Thapsigargin
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.
Thapsigargin is an inhibitor of microsomal Ca2+-ATPase, Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with IC50 value of 0.353 nM [1].
Thapsigargin may induce cell apoptosis in MH7A cells in a time- and dose-dependent manner, and the percentages of cell death reached 44.6% at thapsigargin concentration of 1 μM treated for 4 days compared to the control. The protein and mRNA levels of cyclin D1 decreased gradually with the increasing of thapsigargin concentration and treatment times [2].
In regards to vivo results, tunicamycin is superior in not only inducing ER stress but also recapturing the metabolic alterations associated with ER stress [3].
References:
[3]. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.
- 1. Nana Yan, Yongqiang Wang, et al. "Stromal Interaction Molecule 1 Promotes the Replication of vvIBDV by Mobilizing Ca2+ in the ER." Viruses. 2022 Jul 13;14(7):1524. PMID: 35891504
- 2. 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
- 3. 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
- 4. 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
- 5. 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 | Desiccate at -20°C |
M.Wt | 650.76 |
Cas No. | 67526-95-8 |
Formula | C34H50O12 |
Solubility | ≥39.2 mg/mL in DMSO; ≥24.8 mg/mL in EtOH; ≥4.12 mg/mL in H2O with ultrasonic |
Chemical Name | (3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-acetoxy-4-(butyryloxy)-3,3a-dihydroxy-3,6,9-trimethyl-8-(((Z)-2-methylbut-2-enoyl)oxy)-2-oxo-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-7-yl octanoate |
SDF | Download SDF |
Canonical SMILES | O[C@@]([C@H]1OC(CCC)=O)([C@]2(C)O)[C@H](C([C@H]([C@@H]3OC(CCCCCCC)=O)[C@@](C1)(C)OC(C)=O)=C(C)[C@@H]3OC(/C(C)=C\C)=O)OC2=O |
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 [1,2]: | |
细胞系 |
NG115-401L神经细胞系,分离大鼠肝细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37°C下孵育10分钟,随后在超声波浴中摇匀。-20°C以下可储存数月。 |
反应条件 |
ED50: ~20 nM (NG115-401L神经细胞系); ED50:~80 nM(大鼠肝细胞) |
应用 |
在NG115-401L神经细胞系中,Thapsigargin刺激细胞内[Ca2+]的快速瞬时增加(15秒内),ED50约为20 nM。在分离的大鼠肝细胞中,Thapsigargin以快速和剂量依赖的方式增加[Ca2+],ED50值约为80 nM。 |
动物实验 [3]: | |
动物模型 |
伴有短暂大脑中动脉闭塞(tMCAO)的雄性C57BL/6小鼠 |
给药剂量 |
IC50: 2-20 ng,脑室内注射 |
应用 |
Thapsigargin以剂量依赖性方式减少脑梗塞。Thapsigargin保护小鼠免受缺血再灌注诱发的脑损伤。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Jackson T R, Patterson S I, Thastrup O, et al. A novel tumour promoter, thapsigargin, transiently increases cytoplasmic free Ca2+ without generation of inositol phosphates in NG115-401L neuronal cells[J]. Biochemical Journal, 1988, 253(1): 81-86. [2]. Thastrup O, Cullen P J, Drbak B K, et al. Thapsigargin, a tumor promoter, discharges intracellular Ca2+ stores by specific inhibition of the endoplasmic reticulum Ca2 (+)-ATPase[J]. Proceedings of the National Academy of Sciences, 1990, 87(7): 2466-2470. [3]. Zhang X, Yuan Y, Jiang L, et al. Endoplasmic reticulum stress induced by tunicamycin and thapsigargin protects against transient ischemic brain injury: Involvement of PARK2-dependent mitophagy[J]. Autophagy, 2014, 10(10): 1801-1813. |
质量控制和MSDS
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