Background
Thapsigargin is a cell-permeable sesquiterpene lactone derived from the plant Thapsia garganica that acts as a tumor promoter in mammalian cells (1,2). Studies show that thapsagargin causes a rapid increase in cytosolic Ca2+ concentrations via discharge of intracellular Ca2+ stores. Research indicates that this increase in cytosolic calcium results from the specific inhibition of endoplasmic reticulum Ca2+-ATPases (IC50 = ~30 nM), and does not involve the hydrolysis of inositol phospholipids or protein kinase C (1,2). This disruption of calcium homeostasis is widely used in research studies to induce ER stress. Conflicting information regarding the role of thapsigargin in autophagy has been reported, but recent evidence points to thapsigargin inhibiting autophagy by blocking autophagosome fusion with lysosomes (3-5).
Molecular Formula
C34H50O12
Molecular Weight
650.8 g/mol
Purity
>98%
CAS
67526-95-8
Solubility
Soluble in DMSO at 65mg/ml and EtOH at 20mg/ml.
Storage
Directions for Use
Thapsigargin is supplied as a lyophilized powder. For a 1.25 mM stock, reconstitute the 1 mg in 1.23 ml DMSO. Working concentrations and length of treatments vary depending on the desired effect, but it is typically used at 2-2000 nM for 0.5-24 hours.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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