Overview

Cat #: T-650

Lyophilized Powder yes

Origin Thapsia garganica.

Source Natural

MW: 650.7

Purity: >99% (HPLC)

Effective concentration 50 nM - 1 μM.

Structure

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

References-Activity

Rodriguez-Lopez, A.M. et al. (1999) Cell Physiol. Biochem. 9, 285.
Wei, H. et al. (1998) J. Neurochem. 70, 2305.
Waring, P. and Beaver, J. (1996) Exp. Cell. Res. 227, 264.
Jackson, T.R. et al. (1988) Biochem. J. 253, 81.

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.

Our bioassay

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.
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.
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).
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.

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.¹²Its tumour-promoting function probably results, at least partly, from cytotoxicity, causing a wound response in the skin.¹³The 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

Lyophilized Powder

Image & Title

Alomone 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.

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Thapsigargin

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