Thapsigargin

Catalog No.S7895

For research use only.

Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.

Thapsigargin Chemical Structure

CAS No. 67526-95-8

Selleck's Thapsigargin has been cited by 7 Publications

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Biological Activity

Description Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.
Targets
SERCA [1]
()
In vitro

In human SH-SY5Y neuroblastoma cells, two distinct intracellular Ca2+ stores, a KCl-/caffeine-sensitive and a carbachol-/IP3-sensitive store, are demonstrated previously. Thapsigargin (0.05 nM–20 μM) induces a [Ca2+]i-transient. Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50 = 0.353 nM) or without (IC50 = 0.448 nM) a KCl-prestimulation.[1] Thapsigargin is effective in inducing Endoplasmic Reticulum (ER) stress in hepatocytes.[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HeLaS3 MVnGeY5kfGmxbjDhd5NigQ>? MY[xJJVO MX3JcoR2[3Srb36gc4YhS2F{KzDy[Yxm[XOnIH\yc40h\W6mb4DsZZNucWNicnX0bYN2dHWvIHnueI8h[3m2b4PvcEBqdiCqdX3hckBJ\UyjU{OgZ4VtdHNiYYSgNUB2VSCkeTDmeZJiNTJxQV2tZoF{\WRic4DlZ5Rzd2[udX;yc41mfHKrYzDhcoFtgXOrcx?= M4OzSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEK4PFc{Lz5{NkSyPFg4OzxxYU6=
In vivo

TG at a dose of 0.5 ug/g/body weight is safe and does not elicit any adverse effects on survival in mice. TG treatment in mice results in significant expression of ER stress markers ATF6 and eIF2α in adipose tissue. TG treatment in mice fails to induce the expression of most ER stress and UPR proteins in the liver.[3]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Human SH-SY5Y neuroblastoma cells
  • Concentrations: 0.05 nM–20 μM
  • Incubation Time: 5 min
  • Method:

    The TG-treatment is conducted in several different modes as follows: (1) Applied prior to any stimulus: After a 5-min preincubation with 1.5 mM CaCl2, TG in different concentrations (0.05 nM–20 μM) is added to the cell suspension and the mixture is then incubated for further 5 min at 37 ℃. Stimulation starts with 100 mM KCl followed by 1 mM CAB or vice versa. (2) Applied between two stimuli: TG is added to cell suspension after the Ca2+-transient evoked by the first stimulant (100 mM KCl or 1 mM CAB) has reached its steady state. 5 min after the TG-addition, cells are then challenged for the second time by 1 mM CAB or 100 mM KCl. (3) Applied briefly after the first (KCl- or CAB-) stimulation: In this treatment mode, TG is added briefly ( ~ 10 s) after the first stimulant (100 mM KCl or 1 mM CAB) is applied, before the evoked [Ca2+]i-transient reaches a new steady state. The second stimulant (1 mM CAB or 100 mM KCl) is then applied 5 min after the TG-addition. (4) Applied briefly after the second stimulation: In the CAB→KCl stimulation mode, TG is added briefly ( ~ 10 s) after the second stimulant, i.e. 100 mM KCl.

  • (Only for Reference)
Animal Research:

[3]

  • Animal Models: Male Balb/c mice
  • Dosages: 0.5 mg/kg
  • Administration: IP
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(153.66 mM)
Water 100 mg/mL
(153.66 mM)
Ethanol 100 mg/mL
(153.66 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 650.75
Formula

C34H50O12

CAS No. 67526-95-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCCCCC(=O)OC1C2C(=C(C1OC(=O)C(=CC)C)C)C3C(C(CC2(C)OC(=O)C)OC(=O)CCC)(C(C(=O)O3)(C)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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