Tunicamycin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tunicamycin（TCM或TM）[1] [2]是一种抗生素，可阻断糖蛋白合成第一步中UDP-N-乙酰葡糖胺和多萜醇磷酸之间的反应，从而抑制所有N-连糖蛋白的合成，最终引起内质网（ER）应力[3]。在枯草芽孢杆菌细胞中，TCM抑制多萜醇基焦磷酸N-乙酰氨基葡糖（Dol-p-p-GlcNAc）的形成，IC50值为0.03 μg/ml[2]。
内质网应激反应是一种有效的和进化上保守的反应，对细胞内的代谢应激和错误折叠蛋白做出反应。ER功能的破坏（如向高尔基复合体的运输或蛋白糖基化）或ER腔环境的干扰（如氧化还原状态或钙稳态的改变）可诱导ER应激[3]。
在RAW264.7细胞中，tunicamycin显著减少LPS诱导的亚硝酸盐释放/产生，衰减COX-2和iNOS mRNAs的表达，从而减少其蛋白水平。此外，tunicamycin在0.5 μg/ml浓度时对细胞存活/增殖没有任何影响，但在48 h时，tunicamycin保护激活诱导的巨噬细胞死亡。Tunicamycin以浓度依赖的方式减少LPS诱导的COX-2和iNOS蛋白的表达，同时诱导78-kDa葡萄糖调节蛋白（GRP78）的增加，GRP78是ER的分子伴侣[3]。
在野生型小鼠的小肠中，tunicamycin增加了2倍以上的抑制性1370探针和1291探针的表达水平。在Nrf 2（-/-）小鼠的小肠中，tunicamycin抑制2倍以上的2024探针，而诱导3471探针。与小肠样本的结果相比，在野生型小鼠肝脏中，tunicamycin导致缺乏明确定义的基因超过两倍的抑制（943）或升高（750）。而在Nrf 2（-/-）小鼠的肝脏中，3170被抑制，而39个良好定义的基因被诱导[1]。
参考文献：
[1]. Sujit Nair, Changjiang Xu, Guoxiang Shen, et al. Toxicogenomics of Endoplasmic Reticulum stress inducer Tunicamycin in the Small Intestine and Liver of Nrf2 Knockout and C57BL/6J Mice. Toxicol Lett., 2007, 168(1):21-39.
[2]. Masatoshi Inukai, Fujio Isono and Akira Takatsuki. Selective Inhibition of the Bacterial Translocase Reaction in Peptidoglycan Synthesis by Mureidomycins. Antimicrobial Agents and Chemotherapy, 1993, 37(5): 980-983.
[3]. Song-YiKim, Ji-SunHwang and Inn-OcHan. Tunicamycin inhibits Toll-like receptor-activated inflammation in RAW264.7 cells by suppression of NF-魏B and c-Junactivity via a mechanism that is independent of ER-stress and N-glycosylation. European Journal of Pharmacology, 2013, 721: 294-300.
- 1. Yongzhang Liu, Linhua Lan, et al. "N-glycosylation stabilizes MerTK and promotes hepatocellular carcinoma tumor growth." Redox Biol. 2022 Aug;54:102366. PMID: 35728303
- 2. Jinrui Zhang, Ge Zhang, et al. "Loss of RBMS1 promotes anti-tumor immunity through enabling PD-L1 checkpoint blockade in triple-negative breast cancer." Cell Death Differ. 2022 May 10. PMID: 35538152
- 3. Yiyang Zhao, Linkang He, et al. "2-Hydroxypropyl-β-cyclodextrin Regulates the Epithelial to Mesenchymal Transition in Breast Cancer Cells by Modulating Cholesterol Homeostasis and Endoplasmic Reticulum Stress." Metabolites. 2021 Aug 23;11(8):562. PMID: 34436503
- 4. KE PENG, AIQIN SUN, et al. "Restoration of the ATG5‑dependent autophagy sensitizes DU145 prostate cancer cells to chemotherapeutic drugs." Oncol Lett. 2021 Sep;22(3):638. PMID: 34386060
- 5. Yanan Li, Chaorong Wang, et al. "Discovery of a small molecule inhibitor of cullin neddylation that triggers ER stress to induce autophagy." Acta Pharmaceutica Sinica B.
- 6. Peng Wang, Li-Na Jiang, et al. "Estradiol-induced inhibition of endoplasmic reticulum stress normalizes splenic CD4 + T lymphocytes following hemorrhagic shock." Sci Rep. 2021 Apr 5;11(1):7508. PMID: 33820957
- 7. Fei Wu , Rumin Zhang, et al. "(-)-Clausenamide alleviated ER stress and apoptosis induced by OGD/R in primary neuron cultures." Neurol Res. 2020 Sep;42(9):730-738. PMID: 32588767
- 8. Xu H, Liu P, et al. "FKBP9 promotes the malignant behavior of glioblastoma cells and confers resistance to endoplasmic reticulum stress inducers." J Exp Clin Cancer Res. 2020;39(1):44. Published 2020 Feb 28. PMID: 32111229
- 9. Qin W, Wu X, et al. "Suhuang antitussive capsule inhibits NLRP3 inflammasome activation and ameliorates pulmonary dysfunction via suppression of endoplasmic reticulum stress in cough variant asthma." Biomed Pharmacother. 2019 Jul 14;118:109188. PMID: 31315072
- 10. Jia B, Wang Y, et al. "Naringenin ameliorates insulin resistance by modulating endoplasmic reticulum stress in hepatitis C virus-infected liver." Biomed Pharmacother. 2019 Jul;115:108848. PMID: 31039496
- 11. Chou CK, Liu W, et al. "Ethyl Acetate Extract of Scindapsus cf. hederaceus Exerts the Inhibitory Bioactivity on Human Non-Small Cell Lung Cancer Cells through Modulating ER Stress." Int J Mol Sci. 2018 Jun 21;19(7). pii: E1832. PMID: 29933620
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 844.95 |
| Cas No. | 11089-65-9 |
| Formula | C39H64N4O16 (tunicamycin C, n=10) |
| Solubility | ≥25 mg/mL in DMSO |
| SDF | Download SDF |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
RAW264.7细胞系 |
|
溶解方法 |
在DMSO中的溶解度>25 mg/mL。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应时间 |
48 h，0.5 μg/mL |
|
应用 |
在RAW264.7细胞中，tunicamycin显著减少LPS诱导的亚硝酸盐释放/产生，减少COX-2和iNOS mRNAs的表达，从而减少其蛋白水平。此外，tunicamycin在0.5 μg/ml浓度时对细胞存活/增殖没有任何影响，但在48 h时，tunicamycin保护活化诱导的巨噬细胞死亡。Tunicamycin以浓度依赖的方式减少LPS诱导的COX-2和iNOS蛋白的表达，同时诱导78-kDa葡萄糖调节蛋白（GRP78）的增加，GRP78是内质网的分子伴侣。 |
| 动物实验[2]： | |
|
动物模型 |
野生型C57BL/6J Nrf2 (+/+)小鼠 和 C57BL/6J/Nrf2(-/-) 小鼠 |
|
剂量 |
口服，浓度为2 mg/kg（溶解在50% PEG 400水溶液中），给药3小时后处死小鼠。 |
|
应用 |
在野生型小鼠的小肠中，tunicamycin增加1370个探针的表达，抑制1291个探针的表达，均2倍以上。在Nrf 2(-/-)小鼠的小肠中，tunicamycin抑制2024个探针的表达，并诱导3471个探针的表达，均2倍以上。与小肠样本的结果相比，在野生型小鼠肝脏中，tunicamycin使缺乏明确定义的基因被抑制（943个）或增加（750个），均2倍以上。在Nrf 2(-/-)小鼠的肝脏中，3170个基因被抑制，同时39个明确定义的基因被诱导。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Song-YiKim, Ji-SunHwang and Inn-OcHan. Tunicamycin inhibits Toll-like receptor-activated inflammation in RAW264.7 cells by suppression of NF-κB and c-Jun activity via a mechanism that is independent of ER-stress and N-glycosylation. European Journal of Pharmacology, 2013, 721: 294-300. [2] Sujit Nair, Changjiang Xu, Guoxiang Shen, et al. Toxicogenomics of Endoplasmic Reticulum stress inducer Tunicamycin in the Small Intestine and Liver of Nrf2 Knockout and C57BL/6J Mice. Toxicol Lett., 2007, 168(1):21-39. |
|
质量控制和MSDS
- 批次:
-
纯度 ≥ 95% (mixture of congeners)
- COA (Certificate Of Analysis)
- HPLC
- MSDS (Material Safety Data Sheet)
- Datasheet
化学结构
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