MW 650.8 Da, Purity >98%. A potent, cell-permeable Ca2+-ATPase inhibitor. Releases Ca2+ by inhibiting endoplasmic reticular Ca2+-ATPase (IC50 = 4-13 nM). Both tumorogenic and apoptotic actions reported.
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- The Journal of cell biology 222:2023Tex2 is required for lysosomal functions at TMEM55-dependent ER membrane contact sites.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYuanjiao Du,Weiping Chang,Lei Gao,Lin Deng,Wei-Ke JiPubMed 36705603
- Nature communications 13:42682022Integrin α3β1 promotes vessel formation of glioblastoma-associated endothelial cells through calcium-mediated macropinocytosis and lysosomal exocytosis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesEunnyung Bae,Ping Huang,Gaёlle Müller-Greven,Dolores Hambardzumyan,Andrew Edward Sloan,Amy S Nowacki,Nicholas Marko,Cathleen R Carlin,Candece L GladsonPubMed 35879332
- Biomaterials 284:1214772022Application of piconewton forces to individual filopodia reveals mechanosensory role of L-type Ca channels.Applications:Unspecified applicationReactive species:Unspecified reactive speciesArtem K Efremov,Mingxi Yao,Yuze Sun,Yee Han Tee,Michael P Sheetz,Alexander D Bershadsky,Boris Martinac,Jie YanPubMed 35395455
- Signal transduction and targeted therapy 7:462022Protein C receptor maintains cancer stem cell properties via activating lipid synthesis in nasopharyngeal carcinoma.Applications:Unspecified applicationReactive species:Unspecified reactive speciesPanpan Zhang,Qiuping He,Yaqin Wang,Guanqun Zhou,Yupei Chen,Linglong Tang,Yuan Zhang,Xiaohong Hong,Yanping Mao,Qingmei He,Xiaojing Yang,Na Liu,Jun MaPubMed 35169126
- Journal of animal science and biotechnology 13:92022Ryanodine receptor RyR1-mediated elevation of Ca concentration is required for the late stage of myogenic differentiation and fusion.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKai Qiu,Yubo Wang,Doudou Xu,Linjuan He,Xin Zhang,Enfa Yan,Lu Wang,Jingdong YinPubMed 35144690
- Proceedings of the National Academy of Sciences of the United States of America 118:2021Necroptosis activates UPR sensors without disrupting their binding with GRP78.Applications:Unspecified applicationReactive species:Unspecified reactive speciesWei Liang,Weiwei Qi,Yang Geng,Linhan Wang,Jing Zhao,Kezhou Zhu,Guowei Wu,Zairong Zhang,Heling Pan,Lihui Qian,Junying YuanPubMed 34544877
- PLoS biology 19:e30012632021A chemical screen for modulators of mRNA translation identifies a distinct mechanism of toxicity for sphingosine kinase inhibitors.Applications:Unspecified applicationReactive species:Unspecified reactive speciesAlba Corman,Dimitris C Kanellis,Patrycja Michalska,Maria Häggblad,Vanesa Lafarga,Jiri Bartek,Jordi Carreras-Puigvert,Oscar Fernandez-CapetilloPubMed 34033645
- Cellular signalling 83:1099742021RGS10 physically and functionally interacts with STIM2 and requires store-operated calcium entry to regulate pro-inflammatory gene expression in microglia.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMenbere Y Wendimu,Mohammed Alqinyah,Stephen Vella,Phillip Dean,Faris Almutairi,Roseanne Davila-Rivera,Shima Rayatpisheh,James Wohlschlegel,Silvia Moreno,Shelley B HooksPubMed 33705894
- Nature communications 12:9072021Arachidonic acid-regulated calcium signaling in T cells from patients with rheumatoid arthritis promotes synovial inflammation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesZhongde Ye,Yi Shen,Ke Jin,Jingtao Qiu,Bin Hu,Rohit R Jadhav,Khushboo Sheth,Cornelia M Weyand,Jörg J GoronzyPubMed 33568645
Key facts
- CAS number
- 67526-95-8
- Purity
- > 98%
- Form
- Solid
- Source
- Thapsia garganica
- Molecular weight
- 650.8 Da
- Molecular formula
- C34H50O12
- PubChem identifier
- 446378
- Nature
- Native
Target data
Alternative names
AT2A1_HUMAN, ATP2A, ATP2A1, ATPase Ca++ transporting cardiac muscle fast twitch 1, ATPase Ca++ transporting fast twitch 1, ATPase, Ca(2+)-transporting fast twitch 1, Calcium pump 1, Calcium transporting ATPase sarcoplasmic reticulum type fast twitch skeletal muscle isoform, Calcium-transporting ATPase sarcoplasmic reticulum type, EC 3.6.3.8, Endoplasmic reticulum class 1/2 Ca(2+) ATPase, Fast skeletal muscle SR calcium ATPase, OTTHUMP00000162561, OTTHUMP00000162562, SERCA 1, SERCA1 truncated isoform, included, SR Ca(2+)-ATPase 1, Sarcoendoplasmic reticulum calcium ATPase, Sarcoplasmic reticulum Ca(2+)-ATPase 1, Sarcoplasmic/endoplasmic reticulum calcium ATPase 1, fast twitch skeletal muscle isoform
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MW 650.8 Da, Purity >98%. A potent, cell-permeable Ca2+-ATPase inhibitor. Releases Ca2+ by inhibiting endoplasmic reticular Ca2+-ATPase (IC50 = 4-13 nM). Both tumorogenic and apoptotic actions reported.
Key facts
- CAS number
- 67526-95-8
- Purity
- > 98%
- Form
- Solid
- Source
- Thapsia garganica
- Molecular weight
- 650.8 Da
- Molecular formula
- C34H50O12
- PubChem identifier
- 446378
- Nature
- Native
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- Thapsigargin
- Biological description
A potent, cell-permeable Ca2+-ATPase inhibitor. Releases Ca2+ by inhibiting endoplasmic reticular Ca2+-ATPase (IC50 = 4-13 nM). Both tumorogenic and apoptotic actions reported.
- Canonical SMILES
- CCCCCCCC(=O)OC1C2C(=C(C1OC(=O)C(=CC)C)C)C3C(C(CC2(C)OC(=O)C)OC(=O)CCC)(C(C(=O)O3)(C)O)O
- Isomeric SMILES
- CCCCCCCC(=O)O[C@H]1[C@H]2C(=C([C@@H]1OC(=O)/C(=C\C)/C)C)[C@H]3[C@]([C@H](C[C@]2(C)OC(=O)C)OC(=O)CCC)([C@](C(=O)O3)(C)O)O
- InChI
- InChI=1S/C34H50O12/c1-9-12-13-14-15-17-24(37)43-28-26-25(20(5)27(28)44-30(38)19(4)11-3)29-34(41,33(8,40)31(39)45-29)22(42-23(36)16-10-2)18-32(26,7)46-21(6)35/h11,22,26-29,40-41H,9-10,12-18H2,1-8H3/b19-11-/t22-,26+,27-,28-,29-,32-,33+,34+/m0/s1
- InChIKey
- IXFPJGBNCFXKPI-FSIHEZPISA-N
- IUPAC name
- [(3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-acetyloxy-4-butanoyloxy-3,3a-dihydroxy-3,6,9-trimethyl-8-[(Z)-2-methylbut-2-enoyl]oxy-2-oxo-4,5,6a,7,8,9b-hexahydroazuleno[4,5-b]furan-7-yl] octanoate
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- -20°C
- Appropriate long-term storage conditions
- -20°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
SERCA1 ATPase also known as sarco/endoplasmic reticulum Ca2+ ATPase 1 is an important enzyme responsible for the active transport of Ca2+ ions from the cytosol into the sarcoplasmic reticulum which is important for muscle relaxation. This protein has a molecular weight of about 110 kDa. SERCA1 ATPase predominantly expresses in fast-twitch skeletal muscle allowing these muscles to relax rapidly after contraction. The enzyme utilizes ATP to pump calcium ions which highlights its role as an ATPase protein and its functionality in maintaining calcium homeostasis.
- Biological function summary
SERCA1 ATPase ensures proper calcium regulation and muscle function by facilitating the reuptake of Ca2+ ions into the sarcoplasmic reticulum following muscle contraction. It does not operate as part of a complex but plays a significant role in calcium ion translocation thereby regulating muscle contraction-relaxation cycles. This ATPase protein is directly involved in muscle physiology and its efficient function is critical for fast muscle fibers.
- Pathways
SERCA1 ATPase is a significant component of the calcium signaling and muscle contraction pathways. In the context of muscle contraction the release and reuptake of Ca2+ ions regulated by SERCA1 ATPase are central events. The protein works closely with the ryanodine receptor (RyR) and calsequestrin which also participate in the modulation of intracellular calcium levels. Their interactions ensure precise coordination during muscle contraction and relaxation processes.
- Associated diseases and disorders
Mutations or dysregulation of SERCA1 ATPase can lead to conditions such as Brody disease and certain forms of myopathy. Brody disease is characterized by impaired muscle relaxation which directly relates to the malfunctioning of this Ca2+ ATPase. Additionally the disrupted function of SERCA1 ATPase may also involve interactions with other proteins like the ryanodine receptor which can exacerbate muscle-related symptoms and contribute to the pathophysiology of these disorders.
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Chemical Structure - Thapsigargin, Ca2+-ATPase inhibitor (ab120286)
2D chemical structure image of ab120286, Thapsigargin, Ca2+-ATPase inhibitor
Functional Studies - Thapsigargin, Ca2+-ATPase inhibitor (ab120286)
ab58668 staining ATF3 in serum starved A549 cells treated with thapsigargin (ab120286), by ICC/IF. Increase of ATF3 correlates with increased concentration of thapsigargin, as described in literature.
The cells were incubated at 37°C for 1h in media containing different concentrations of ab120286 (thapsigargin) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab58668 (10 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-mouse polyclonal antibody (Goat Anti-Mouse IgG H&L (DyLight® 488) preadsorbed ab96879) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
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