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Thapsigargin

Catalog #: 1138
42 Citations Datasheet
Catalog # Availability Size / Price Qty
1138/1
Thapsigargin | CAS No. 67526-95-8 | Ca2+-ATPase Inhibitors
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Description: Potent inhibitor of SERCA ATPase

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-oxobutoxy)azuleno[4,5-b]furan-7-yl octanoate

Purity: ≥97%

Product Details
Citations (42)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

M.Wt:
650.76
Formula:
C34H50O12
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Store 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

  1. GPN does not release lysosomal Ca2+, but evokes ER Ca2+ release by increasing cytosolic pH independent of cathepsin C
    P Atakpa, LM van Marrew, M Apta-Smith, S Chakrabort, CW Taylor
    J. Cell. Sci., 2019;0(0):.
  2. IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes
    P Atakpa, NB Thillaiapp, S Mataragka, DL Prole, CW Taylor
    Cell Rep, 2018;25(11):3180-3193.e7.
  3. The Complement System Component C5a Produces Thermal Hyperalgesia via Macrophage-to-Nociceptor Signaling That Requires NGF and TRPV1

    J Neurosci, 2016;36(18):5055-70.
  4. Serotonin (5-HT) activation of immortalized hypothalamic neuronal cells through the 5-HT1B serotonin receptor.
    Tung S, Hardy A, Wheeler M, Belsham D
    Endocrinology, 2012;153(10):4862-73.
  5. The Endocannabinoid Metabolite Prostaglandin E2 (PGE2)-Glycerol Inhibits Human Neutrophil Functions: Involvement of Its Hydrolysis into PGE2 and EP Receptors
    C Turcotte, S Zarini, S Jean, C Martin, RC Murphy, D Marsolais, M Laviolette, MR Blanchet, N Flamand
    J. Immunol, 2017;0(0):.
  6. Calcium oscillations coordinate feather mesenchymal cell movement by SHH dependent modulation of gap junction networks
    A Li, JH Cho, B Reid, CC Tseng, L He, P Tan, CY Yeh, P Wu, Y Li, RB Widelitz, Y Zhou, M Zhao, RH Chow, CM Chuong
    Nat Commun, 2018;9(1):5377.
  7. Methionine sulfoxide reductase B3 protects from endoplasmic reticulum stress in Drosophila and in mammalian cells.
    Kwak GH, Lim DH, Han JY, Lee YS, Kim HY
    Biochem. Biophys. Res. Commun., 2012;420(1):130-5.
  8. Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival.
    Ding et al.
    J.Biol.Chem., 2007;282:4702
  9. Kinetics of thapsigargin-Ca2+-ATPase (sarcoplasmic reticulum) interaction reveals a two-step binding mechanism and picomolar inhibition.
    Davidson and Varhol
    J.Biol.Chem., 1995;270:11731
  10. A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases.
    Treiman et al.
    TiPS, 1998;19:131
  11. 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
  12. Thapsigargin is a broad-Spectrum inhibitor of major human respiratory viruses: coronavirus, respiratory syncytial virus and influenza A virus.
    Al-Beltagi et al.
    Viruses, 2021;13:234
  13. Thapsigargin at non-cytotoxic levels induces a potent host antiviral response that blocks influenza A virus replication.
    Goulding et al.
    Viruses, 2020;12:1093

Product Datasheets

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Citations for Thapsigargin

The citations listed below are publications that use Tocris products. Selected citations for Thapsigargin include:

42 Citations: Showing 1 - 10

  1. Swelling-activated Ca2+ channels trigger Ca2+ signals in Merkel cells.
    Authors: Haeberle Et al.
    MBio  ;3:e1750
  2. Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation
    Authors: McEwan Et al.
    Life Sci  2021;283:119850
  3. Caspase-mediated cleavage of IRE1 controls apoptotic cell commitment during endoplasmic reticulum stress.
    Authors: Shemorry Et al.
    Elife  2019;8:e47084
  4. Dysfunctional autophagy following exposure to pro-inflammatory cytokines contributes to pancreatic β-cell apoptosis.
    Authors: Lambelet Et al.
    Cell Death Dis  2018;9:96
  5. Hyperactivation of nuclear receptor coactivators induces PERK-dependent cell death.
    Authors: Hossain Et al.
    Oncotarget  2018;9:11707
  6. Mechanical regulation of stem-cell differentiation by the stretch-activated Piezo channel.
    Authors: He Et al.
    Nature  2018;555:103
  7. IP3 Receptors Preferentially Associate with ER-Lysosome Contact Sites and Selectively Deliver Ca2+ to Lysosomes.
    Authors: Atakpa Et al.
    Cell Rep  2018;25:3180
  8. Mitochondria-Derived Vesicles Deliver Antimicrobial Reactive Oxygen Species to Control Phagosome-Localized Staphylococcus aureus.
    Authors: Abuaita Et al.
    Cell Host Microbe  2018;24:625
  9. 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 Cancer  2018;119:65
  10. Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma.
    Authors: Florea Et al.
    Oncotarget  2017;8:22876
  11. Role of two sequence motifs of mesencephalic astrocyte-derived neurotrophic factor in its survival-promoting activity.
    Authors: Mätlik Et al.
    Cell Death Dis  2016;6:e2032
  12. NCOA3 coactivator is a transcriptional target of XBP1 and regulates PERK-eIF2α-ATF4 signalling in breast cancer.
    Authors: Gupta Et al.
    Oncogene  2016;35:5860
  13. Presynaptic Spike Timing-Dependent Long-Term Depression in the Mouse Hippocampus.
    Authors: Andrade-Talavera Et al.
    Cereb Cortex  2016;26:3637
  14. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.
    Authors: Salzer Et al.
    Neuropharmacology  2016;110 (A):277
  15. α-1 adrenoreceptors modulate GABA release onto ventral tegmental area DA neurons.
    Authors: Velásquez-Martínez Et al.
    Pflugers Arch  2015;88:110
  16. 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.
    Endocrinology  2015;6:e01552-15
  17. Calcium release through P2X4 activates calmodulin to promote endolysosomal membrane fusion.
    Authors: Cao Et al.
    PLoS One  2015;209:879
  18. Differential regulation of GnRH secretion in the preoptic area (POA) and the median eminence (ME) in male mice.
    Authors: Glanowska and Moenter
    Neuropharmacology  2015;156:231
  19. TMEM203 Is a Novel Regulator of Intracellular Calcium Homeostasis and Is Required for Spermatogenesis.
    Authors: Shambharkar Et al.
    J Cell Biol  2015;10:e0127480
  20. Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling.
    Authors: Dobson Et al.
    J Neuroinflammation  2015;10:e0125974
  21. Orai1 and STIM1 mediate SOCE and contribute to apoptotic resistance of pancreatic adenocarcinoma.
    Authors: Kondratska Et al.
    PLoS One  2014;1843:2263
  22. 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 Acta  2014;13:3727
  23. Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells.
    Authors: Soltoff and Lannon
    PLoS One  2013;8:e72881
  24. Optogenetic probing and manipulation of the calyx-type presynaptic terminal in the embryonic chick ciliary ganglion.
    Authors: Egawa Et al.
    PLoS One  2013;8:e59179
  25. Endoplasmic reticulum membrane reorganization is regulated by ionic homeostasis.
    Authors: Varadarajan Et al.
    PLoS One  2013;8:e56603
  26. Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.
    Authors: Rojas Et al.
    Mol Pharmacol  2013;83:106
  27. Recruitment of the intracellular Ca2+ by ultrashort electric stimuli: the impact of pulse duration.
    Authors: Semenov Et al.
    Cell Calcium  2013;54:145
  28. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res  2013;14:134
  29. Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation.
    Authors: Pinheiro Et al.
    Cell Commun Signal  2013;11:70
  30. 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 A  2012;109:E452
  31. ER stress induces anabolic resistance in muscle cells through PKB-induced blockade of mTORC1.
    Authors: Deldicque Et al.
    PLoS One  2011;6:e20993
  32. Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms.
    Authors: Li and Burrell
    Learn Mem  2011;18:545
  33. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem  2011;116:984
  34. Dysregulation of presynaptic calcium and synaptic plasticity in a mouse model of 22q11 deletion syndrome.
    Authors: Earls Et al.
    PLoS One  2010;30:15843
  35. Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors.
    Authors: Moore Et al.
    Neuron  2009;61:287
  36. Calcium homeostasis and cone signaling are regulated by interactions between calcium stores and plasma membrane ion channels.
    Authors: Szikra Et al.
    PLoS One  2009;4:e6723
  37. H(2)O(2)-mediated modulation of cytosolic signaling and organelle function in rat hippocampus.
    Authors: Gerich Et al.
    J Neurosci  2009;458:937
  38. A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients.
    Authors: Dai Et al.
    Neurosignals  2008;16:112
  39. The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons.
    Authors: Kelm Et al.
    J Neurophysiol  2008;100:3417
  40. Calcium release from presynaptic internal stores is required for ethanol to increase spontaneous γ-aminobutyric acid release onto cerebellum Purkinje neurons.
    Authors: Kelm Et al.
    Cell Cycle  2007;323:356
  41. Mechanism of graded persistent cellular activity of entorhinal cortex layer v neurons.
    Authors: Fransen Et al.
    Neuron  2006;49:735
  42. Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex.
    Authors: Bender Et al.
    J Neurosci  2006;26:4166

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