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Tunicamycin

现货
Catalog No.
B7417
抗生素,抑制GlcNAc磷酸转移酶(GPT)
组合的产品项目
规格价格库存 数量
5mg
¥ 988.00
Ship with 10-15 days
10mg
¥ 1,482.00
Ship with 10-15 days

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Background

Tunicamycin (TCM or TM) [1] [2] is an antibiotic. It can block the reaction between UDP-N-acetylglucosamine and dolichol phosphate in the first step of glycoprotein synthesis and thus inhibit the synthesis of all N-linked glycoproteins, finally cause endoplasmic reticulum (ER) stress [3]. In Bacillus subtilis cells, the IC50 for TCM to inhibit the formation of dolichyl pyrophosphoryl N-acetylglucosamine (Dol-p-p-GlcNAc) is 0.03 μg/ml [2].

The ER stress response is a potent, evolutionarily conserved response to cellular metabolic stress and misfolded proteins. ER stress is induced by disruption of ER functions, such as transport to the Golgi complex or protein glycosylation, or by disturbances in the ER lumen environment, such as redox status or altered calcium homeostasis [3].

In RAW264.7 cells, tunicamycin significantly reduced LPS-induced nitrite release/production and attenuated the expression of mRNAs and hence proteins of COX-2 and iNOS. In addition, tunicamycin at a concentration of 0.5 μg/ml did not have any effect on cell survival/proliferation, but at 48h tunicamycin provided protection against activation-induced macrophage cell death. In a concentration-dependent manner, tunicamycin reduced COX-2 and iNOS protein expressions in response to LPS and induced a concurrent increase in 78-kDa glucose-regulated protein (GRP78), an ER chaperone [3].

In the small intestine of wild-type mice, tunicamycin elevated expression levels of suppressed 1370 probes and 1291 probes by >2 fold. In the small intestine of Nrf 2 (-/-) mice, tunicamycin inhibited 2024 probes and induced 3471 probes by >2 fold. Compared with results of small intestine samples, in wild-type mice liver, less well-defined genes were either suppressed (943) or elevated (750) >2 fold by tunicamycin; whereas in Nrf2 (-/-) mice liver, 3170 genes were inhibited or 39 well-defined genes were induced [1].

Reference:
[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-κB and c-Junactivity via a mechanism that is independent of ER-stress and N-glycosylation. European Journal of Pharmacology, 2013, 721: 294-300.

文献引用

1. 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
2. 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

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt844.95
Cas No.11089-65-9
FormulaC39H64N4O16 (tunicamycin C, n=10)
Solubility≥25mg/mL in DMSO
SDFDownload SDF
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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

质量控制和MSDS

批次:

化学结构

Tunicamycin

相关生物数据

Tunicamycin

相关生物数据

Tunicamycin