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company name :
Alomone Labs
product type :
chemical
product name :
Thapsigargin
catalog :
T-650
more info or order :
citations: 51
Reference
Fan G, Kaßmann M, Cui Y, Matthaeus C, Kunz S, Zhong C, et al. Age attenuates the T-type CaV 3.2-RyR axis in vascular smooth muscle. Aging Cell. 2020;19:e13134 pubmed publisher
Uzureau S, Lecordier L, Uzureau P, Hennig D, Graversen J, Homble F, et al. APOL1 C-Terminal Variants May Trigger Kidney Disease through Interference with APOL3 Control of Actomyosin. Cell Rep. 2020;30:3821-3836.e13 pubmed publisher
Kim Y, Jo Y, Lee Y, Park K, Park H, Choi S. Zn2+ stimulates salivary secretions via metabotropic zinc receptor ZnR/GPR39 in human salivary gland cells. Sci Rep. 2019;9:17648 pubmed publisher
Vierra N, Kirmiz M, van der List D, Santana L, Trimmer J. Kv2.1 mediates spatial and functional coupling of L-type calcium channels and ryanodine receptors in mammalian neurons. elife. 2019;8: pubmed publisher
Liu D, Eagleman D, Tsai N. Novel roles of ER stress in repressing neural activity and seizures through Mdm2- and p53-dependent protein translation. PLoS Genet. 2019;15:e1008364 pubmed publisher
Gutiérrez L, Hernández Morales M, Núñez L, Villalobos C. Inhibition of Polyamine Biosynthesis Reverses Ca2+ Channel Remodeling in Colon Cancer Cells. Cancers (Basel). 2019;11: pubmed publisher
Kostić M, Katoshevski T, Sekler I. Allosteric Regulation of NCLX by Mitochondrial Membrane Potential Links the Metabolic State and Ca2+ Signaling in Mitochondria. Cell Rep. 2018;25:3465-3475.e4 pubmed publisher
Roest G, Hesemans E, Welkenhuyzen K, Luyten T, Engedal N, Bultynck G, et al. The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells. 2018;7: pubmed publisher
Bittremieux M, La Rovere R, Schuermans M, Luyten T, Mikoshiba K, Vangheluwe P, et al. Extracellular and ER-stored Ca2+ contribute to BIRD-2-induced cell death in diffuse large B-cell lymphoma cells. Cell Death Discov. 2018;4:101 pubmed publisher
Maggio N, Vlachos A. Tumor necrosis factor (TNF) modulates synaptic plasticity in a concentration-dependent manner through intracellular calcium stores. J Mol Med (Berl). 2018;96:1039-1047 pubmed publisher
Smaardijk S, Chen J, Kerselaers S, Voets T, Eggermont J, Vangheluwe P. Store-independent coupling between the Secretory Pathway Ca2+ transport ATPase SPCA1 and Orai1 in Golgi stress and Hailey-Hailey disease. Biochim Biophys Acta Mol Cell Res. 2018;1865:855-862 pubmed publisher
Whitt J, McNally B, Meredith A. Differential contribution of Ca2+ sources to day and night BK current activation in the circadian clock. J Gen Physiol. 2018;150:259-275 pubmed publisher
Tseng H, Vong C, Kwan Y, Lee S, Hoi M. Lysosomal Ca2+ Signaling Regulates High Glucose-Mediated Interleukin-1? Secretion via Transcription Factor EB in Human Monocytic Cells. Front Immunol. 2017;8:1161 pubmed publisher
Vierra N, Dadi P, Milian S, Dickerson M, Jordan K, Gilon P, et al. TALK-1 channels control β cell endoplasmic reticulum Ca2+ homeostasis. Sci Signal. 2017;10: pubmed publisher
Taylor E, Pantazaka E, Shelley K, Taylor C. Prostaglandin E2 Inhibits Histamine-Evoked Ca2+ Release in Human Aortic Smooth Muscle Cells through Hyperactive cAMP Signaling Junctions and Protein Kinase A. Mol Pharmacol. 2017;92:533-545 pubmed publisher
Makitani K, Nakagawa S, Izumi Y, Akaike A, Kume T. Inhibitory effect of donepezil on bradykinin-induced increase in the intracellular calcium concentration in cultured cortical astrocytes. J Pharmacol Sci. 2017;134:37-44 pubmed publisher
Chen J, De Raeymaecker J, Hovgaard J, Smaardijk S, Vandecaetsbeek I, Wuytack F, et al. Structure/activity relationship of thapsigargin inhibition on the purified Golgi/secretory pathway Ca2+/Mn2+-transport ATPase (SPCA1a). J Biol Chem. 2017;292:6938-6951 pubmed publisher
González Sánchez P, Pla Martín D, Martinez Valero P, Rueda C, Calpena E, del Arco A, et al. CMT-linked loss-of-function mutations in GDAP1 impair store-operated Ca2+ entry-stimulated respiration. Sci Rep. 2017;7:42993 pubmed publisher
Bittremieux M, Gerasimenko J, Schuermans M, Luyten T, Stapleton E, Alzayady K, et al. DPB162-AE, an inhibitor of store-operated Ca2+ entry, can deplete the endoplasmic reticulum Ca2+ store. Cell Calcium. 2017;62:60-70 pubmed publisher
Fung Leung W, EDWARDS W, Liu Y, Ngo K, Angsana J, Castro G, et al. T Cell Subset and Stimulation Strength-Dependent Modulation of T Cell Activation by Kv1.3 Blockers. PLoS ONE. 2017;12:e0170102 pubmed publisher
Smaardijk S, Chen J, Wuytack F, Vangheluwe P. SPCA2 couples Ca2+ influx via Orai1 to Ca2+ uptake into the Golgi/secretory pathway. Tissue Cell. 2017;49:141-149 pubmed publisher
Srivats S, Balasuriya D, Pasche M, Vistal G, Edwardson J, Taylor C, et al. Sigma1 receptors inhibit store-operated Ca2+ entry by attenuating coupling of STIM1 to Orai1. J Cell Biol. 2016;213:65-79 pubmed publisher
Zhao N, Dong Q, Qian C, Li S, Wu Q, Ding D, et al. Lovastatin blocks Kv1.3 channel in human T cells: a new mechanism to explain its immunomodulatory properties. Sci Rep. 2015;5:17381 pubmed publisher
Landowski L, Pavez M, Brown L, Gasperini R, Taylor B, West A, et al. Low-density Lipoprotein Receptor-related Proteins in a Novel Mechanism of Axon Guidance and Peripheral Nerve Regeneration. J Biol Chem. 2016;291:1092-102 pubmed publisher
Murray J, Qian Y, Liu B, Elliott R, Aral J, Park C, et al. Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3. J Med Chem. 2015;58:6784-802 pubmed publisher
Vutthasathien P, Wattanapermpool J. Regular exercise improves cardiac contractile activation by modulating MHC isoforms and SERCA activity in orchidectomized rats. J Appl Physiol (1985). 2015;119:831-9 pubmed publisher
Lopez Sanjurjo C, Tovey S, Taylor C. Rapid recycling of Ca2+ between IP3-sensitive stores and lysosomes. PLoS ONE. 2014;9:e111275 pubmed publisher
Hu J, Oda S, Shotts K, Donovan E, Strauch P, Pujanauski L, et al. Lysophosphatidic acid receptor 5 inhibits B cell antigen receptor signaling and antibody response. J Immunol. 2014;193:85-95 pubmed publisher
Bolinches Amorós A, Molla B, Pla Martín D, Palau F, Gonzalez Cabo P. Mitochondrial dysfunction induced by frataxin deficiency is associated with cellular senescence and abnormal calcium metabolism. Front Cell Neurosci. 2014;8:124 pubmed publisher
Mariqueo T, Agurto A, Muñoz B, San Martin L, Coronado C, Fernandez Perez E, et al. Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons. J Neurophysiol. 2014;111:1940-8 pubmed publisher
Tamura A, Yamada N, Yaguchi Y, Machida Y, Mori I, Osanai M. Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum. PLoS ONE. 2014;9:e85351 pubmed publisher
Habourdin C, Klein G, Araki T, Williams J, Aubry L. The arrestin-domain containing protein AdcA is a response element to stress. Cell Commun Signal. 2013;11:91 pubmed publisher
Zhao N, Dong Q, Du L, Fu X, Du Y, Liao Y. Potent suppression of Kv1.3 potassium channel and IL-2 secretion by diphenyl phosphine oxide-1 in human T cells. PLoS ONE. 2013;8:e64629 pubmed publisher
Pantazaka E, Taylor E, Bernard W, Taylor C. Ca(2+) signals evoked by histamine H1 receptors are attenuated by activation of prostaglandin EP2 and EP4 receptors in human aortic smooth muscle cells. Br J Pharmacol. 2013;169:1624-34 pubmed publisher
Lin F, Elliott R, Colombero A, Gaida K, Kelley L, Moksa A, et al. Generation and characterization of fully human monoclonal antibodies against human Orai1 for autoimmune disease. J Pharmacol Exp Ther. 2013;345:225-38 pubmed publisher
Witayavanitkul N, Woranush W, Bupha Intr T, Wattanapermpool J. Testosterone regulates cardiac contractile activation by modulating SERCA but not NCX activity. Am J Physiol Heart Circ Physiol. 2013;304:H465-72 pubmed publisher
Jover E, Tawk M, Laventie B, Poulain B, Prevost G. Staphylococcal leukotoxins trigger free intracellular Ca(2+) rise in neurones, signalling through acidic stores and activation of store-operated channels. Cell Microbiol. 2013;15:742-58 pubmed publisher
Peng Y, Chen J, He S, Yang J, Wu H. Release of ATP from marginal cells in the cochlea of neonatal rats can be induced by changes in extracellular and intracellular ion concentrations. PLoS ONE. 2012;7:e47124 pubmed publisher
Mitchell C, Gasperini R, Small D, Foa L. STIM1 is necessary for store-operated calcium entry in turning growth cones. J Neurochem. 2012;122:1155-66 pubmed publisher
Shakiryanova D, Morimoto T, Zhou C, Chouhan A, Sigrist S, Nose A, et al. Differential control of presynaptic CaMKII activation and translocation to active zones. J Neurosci. 2011;31:9093-100 pubmed publisher
Tamagawa Y, Saino T, Matsuura M, Satoh Y. The effects of diuretics on intracellular Ca2+ dynamics of arteriole smooth muscles as revealed by laser confocal microscopy. Acta Histochem Cytochem. 2009;42:121-8 pubmed publisher
Fekete A, Franklin L, Ikemoto T, Rozsa B, Lendvai B, Sylvester Vizi E, et al. Mechanism of the persistent sodium current activator veratridine-evoked Ca elevation: implication for epilepsy. J Neurochem. 2009;111:745-56 pubmed publisher
Gasperini R, Choi Lundberg D, Thompson M, Mitchell C, Foa L. Homer regulates calcium signalling in growth cone turning. Neural Dev. 2009;4:29 pubmed publisher
Berrout J, Isokawa M. Homeostatic and stimulus-induced coupling of the L-type Ca2+ channel to the ryanodine receptor in the hippocampal neuron in slices. Cell Calcium. 2009;46:30-8 pubmed publisher
Hall A, Herrera Y, Ajmo C, Cuevas J, Pennypacker K. Sigma receptors suppress multiple aspects of microglial activation. Glia. 2009;57:744-54 pubmed publisher
A F, C J, H J A. Properties of the SR Ca-ATPase in an Open Microsomal Membrane Preparation. Open Biochem J. 2008;2:91-9 pubmed publisher
Tovey S, Dedos S, Taylor E, Church J, Taylor C. Selective coupling of type 6 adenylyl cyclase with type 2 IP3 receptors mediates direct sensitization of IP3 receptors by cAMP. J Cell Biol. 2008;183:297-311 pubmed publisher
Tanaka M, Watanabe Y, Yoshimoto K. Regulation of relaxin 3 gene expression via cAMP-PKA in a neuroblastoma cell line. J Neurosci Res. 2009;87:820-9 pubmed publisher
Herrera Y, Katnik C, Rodriguez J, Hall A, Willing A, Pennypacker K, et al. sigma-1 receptor modulation of acid-sensing ion channel a (ASIC1a) and ASIC1a-induced Ca2+ influx in rat cortical neurons. J Pharmacol Exp Ther. 2008;327:491-502 pubmed publisher
Fajardo O, Meseguer V, Belmonte C, Viana F. TRPA1 channels mediate cold temperature sensing in mammalian vagal sensory neurons: pharmacological and genetic evidence. J Neurosci. 2008;28:7863-75 pubmed publisher
Wong M, Shakiryanova D, Levitan E. Presynaptic ryanodine receptor-CamKII signaling is required for activity-dependent capture of transiting vesicles. J Mol Neurosci. 2009;37:146-50 pubmed publisher
image
image 1 :
Alomone Labs T-650 image 1
Alomone Labs Thapsigargin induces cytosolic Ca2+increase in HEK 293 cells. - Ca2+ traces from Fluo-3 AM loaded HEK 293 cells treated with 5 M Thapsigargin (#T-650) in the presence of 5 mM EGTA.
image 2 :
Alomone Labs T-650 image 2
Alomone Labs Thapsigargin induces apoptosis in Jurkat cells. - Cells were grown to 70% confluency. 1 ?MThapsigargin(#T-650) or vehicle was added for six hours. Cell extracts were then probed for cleaved Caspase 3 with specific antibodies.
product information
CAT :
T-650
SKU :
T-650_0.65 mg
Product Name :
Thapsigargin
Group Type :
Non Antibodies
Product Type :
S. Molecules
Shipping and storage :
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
Product Page - 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
Supplier :
Alomone Labs
Target :
SERCA
Long Description :
Thapsigargin (#T-650) is a highly pure, natural and biologically active compound.
Short Description :
A Potent and Cell-Permeable Inhibitor of SERCA Pump Ca2+-ATPase/an Intracellular Ca2+ Mobilizer
MW :
650.7
Source :
Natural
Molecular formula :
C34H50O12.
Effective Concentration :
50 nM - 1 μM.
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
Reconstitution and Solubility :
DMSO, ethanol or acetone. Centrifuge all product preparations before use (10000 x g 5 min).
Solubility :
DMSO, ethanol or acetone. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions :
Up to one week at 4°C or three months at -20°C.
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.
Purity :
>99% (HPLC)
CAS No :
67526-95-8
Form :
Lyophilized Powder
Comment :
Contact Alomone Labs for technical support and product customization
UNSPSC :
41116134
Bioassay Tested :
Yes
Cited Application :
Electrophysiology
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.
more info or order :
company information
Alomone Labs
Jerusalem BioPark (JBP), Hadassah Ein Kerem
P.O. Box 4287
Jerusalem 9104201
info@alomone.com
http://www.alomone.com
972 2 531 8002
headquarters: Israel