Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.
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Thapsigargin Chemical Structure
CAS No. : 67526-95-8
This product is a controlled substance and not for sale in your territory.
Based on 61 publication(s) in Google Scholar
Thapsigargin purchased from MedChemExpress. Usage Cited in:
Microbiol Spectr. 2022 Nov 15;e0328222.
[Abstract]
Both PK-15 and 3D4/21cells are transfected with MGF110-7L-expressing plasmids with an increasing dose or empty vector and treated with Thapsigargin (TG) as positive controls. TG significant increases the levels of phosphorylated eIF2a (P-eIF2a) and ATF4 protein in the cells.
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Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types[1][2][3][4][5].
IC50 & Target
Ca2+-ATPase[1]
In Vitro
Thapsigargin (0.001- 1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner[2].
Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner[2].
Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells[2].
Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes[1].
Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC50=4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca2+]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation[3].
Thapsigargin also phosphorylate p38 MAPK by Ca2+ influx through SOCE, leading to suppression of TNF-α-induced NF-κB phosphorylation[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Thapsigargin Related Antibodies
Cell Proliferation Assay[2]
Cell Line:
MH7A human rheumatoid arthritis synovial cells
Concentration:
0.001, 0.1, and 1 μM
Incubation Time:
For 2 and 4 days
Result:
Arrested cell proliferations in a time- and dose-dependent manner.
Apoptosis Analysis[2]
Cell Line:
MH7A human rheumatoid arthritis synovial cells
Concentration:
0.001, 0.1, and 1 μM
Incubation Time:
For 2 and 4 days
Result:
Induces cell apoptosis in a time- and dose-dependent manner.
Western Blot Analysis[2]
Cell Line:
MH7A human rheumatoid arthritis synovial cells
Concentration:
0.001, 0.1, and 1 μM
Incubation Time:
For 2 and 4 days
Result:
Impairs mTOR activity and leads to cyclin D1 expressions
In Vivo
Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Balb/c mice (20-25 g)[4]
Dosage:
0.25 ug/g, 0.5 ug/g and 1 ug/g
Administration:
Injection; 24 hours
Result:
Increased of 2 to 5-fold in chemokine and pro-inflammatory expression.
Room temperature in continental US; may vary elsewhere.
Stockage
-20°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (76.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.5367 mL
7.6834 mL
15.3669 mL
5 mM
0.3073 mL
1.5367 mL
3.0734 mL
10 mM
0.1537 mL
0.7683 mL
1.5367 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% Saline
Solubility: 5 mg/mL (7.68 mM); Suspended solution; Need ultrasonic
Protocol 2
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Geiszt M, et al. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Biochem J. 1995 Jan 15;305 ( Pt 2):525-8.
[Content Brief]
[2]. Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014 Feb 9;2014:605416.
[Content Brief]
[3]. Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004 Jun 18;1011(2):177-86.
[Content Brief]
[4]. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.
[Content Brief]
[5]. Mohammed Samer Shaban, et al. Inhibiting coronavirus replication in cultured cells by chemical ER stress. bioRxiv 2020.08.26.266304;
[6]. Junsuke Uwada, et al. Store-operated calcium entry (SOCE) contributes to phosphorylation of p38 MAPK and suppression of TNF-α signalling in the intestinal epithelial cells. Cell Signal. 2019 Nov;63:109358.
[Content Brief]
[1]. Geiszt M, et al. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Biochem J. 1995 Jan 15;305 ( Pt 2):525-8.
[2]. Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014 Feb 9;2014:605416.
[3]. Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004 Jun 18;1011(2):177-86.
[4]. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.
[5]. Mohammed Samer Shaban, et al. Inhibiting coronavirus replication in cultured cells by chemical ER stress. bioRxiv 2020.08.26.266304;
[6]. Junsuke Uwada, et al. Store-operated calcium entry (SOCE) contributes to phosphorylation of p38 MAPK and suppression of TNF-α signalling in the intestinal epithelial cells. Cell Signal. 2019 Nov;63:109358.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
1.5367 mL
7.6834 mL
15.3669 mL
38.4172 mL
5 mM
0.3073 mL
1.5367 mL
3.0734 mL
7.6834 mL
10 mM
0.1537 mL
0.7683 mL
1.5367 mL
3.8417 mL
15 mM
0.1024 mL
0.5122 mL
1.0245 mL
2.5611 mL
20 mM
0.0768 mL
0.3842 mL
0.7683 mL
1.9209 mL
25 mM
0.0615 mL
0.3073 mL
0.6147 mL
1.5367 mL
30 mM
0.0512 mL
0.2561 mL
0.5122 mL
1.2806 mL
40 mM
0.0384 mL
0.1921 mL
0.3842 mL
0.9604 mL
50 mM
0.0307 mL
0.1537 mL
0.3073 mL
0.7683 mL
60 mM
0.0256 mL
0.1281 mL
0.2561 mL
0.6403 mL
Thapsigargin Related Classifications
InfectionCancer
Cancer Targeted TherapyCancer ImmunotherapyCancer Metabolism and Metastasis
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.