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Thapsigargin

Thapsigargin 属于天然产物，是一种肌/内质网 Ca2+ ATP 酶 (SERCA) 的抑制剂，也是一种内质网应激诱导剂。Thapsigargin 通过阻断细胞将钙泵入肌浆和内质网的能力来提高胞浆钙浓度。

CAS号

67526-95-8

分子式

C34H50O12

主要靶点

SARS-CoV|Apoptosis|Calcium Channel

仅限科研使用

Cat No : CM03067

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Synonyms

protein ,response|unfolded|stress|SARS-CoV|SARSCoV|SARS coronavirus|Thapsigargin|毒胡萝卜素|Apoptosis|coronavirus|Ca channels|Ca2+ channels|Ca2+-ATPase|Calcium Channel|CalciumChannel|Inhibitor|inhibit

验证数据展示

  • CAS No.: 67526-95-8

    Thapsigargin
    CAS#: 67526-95-8

产品信息

Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

CAS号 67526-95-8
分子式 C34H50O12
主要靶点 SARS-CoV|Apoptosis|Calcium Channel
主要通路 凋亡|微生物学|代谢|离子通道
分子量 650.75
纯度 99.22%， 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 Store at low temperature,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 protein ,response|unfolded|stress|SARS-CoV|SARSCoV|SARS coronavirus|Thapsigargin|毒胡萝卜素|Apoptosis|coronavirus|Ca channels|Ca2+ channels|Ca2+-ATPase|Calcium Channel|CalciumChannel|Inhibitor|inhibit

靶点活性

PC3 cells:2.4 μM|CCRF S-180 cells:30 nM|CCRF-CEM cells:0.27 μM|K562 cells:0.17 μM|MCF-7 cells:2.3 μM|HL-60 cells:0.007 μM|EL4 cells:0.1 μM

体内活性

方法：为检测体内诱导 ER 应激的活性，将 Thapsigargin (0.25-1 μg/g in 150 mM dextrose containing 1% DMSO) 单次腹腔注射给 Balb/c 小鼠。 结果：Thapsigargin 治疗导致脂肪组织中 ER 应激标记物 ATF6 和 eIF2α 的显著表达。Thapsigargin 治疗未能诱导肝脏中大多数 ER 应激和 UPR 蛋白的表达。[2] 方法：为研究在体内的抗病毒功能，将 Thapsigargin (30 ng/mouse) 灌胃给药给感染 PR8 病毒的 BALB/c 小鼠，每天一次，持续七天。 结果：小鼠口服 Thapsigargin 显著降低了严重程度和病毒脱落，并提高了致命流感病毒感染期间的存活率。[3]

体外活性

方法：人类风湿性关节炎滑膜细胞 MH7A 用 Thapsigargin (0.001-1 μM) 处理 2-4 天，使用 SRB 方法检测细胞增殖。 结果：Thapsigargin 以时间和剂量依赖的方式抑制 MH7A 细胞的增殖。[1] 方法：人肝癌细胞 HepG2 用 Thapsigargin (25-100 nM) 处理 24 h，使用 RT-qPCR 检测内质网应激/UPR 基因表达。 结果：Thapsigargin 治疗仅在 50 和 100 nM 的升高浓度下持续诱导ER应激基因表达。[2]

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.68 mM);DMSO:252.5 mg/mL (388.01 mM)

细胞实验

Cell Line: MH7A human rheumatoid arthritis synovial cells. Concentration: 0.001, 0.1, and 1?μM. Incubation Time: For 2 and 4 days [2]

动物实验

Animal Model: Male Balb/c mice (20-25g). Dosage: 0.25ug/g, 0.5ug/g and 1ug/g. Administration: Injection; 24 hours [4]

参考文献

1.Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovial cells. ScientificWorldJournal. 2014 Feb 9;2014:605416.
2.Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.
3.Goulding LV, et al. Thapsigargin at Non-Cytotoxic Levels Induces a Potent Host Antiviral Response that Blocks Influenza A Virus Replication. Viruses. 2020 Sep 27;12(10):1093.
4.Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.

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