1. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection Apoptosis
  2. Calcium Channel SARS-CoV Apoptosis
  3. Thapsigargin

Thapsigargin 

Cat. No.: HY-13433 Purity: 99.78%
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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.

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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5 mg USD 280 In-stock
10 mg USD 450 In-stock
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50 mg USD 1450 In-stock
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Customer Review

Based on 41 publication(s) in Google Scholar

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Thapsigargin

WB

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    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

    Appearance

    Solid

    Formula

    C34H50O12

    CAS No.
    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)

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

      Add each solvent one by one:  10% DMSO    90% Saline

      Solubility: 5 mg/mL (7.68 mM); Suspended solution; Need ultrasonic

    • 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

    • 3.

      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 available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

    References
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    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.

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    Product Name:
    Thapsigargin
    Cat. No.:
    HY-13433
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