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Biological Activity for Thapsigargin
Thapsigargin is a potent inhibitor of sarco/endoplasmic reticulum Ca2+-ATPases (SERCA) that causes endoplasmic reticulum (ER) stress. Thapsigargin can be used to induce autophagy in mammalian cells. In vitro, thapsigargin blocks infection of immortilized and primary human cells with respiratory syncytial virus (RSV), SARS-CoV-2 and influenza A. Thapsigargin protects mice against lethal influenza A viral infection and reduces virus titres in the lungs of treated mice.
Technical Data for Thapsigargin
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Thapsigargin
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Thapsigargin
The following data is based on the product molecular weight 650.76. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.54 mL||7.68 mL||15.37 mL|
|5 mM||0.31 mL||1.54 mL||3.07 mL|
|10 mM||0.15 mL||0.77 mL||1.54 mL|
|50 mM||0.03 mL||0.15 mL||0.31 mL|
References for Thapsigargin
References are publications that support the biological activity of the product.
Davidson and Varhol (1995) Kinetics of thapsigargin-Ca2+-ATPase (sarcoplasmic reticulum) interaction reveals a two-step binding mechanism and picomolar inhibition. J.Biol.Chem. 270 11731 PMID: 7744817
Treiman et al (1998) A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases. TiPS 19 131 PMID: 9612087
Yu et al (1998) Specific substitutions at amino acid 256 of the sarcoplasmic/endoplasmic reticulum Ca2+ transport ATPase mediate resistance to thapsigargin in thapsigargin-resistant hamster cells. J.Biol.Chem. 273 3542 PMID: 9452480
Ding et al (2007) Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival. J.Biol.Chem. 282 4702 PMID: 17135238
Al-Beltagi et al (2021) Thapsigargin is a broad-Spectrum inhibitor of major human respiratory viruses: coronavirus, respiratory syncytial virus and influenza A virus. Viruses 13 234 PMID: 33546185
Goulding et al (2020) Thapsigargin at non-cytotoxic levels induces a potent host antiviral response that blocks influenza A virus replication. Viruses 12 1093 PMID: 32992478
If you know of a relevant reference for Thapsigargin, please let us know.
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Keywords: Thapsigargin, Thapsigargin supplier, Potent, inhibitors, inhibits, SERCA, ATPase, Ca2+, modulators, Ca2+-ATPase, Signaling, Signalling, Calcium-ATPase, P-type, Transporters, Ion, Pumps, Autophagy, Coronavirus, Influenza, Viruses, 1138, Tocris Bioscience
42 Citations for Thapsigargin
Citations are publications that use Tocris products. Selected citations for Thapsigargin include:
McEwan et al (2021) Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation Life Sci 283 119850 PMID: 34314735
Salzer et al (2016) Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels. Neuropharmacology 110 (A) 277 PMID: 27511837
Earls et al (2010) Dysregulation of presynaptic calcium and synaptic plasticity in a mouse model of 22q11 deletion syndrome. PLoS One 30 15843 PMID: 21106823
Kelm et al (2007) Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons. Cell Cycle 323 356 PMID: 17652632
Andrade-Talavera et al (2016) Presynaptic Spike Timing-Dependent Long-Term Depression in the Mouse Hippocampus. Cereb Cortex 26 3637 PMID: 27282393
Egawa et al (2013) Optogenetic probing and manipulation of the calyx-type presynaptic terminal in the embryonic chick ciliary ganglion. PLoS One 8 e59179 PMID: 23555628
Rojas et al (2013) Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors. Mol Pharmacol 83 106 PMID: 23066089
Shemorry et al (2019) Caspase-mediated cleavage of IRE1 controls apoptotic cell commitment during endoplasmic reticulum stress. Elife 8 e47084 PMID: 31453810
Glanowska and Moenter (2015) Differential regulation of GnRH secretion in the preoptic area (POA) and the median eminence (ME) in male mice. Neuropharmacology 156 231 PMID: 25314270
Florea et al (2017) Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma. Oncotarget 8 22876 PMID: 28206967
Soltoff and Lannon (2013) Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells. PLoS One 8 e72881 PMID: 24009711
Grassin-Delyle et al (2013) The expression and relaxant effect of bitter taste receptors in human bronchi. Respir Res 14 134 PMID: 24266887
Semenov et al (2013) Recruitment of the intracellular Ca2+ by ultrashort electric stimuli: the impact of pulse duration. Cell Calcium 54 145 PMID: 23777980
Varadarajan et al (2013) Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis. PLoS One 8 e56603 PMID: 23457590
Pinheiro et al (2013) Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation. Cell Commun Signal 11 70 PMID: 24047499
Moore et al (2009) Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors. Neuron 61 287 PMID: 19186170
Szikra et al (2009) Calcium homeostasis and cone signaling are regulated by interactions between calcium stores and plasma membrane ion channels. PLoS One 4 e6723 PMID: 19696927
Haeberle et al Swelling-activated Ca2+ channels trigger Ca2+ signals in Merkel cells. MBio 3 e1750 PMID: 18454189
Podszywalow-Bartnicka et al (2014) Downregulation of BRCA1 protein in BCR-ABL1 leukemia cells depends on stress-triggered TIAR-mediated suppression of translation. Biochim Biophys Acta 13 3727 PMID: 25483082
Kondratska et al (2014) Orai1 and STIM1 mediate SOCE and contribute to apoptotic resistance of pancreatic adenocarcinoma. PLoS One 1843 2263 PMID: 24583265
Gerich et al (2009) H(2)O(2)-mediated modulation of cytosolic signaling and organelle function in rat hippocampus. J Neurosci 458 937 PMID: 19430810
Deldicque et al (2011) ER stress induces anabolic resistance in muscle cells through PKB-induced blockade of mTORC1. PLoS One 6 e20993 PMID: 21698202
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Li and Burrell (2011) Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms. Learn Mem 18 545 PMID: 21844187
He et al (2018) Mechanical regulation of stem-cell differentiation by the stretch-activated Piezo channel. Nature 555 103 PMID: 29414942
Abuaita et al (2018) Mitochondria-Derived Vesicles Deliver Antimicrobial Reactive Oxygen Species to Control Phagosome-Localized Staphylococcus aureus. Cell Host Microbe 24 625 PMID: 30449314
Atakpa et al (2018) IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes. Cell Rep 25 3180 PMID: 30540949
Lambelet et al (2018) Dysfunctional autophagy following exposure to pro-inflammatory cytokines contributes to pancreatic β-cell apoptosis. Cell Death Dis 9 96 PMID: 29367588
Hossain et al (2018) Hyperactivation of nuclear receptor coactivators induces PERK-dependent cell death. Oncotarget 9 11707 PMID: 29545931
Mätlik et al (2016) Role of two sequence motifs of mesencephalic astrocyte-derived neurotrophic factor in its survival-promoting activity. Cell Death Dis 6 e2032 PMID: 26720341
Gupta et al (2016) NCOA3 coactivator is a transcriptional target of XBP1 and regulates PERK-eIF2α-ATF4 signalling in breast cancer. Oncogene 35 5860 PMID: 27109102
Kelm et al (2008) The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons. J Neurophysiol 100 3417 PMID: 18945815
Dai et al (2008) A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients. Neurosignals 16 112 PMID: 18253052
Xu et al (2018) Increased sensitivity to apoptosis upon endoplasmic reticulum stress-induced activation of the unfolded protein response in chemotherapy-resistant malignant pleural mesothelioma. Br J Cancer 119 65 PMID: 29921948
Shambharkar et al (2015) TMEM203 Is a Novel Regulator of Intracellular Calcium Homeostasis and Is Required for Spermatogenesis. J Cell Biol 10 e0127480 PMID: 25996873
Cao et al (2015) Calcium release through P2X4 activates calmodulin to promote endolysosomal membrane fusion. PLoS One 209 879 PMID: 26101220
Azab et al (2015) Binding of αherpesvirus Glycoprotein H to Surface α4β1-Integrins Activates Calcium-Signaling Pathways and Induces Phosphatidylserine Exposure on the Plasma Membrane. Endocrinology 6 e01552-15 PMID: 26489864
Velásquez-Martínez et al (2015) α-1 adrenoreceptors modulate GABA release onto ventral tegmental area DA neurons. Pflugers Arch 88 110 PMID: 25261018
Dobson et al (2015) Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling. J Neuroinflammation 10 e0125974 PMID: 25933382
Few et al (2012) Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release. Proc Natl Acad Sci U S A 109 E452 PMID: 22308469
Bender et al (2006) Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex. J Neurosci 26 4166 PMID: 16624937
Fransen et al (2006) Mechanism of graded persistent cellular activity of entorhinal cortex layer v neurons. Neuron 49 735 PMID: 16504948
Do you know of a great paper that uses Thapsigargin from Tocris? Please let us know.
Reviews for Thapsigargin
Average Rating: 4.3 (Based on 6 Reviews.)
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Dissolved in DMSO. We treated cells for 16 hr.
Thapsigargin was used to block SERCA in activated CD8+ T-cells. This maintained high intracellular Ca2+, leading to increased activation of CD8+ T-cells as measured by IFNg production via intracellular flow cytometry.
This compound is often used to deplete intracellular calcium stores in cell culture or other applications. It worked as expected in our tissue preparations.
Cytosolic Ca2+ sensitive indicator, Fura-2 was loaded in RBL-2H3 cells and excited alternately at 340 and 380 nm and fluorescence was captured at 510 nm.ER store was depleted with 500 nM thapsigargin which promotes store-operated Ca2+ entry via STIM1/Orai1 pathway into the cells upon addition of 2 mM extracellular Ca2+.RBL-2H3 cells were loaded with FURA-2AM (2 μM) and Pluronic F127 (0.02%) for 30 min followed by washing with normal-Tyrode solution. Cells were stimulated at 1 Hz frequency and fluorescence intensities were measured.
Used it as a positive control to test if the mechanism of a novel small molecule (compound x) was to reduce ER stress. Cells were treated with 5um Thapsigargin for 24 hours, and splicing of XBP1 was determined by semi-quantitative RT-PCR
for calcium release from the ER