Thapsigargin

Product details

• 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.
• CAS number: 67526-95-8
• Molecular formula: C34H50O12.
• Purity: >99% (HPLC)
• Concentration: 50 nM - 1 μM.
• Form: Lyophilized Powder
• Solubility: DMSO, ethanol or acetone. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: DMSO, ethanol or acetone. Centrifuge all product preparations before use (10000 x g 5 min).
• Shipping: 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.
• Target: SERCA
• Source: Natural
• 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

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

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

Cited application(s)

Electrophysiology

• SDS (PDF)

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