Thapsigargin

Name: Thapsigargin
Brand: MedChemExpress
SKU: HY-13433
Rating: 5.0 (85 reviews)

Cat. No.: HY-13433 Purity: 99.87%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Thapsigargin Chemical Structure

CAS No. : 67526-95-8

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 85 publication(s) in Google Scholar

81 Publications Citing Use of MCE Thapsigargin

RT-PCR

: Thapsigargin purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 30;9(1):367. [Abstract]; Tunicamycin (0.1 μM; 18 h) doesn't decrease the mRNA levels of Irf2bp2 in LPS-stimulated macrophages.

: Thapsigargin purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 30;9(1):367. [Abstract]; Tunicamycin (0.1 μM; 18 h) significantly reduces the protein abundance of IRF2BP2 in LPS-stimulated macrophages in a BiP-dependent manner.

: Thapsigargin purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]; Thapsigargin (10 nM) increases p-PERK, p-eIF2α, and ATF4 expressions as well as CD8+ T cell death and dysfunction in human CD8+ T cells.

: 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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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Ca²⁺-ATPase^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF S-180	IC₅₀	30 nM Compound: 3; TPG	Cytotoxicity against mouse CCRF S-180 cells incubated for 48 hrs by sulforhodamine B staining based ELISA Cytotoxicity against mouse CCRF S-180 cells incubated for 48 hrs by sulforhodamine B staining based ELISA	[PMID: 33289552]
CCRF-CEM	IC₅₀	0.27 μM Compound: 6	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
EL4	IC₅₀	0.1 μM Compound: 3; TPG	Cytotoxicity against mouse EL4 cells incubated for 48 hrs by sulforhodamine B staining based ELISA Cytotoxicity against mouse EL4 cells incubated for 48 hrs by sulforhodamine B staining based ELISA	[PMID: 33289552]
EL4	IC₅₀	1.4 μM Compound: thapsigargin	Cytotoxicity against mouse EL4 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against mouse EL4 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25951057]
HL-60	IC₅₀	0.007 μM Compound: 6	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
K562	IC₅₀	0.17 μM Compound: 6	Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
MCF7	IC₅₀	2.3 μM Compound: 3; TPG	Cytotoxicity against human MCF7 cells incubated for 48 hrs by sulforhodamine B staining based ELISA Cytotoxicity against human MCF7 cells incubated for 48 hrs by sulforhodamine B staining based ELISA	[PMID: 33289552]
MCF7	IC₅₀	2.7 μM Compound: thapsigargin	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25951057]
MCF7	GI₅₀	5 μM Compound: Thapsigargin	Cytotoxicity against human MCF7 cells after 24 hrs by CellTiter-Glo assay Cytotoxicity against human MCF7 cells after 24 hrs by CellTiter-Glo assay	[PMID: 30528127]
PC-3	IC₅₀	2.4 μM Compound: thapsigargin	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25951057]

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.

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.

Molecular Weight

650.75

Formula

C₃₄H₅₀O₁₂

CAS No.

67526-95-8

Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCC(O[C@@H]1[C@@H](OC(/C(C)=C\C)=O)C(C)=C2[C@@]1([H])[C@@](C)(OC(C)=O)C[C@H](OC(CCC)=O)[C@@]([C@@]3(O)C)(O)[C@@]2([H])OC3=O)=O

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-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)

Solvent & Solubility

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

Concentration Solvent Mass	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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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
Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO 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
Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

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 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

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.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (284 KB) SDS (557 KB)

COA (255 KB) HNMR (297 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Help & FAQs

Do most proteins show cross-species activity?
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.

Keywords:

Thapsigargin67526-95-8Calcium ChannelSARS-CoVApoptosisCa2+ channelsCa channelsSARS coronavirusERstresscoronavirusunfoldedprotein ,responseInhibitorinhibitorinhibit

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Thapsigargin

Customer Review

Thapsigargin Related Antibodies

81 Publications Citing Use of MCE Thapsigargin

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•Related Screening Libraries:

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View All Calcium Channel Isoform Specific Products:

Biological Activity

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References

Customer Review

Thapsigargin Related Antibodies

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Complete Stock Solution Preparation Table

Thapsigargin Related Classifications

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