Thapsigargin

A Potent and Cell-Permeable Inhibitor of SERCA Pump Ca2+-ATPase/an Intracellular Ca2+ Mobilizer
    Cat #: T-650
  • Lyophilized Powder
  • Bioassay Tested
  • Origin Thapsia garganica.
    Source Natural
    MW: 650.7
    Purity: >99% (HPLC)
    Effective concentration 50 nM - 1 μM.
      • Thapsigargin
    Chemical name (3S,3aR,4S,6S,6AR,7S,8S,9bS)-6-(Acetyloxy)-2,3,3a,4,5,6 ,6a,7,8,9b-decahydro-3,3a-dihydroxy-3,6,9-trimethyl-8-[ [(2Z)-2-methyl-1-oxo-2-butenyl]oxy]-2-oxo-4-(1-oxobutox y)azuleno[4,5-b]furan-7-yl octanoate.
    Molecular formula C34H50O12.
    CAS No.: 67526-95-8.
    Activity Thapsigargin is a highly potent inhibitor of the sarco-endoplasmic reticulum Ca2+-ATPases (SERCAs), inhibiting Ca2+ pumping to intracellular stores at nanomolar concentrations, with IC50 ranging from 0.2 nM to 50 nM in various mammalian cell types.1 Thapsigargin-induced depletion of Ca2+ stores leads to apoptosis in various cell lines.2-4
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO, ethanol or acetone. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
      • Thapsigargin
        Alomone Labs Thapsigargin induces cytosolic Ca2+ increase in Jurkat cells.
        Cells were loaded with Fluo-3-AM dye in the presence of 5 mM EGTA. 20 nM Thapsigargin (#T-650) application induces a significant increase in intracellular Ca2+. Changes in intracellular Ca2+ were detected as changes in Fluo-3 fluorescent emission following the application (arrow) of control or Thapsigargin.
        Thapsigargin
        Alomone Labs Thapsigargin induces apoptosis in Jurkat cells.
        Cells were grown to 70% confluency. 1 μM Thapsigargin (#T-650) or vehicle was added for six hours. Cell extracts were then probed for cleaved Caspase 3 with specific antibodies.
        Thapsigargin
        Alomone Labs Thapsigargin increases intracellular Ca2+ by modulating  the autophosphorylation of CaMK II in 3T3-L1 cells. 
        Cells were starved for 2h and then stimulated with 1 or 5 µM Thapsigargin (#T-650) for the indicated times. The cell extracts were blotted and probed with an antibody for phospho-(Thr268)-CAMKII (Calmodulin dependent kinase II).
        Thapsigargin
        Alomone Labs Thapsigargin induces cytosolic Ca2+ increase in HEK 293 cells.
        Ca2+ traces from Fluo-3 AM loaded HEK 293 cells treated with 5 µM Thapsigargin (#T-650) in the presence of 5 mM EGTA.
    References - Scientific background
      • Thapsigargin, derived from the plant genus Thapsia,1-3 is an extremely tight-binding inhibitor of intracellular Ca2+ pumps. It was initially described as a tumor promoting agent which induces rapid Ca2+ release from intracellular stores4 by inhibition of the sarcoplasmic/endoplasmic reticulum Ca2+-dependent ATPase pump without inositol phosphate formation.5-7 The thapsigargin induced depletion of Ca2+ stores causes apoptosis in most cell lines.8-10 It has also been shown to cause histamine secretion from rat mast cells,11 and to stimulate arachidonic acid metabolism in macrophages.12 Its tumour-promoting function probably results, at least partly, from cytotoxicity, causing a wound response in the skin.13 The tumorogenic activity of thapsigargin might be due to its activation of protein kinase B (Akt) which subsequently stimulates MAP kinase signaling via Src and Raf-1.12,13
    Target SERCA
    Image & Title ThapsigarginAlomone Labs Thapsigargin decreases Ca2+ signals in rat mossy fibers.Rat hippocampal slices were incubated with 10 µM Thapsigargin (#T-650) for 60 min. The Ca2+ signals from mossy fiber terminals decreased significantly after wash-in.Adapted from Liang, Y. et al. (2002) J. Neurophysiol. 87, 1132. with permission of The American Physiological Society.
    Last update: 21/11/2019

    Thapsigargin (#T-650) is a highly pure, natural and biologically active compound.

    For research purposes only, not for human use
    Citations
      • Mouse α-cells (single cell).
        Dickerson, M.T. et al. (2019) Am. J. Physiol. 316, E646.
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