bacterial, anti-fungal, and anti-viral activity. |
| In vitro | 方法：人肝癌细胞 Hep3B 用 Tunicamycin (1 μg/mL)、camptothecin (3 μM)、etoposide (5 μM)、taxol (0.1 μM) 和 vincristine (0.1 μM) 处理 48 h，使用 Flow Cytometry 检测细胞死亡情况。结果：Tunicamycin 显著抑制 TOP 抑制剂（camptothecin 和 etoposide）引起的凋亡作用，但不抑制微管蛋白靶向药物（taxol 和 vincristine) 引起的凋亡。[1]方法：人肝癌细胞 PLC/PRF/5、MHCC-97L 和 MHCC-97H 用 Tunicamycin (2.5 μg/mL) 处理 24 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：在三种肝癌细胞系中，Tunicamycin 抑制 Akt 磷酸化。[2] |
| In vivo | 方法：为研究对肝脏能量代谢的影响，将 Tunicamycin (1 mg/kg) 单次腹腔注射给 C57BL/6 小鼠。结果：Tunicamycin 可显著诱导肝脏呈黄色和内质网应激，并提高血清天冬氨酸转氨酶和丙氨酸转氨酶水平。Tunicamycin 通过增加甘油三酯积累和降低糖原含量来改变肝脏能量稳态。[3]方法：为检测体内抗肿瘤活性，将 Tunicamycin (0.25 mg/kg) 口服给药给携带人三阴性乳腺癌肿瘤 MDA-MB-231 的 Balb/c (nu/nu) 小鼠，每周两次，持续四周。结果：在口服给予 Tunicamycin 的一周内，MDA-MB-231 肿瘤异种移植物减少 65% ，并且没有全身和/或器官衰竭。[4] |
| molecular weight | 844.94 (n=10) |
| Molecular formula | C39H64N4O16 |
| CAS | 11089-65-9 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 14.37 mg/mL (20 mM), Sonication is recommended. |
| References | 1. Hsu JL, et al. Tunicamycin induces resistance to camptothecin and etoposide in human hepatocellular carcinoma cells: role of cell-cycle arrest and GRP78. Naunyn Schmiedebergs Arch Pharmacol. 2009 Nov;380(5):373-82. 2. Hou H, et al. Tunicamycin potentiates cisplatin anticancer efficacy through the DPAGT1/Akt/ABCG2 pathway in mouse Xenograft models of human hepatocellular carcinoma. Mol Cancer Ther. 2013 Dec;12(12):2874-84. 3. Feng B, et al. Endoplasmic Reticulum Stress Inducer Tunicamycin Alters Hepatic Energy Homeostasis in Mice. Int J Mol Sci. 2017 Aug 4;18(8):1710. 4. Banerjee A, et al. Unfolded protein response is required in nu/nu mice microvasculature for treating breast tumor with tunicamycin. J Biol Chem. 2011 Aug 19;286(33):29127-29138. |