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Tunicamycin

Tunicamycin 是一种抗生素的混合物,通过阻断 GlcNAc 磷酸转移酶 (GPT),抑制 N-连接糖基化。Tunicamycin 具有抗肿瘤活性,还具有抗细菌、抗真菌和抗病毒活性。

CAS号

11089-65-9

分子式

C39H64N4O16

主要靶点

Influenza Virus|Antibacterial|Antifungal|Antibiotic

仅限科研使用

Cat No : CM06925

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Synonyms

ATF6|Bacterial|anti-cancer|Antibiotic|antiFungal|DNA|glycoprotein|Fungal|invasion|Influenza virus|InfluenzaVirus|inhibit|Inhibitor|N-linked|XBP-1|synthesis|Tunicamycin|衣霉素|UDP-HexNAc



产品信息

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.

CAS号 11089-65-9
分子式 C39H64N4O16
主要靶点 Influenza Virus|Antibacterial|Antifungal|Antibiotic
主要通路 微生物学|微生物学|微生物学|微生物学
分子量 844.94 (n=10)
纯度 98.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 ATF6|Bacterial|anti-cancer|Antibiotic|antiFungal|DNA|glycoprotein|Fungal|invasion|Influenza virus|InfluenzaVirus|inhibit|Inhibitor|N-linked|XBP-1|synthesis|Tunicamycin|衣霉素|UDP-HexNAc

靶点活性

Phospho-N-acetylmuramyl-pentapeptide transferase (MraY):0.31 µM

体内活性

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]

体外活性

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]

溶解度

DMSO:14.37 mg/mL;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL

参考文献

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.

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