1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    Apoptosis
  2. Calcium Channel
    Apoptosis
  3. Thapsigargin

Thapsigargin (Synonyms: Thapsigargin (TG))

Cat. No.: HY-13433 Purity: 99.28%
Handling Instructions

Thapsigargin is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin is a well characterized Endoplasmic Reticulum (ER) stress inducing agent.

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

Thapsigargin Chemical Structure

Thapsigargin Chemical Structure

CAS No. : 67526-95-8

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1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

Thapsigargin is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin is a well characterized Endoplasmic Reticulum (ER) stress inducing agent[1][2][3][4].

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].

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; 0.25ug/g, 0.5ug/g and 1ug/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].

Animal Model: Male Balb/c mice (20-25g) [4]
Dosage: 0.25ug/g, 0.5ug/g and 1ug/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

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (384.17 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.28%

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