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商品描述
Biological Activity Technical DataBackground Product DatasheetsCalculators
Biological Activity
Potent inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases. Causes ER stress; can be used to induce autophagy in mammalian cells.Technical Data
M.Wt:
650.76
Formula:
C34H50O12
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Desiccate at -20°C
CAS No:
67526-95-8
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.
Background References
- Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival.Ding et al.J.Biol.Chem., 2007;282:4702
- Kinetics of thapsigargin-Ca2+-ATPase (sarcoplasmic reticulum) interaction reveals a two-step binding mechanism and picomolar inhibition.Davidson and VarholJ.Biol.Chem., 1995;270:11731
- A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases.Treiman et al.TiPS, 1998;19:131
- Specific substitutions at amino acid 256 of the sarcoplasmic/endoplasmic reticulum Ca2+ transport ATPase mediate resistance to thapsigargin in thapsigargin-resistant hamster cells.Yu et al.J.Biol.Chem., 1998;273:3542
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Citations for Thapsigargin
The citations listed below are publications that use Tocris products.Selected citations for Thapsigargin include:
41Citations: Showing 1 - 10
- Swelling-activated Ca2+ channels trigger Ca2+ signals in Merkel cells.Authors: Haeberle Et al.MBio;3:e1750
- Caspase-mediated cleavage of IRE1 controls apoptotic cell commitment during endoplasmic reticulum stress.Authors: Shemorry Et al.Elife2019;8
- Dysfunctional autophagy following exposure to pro-inflammatory cytokines contributes to pancreatic β-cell apoptosis.Authors: Lambelet Et al.Cell Death Dis2018;9:96
- Hyperactivation of nuclear receptor coactivators induces PERK-dependent cell death.Authors: Hossain Et al.Oncotarget2018;9:11707
- Mechanical regulation of stem-cell differentiation by the stretch-activated Piezo channel.Authors: He Et al.Nature2018;555:103
- IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes.Authors: Atakpa Et al.Cell Rep2018;25:3180
- Mitochondria-Derived Vesicles Deliver Antimicrobial Reactive Oxygen Species to Control Phagosome-Localized Staphylococcus aureus.Authors: Abuaita Et al.Cell Host Microbe2018;24:625
- Increased sensitivity to apoptosis upon endoplasmic reticulum stress-induced activation of the unfolded protein response in chemotherapy-resistant malignant pleural mesothelioma.Authors: Xu Et al.Br J Cancer2018;119:65
- Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma.Authors: Florea Et al.Oncotarget2017;8:22876
- Role of two sequence motifs of mesencephalic astrocyte-derived neurotrophic factor in its survival-promoting activity.Authors: Mätlik Et al.Cell Death Dis2016;6:e2032
- NCOA3 coactivator is a transcriptional target of XBP1 and regulates PERK-eIF2α-ATF4 signalling in breast cancer.Authors: Gupta Et al.Oncogene2016;35:5860
- Presynaptic Spike Timing-Dependent Long-Term Depression in the Mouse Hippocampus.Authors: Andrade-Talavera Et al.Cereb Cortex2016;26:3637
- Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.Authors: Salzer Et al.Neuropharmacology2016;110 (A):277
- α-1 adrenoreceptors modulate GABA release onto ventral tegmental area DA neurons.Authors: Velásquez-Martínez Et al.Pflugers Arch2015;88:110
- Binding of αherpesvirus Glycoprotein H to Surface α4β1-Integrins Activates Calcium-Signaling Pathways and Induces Phosphatidylserine Exposure on the Plasma Membrane.Authors: Azab Et al.Endocrinology2015;6
- Calcium release through P2X4 activates calmodulin to promote endolysosomal membrane fusion.Authors: Cao Et al.PLoS One2015;209:879
- Differential regulation of GnRH secretion in the preoptic area (POA) and the median eminence (ME) in male mice.Authors: Glanowska and MoenterNeuropharmacology2015;156:231
- TMEM203 Is a Novel Regulator of Intracellular Calcium Homeostasis and Is Required for Spermatogenesis.Authors: Shambharkar Et al.J Cell Biol2015;10:e0127480
- Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling.Authors: Dobson Et al.J Neuroinflammation2015;10:e0125974
- Orai1 and STIM1 mediate SOCE and contribute to apoptotic resistance of pancreatic adenocarcinoma.Authors: Kondratska Et al.PLoS One2014;1843:2263
- Downregulation of BRCA1 protein in BCR-ABL1 leukemia cells depends on stress-triggered TIAR-mediated suppression of translation.Authors: Podszywalow-Bartnicka Et al.Biochim Biophys Acta2014;13:3727
- Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells.Authors: Soltoff and LannonPLoS One2013;8:e72881
- Optogenetic probing and manipulation of the calyx-type presynaptic terminal in the embryonic chick ciliary ganglion.Authors: Egawa Et al.PLoS One2013;8:e59179
- Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis.Authors: Varadarajan Et al.PLoS One2013;8:e56603
- Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.Authors: Rojas Et al.Mol Pharmacol2013;83:106
- Recruitment of the intracellular Ca2+ by ultrashort electric stimuli: the impact of pulse duration.Authors: Semenov Et al.Cell Calcium2013;54:145
- The expression and relaxant effect of bitter taste receptors in human bronchi.Authors: Grassin-Delyle Et al.Respir Res2013;14:134
- Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation.Authors: Pinheiro Et al.Cell Commun Signal2013;11:70
- Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release.Authors: Few Et al.Proc Natl Acad Sci U S A2012;109:E452
- ER stress induces anabolic resistance in muscle cells through PKB-induced blockade of mTORC1.Authors: Deldicque Et al.PLoS One2011;6:e20993
- Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms.Authors: Li and BurrellLearn Mem2011;18:545
- β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.Authors: Meitzen Et al.J Neurochem2011;116:984
- Dysregulation of presynaptic calcium and synaptic plasticity in a mouse model of 22q11 deletion syndrome.Authors: Earls Et al.PLoS One2010;30:15843
- Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors.Authors: Moore Et al.Neuron2009;61:287
- Calcium homeostasis and cone signaling are regulated by interactions between calcium stores and plasma membrane ion channels.Authors: Szikra Et al.PLoS One2009;4:e6723
- H(2)O(2)-mediated modulation of cytosolic signaling and organelle function in rat hippocampus.Authors: Gerich Et al.J Neurosci2009;458:937
- A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients.Authors: Dai Et al.Neurosignals2008;16:112
- The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons.Authors: Kelm Et al.J Neurophysiol2008;100:3417
- Calcium release from presynaptic internal stores is required for ethanol to increase spontaneousγ-aminobutyric acid release onto cerebellum Purkinje neurons.Authors: Kelm Et al.Cell Cycle2007;323:356
- Mechanism of graded persistent cellular activity of entorhinal cortex layer v neurons.Authors: Fransen Et al.Neuron2006;49:735
- Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex.Authors: Bender Et al.J Neurosci2006;26:4166
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Usage Information
By Anonymouson 06/20/2020
Application: Species:Human
100 nM
Thapsigargin Blocks Re-Uptake of Ca2+ Into ER leading to increased T-cell activation by IFNg
By Li Zhuon 01/23/2019
Application: Species:Human
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.
Intracellular calcium depletion
By Anonymouson 11/19/2018
Application: Species:Mouse
This compound is often used to deplete intracellular calcium stores in cell culture or other applications. It worked as expected in our tissue preparations.
Thapsigargin elicits store-operated Ca2+ entry after ER store depletion in RBL-2H3 cells.
By Niroj Shresthaon 10/27/2018
Application: Species:Rat
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.
XBP1 splicing
By Preethi Vijayarajon 05/01/2018
Application: Species:Human
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
Thapsigargin calcium assay
By Anonymouson 12/12/2017
Application: Species:Human
for calcium release from the ER
