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Thapsigargin

Catalog No.
B6614
sarco-endoplasmic reticulum Ca2+-ATPases inhibitor
Grouped product items
SizePriceStock Qty
1mg
$68.00
In stock
5mg
$275.00
Ship with 5-10 days
10mg
$502.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

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:

[1].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.

[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]. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.

Product Citation

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at -20°C
M.Wt650.76
Cas No.67526-95-8
FormulaC34H50O12
SolubilitySoluble in DMSO
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
SDFDownload SDF
Canonical SMILESO[[email protected]@]([[email protected]]1OC(CCC)=O)([[email protected]]2(C)O)[[email protected]](C([[email protected]]([[email protected]@H]3OC(CCCCCCC)=O)[[email protected]@](C1)(C)OC(C)=O)=C(C)[[email protected]@H]3OC(/C(C)=C\C)=O)OC2=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1,2]:

Cell lines

NG115-401L neural cell line, isolated rat hepatocytes

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

ED50: ~20 nM (NG115-401L neural cell line); ED50 ~80 nM (isolated rat hepatocytes)

Applications

Thapsigargin stimulated a rapid (within 15 s) transient increase in intracellular [Ca2+] in the NG115-401L neural cell line with the ED50 of around 20 nM. In isolated rat hepatocytes, Thapsigargin increased [Ca2+] in a rapid and dose-dependent manner, with an ED50 value of ~80 nM.

Animal experiment [3]:

Animal models

Male C57BL/6 mice with transient middle cerebral artery occlusion (tMCAO)

Dosage form

IC50: 2 to 20 ng, icv injection

Application

Thapsigargin dose-dependently reduced the brain infarct. Thapsigargin (TG) protected mice against ischemia-reperfusion-induced brain injury.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

Quality Control

Quality Control & MSDS

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Chemical structure

Thapsigargin

Related Biological Data

Thapsigargin

Related Biological Data

Thapsigargin

Related Biological Data

Thapsigargin