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Submit ReviewGsMTx4
Description: TRPC1 and TRPC6 inhibitor; inhibits mechanosensitive ion channels
Purity: ≥95% (HPLC)
Biological Activity for GsMTx4
GsMTx4 is a spider venom peptide that selectively inhibits cationic mechanosensitive channels (MSCs) such as TRPC1 and TRPC6 and Piezo channels. GsMTx4 blocks stretch-activated cation channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells. GsMTx4 also inhibits TACAN, a mechanosensitive ion channel involved in the pain response. GsMTx4 decreases the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells. GsMTx4 is neuroprotective and inhibits lysophosphatidylcholine-induced astrocyte toxicity in vivo in mice. GsMTx4 suppresses neurogenesis and enhances astrogenesis in human neural stem cells.
Licensing Information
Sold under license from The Research Foundation of The State University of New York
Technical Data for GsMTx4
| M. Wt | 4095.86 |
| Formula | C185H273N49O45S6 |
| Sequence |
GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF (Modifications: Disulfide bridges: 2-17, 9-23, 16-30), Phe-34 = C-terminal amide) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 1209500-46-8 |
| PubChem ID | 90488987 |
| InChI Key | WVDNTWXIIKNMHY-UHFFFAOYSA-N |
| Smiles | [H]NCC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC1=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(N)=O |
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 GsMTx4
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for GsMTx4
References for GsMTx4
References are publications that support the biological activity of the product.
Bowman et al (2007) Mechanosensitive ion channels and the peptide inhibitor GsMTx-4: history, properties, mechanisms and pharmacology. Toxicon. 49 249 PMID: 17157345
Suchyna et al (2000) Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J.Gen.Physiol. 115 583 PMID: 10779316
Drew et al (2007) High-threshold mechanosensitive ion channels blocked by a novel conopeptide mediate pressure-evoked pain. PLoS One 2 e515 PMID: 17565368
Bae et al (2011) The mechanosensitive ion channel Piezo1 is inhibited by the peptide GsMTx4. Biochemistry 50 6295 PMID: 21696149
Beaulieu-Laroche et al (2020) TACAN is an ion channel involved in sensing mechanical pain. Cell 180 956 PMID: 32084332
Acheva et al (2021) Adipokine leptin co-operates with mechanosensitive Ca2 +-Channels and triggers actomyosin-mediated motility of breast epithelial cells. Front.Cell.Dev.Biol. 8 607038 PMID: 33490070
Velasco-Estevez et al (2020) Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia 68 356 PMID: 31596529
Pathak et al (2014) Stretch-activated ion channel Piezo1 directs lineage choice in human neural stem cells. Proc.Natl.Acad.Sci.U.S.A. 111 16148 PMID: 25349416
If you know of a relevant reference for GsMTx4, please let us know.
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Keywords: GsMTx4, GsMTx4 supplier, TRPC, transient, receptor, potential, TRPC1, and, TRPC6, mechanosensitive, ion, channels, MSCs, blockers, blocks, inhibits, inhibitors, venoms, TACAN, pain, TMEM120A, TMEM, neuroprotective, Piezo, Channels, Other, Channel, Modulators, Neural, Stem, Cells, 4912, Tocris Bioscience
10 Citations for GsMTx4
Citations are publications that use Tocris products. Selected citations for GsMTx4 include:
Agbani et al (2018) Aquaporin-1 regulates platelet procoagulant membrane dynamics and in vivo thrombosis. JCI Insight 3 PMID: 29769447
Wong et al (2018) Mechanical Stretching Simulates Cardiac Physiology and Pathology through Mechanosensor Piezo1. J Clin Med 7 PMID: 30400259
Matthew J et al (2017) Stimulation of 3D osteogenesis by mesenchymal stem cells using a nanovibrational bioreactor. Nat Biomed Eng 1 758-770 PMID: 31015671
Yuri et al (2021) Selective Chemical Activation of Piezo1 in Leukemia Cell Membrane: Single Channel Analysis. Int J Mol Sci 22 PMID: 34360605
Sun et al (2019) The mechanosensitive Piezo1 channel is required for bone formation. Elife 8 PMID: 31290742
Dela Paz (2018) Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun 497 220 PMID: 29428723
Vincent et al (2022) Mechanotransduction in hippocampal neurons operates under localized low picoNewton forces. iScience 25 103807 PMID: 35198872
Rupalatha et al (2022) Mechanical Load and Piezo1 Channel Regulated Myosin II Activity in Mouse Lenses. Int J Mol Sci 23 PMID: 35563101
Ting et al (2022) Mechanosensation by endothelial PIEZO1 is required for leukocyte diapedesis. Blood 140 171-183 PMID: 35443048
Beaulieu-Laroche et al (2020) TACAN is an ion channel involved in sensing mechanical pain. Cell 180 956 PMID: 32084332
Do you know of a great paper that uses GsMTx4 from Tocris? Please let us know.
Reviews for GsMTx4
Average Rating: 4 (Based on 1 Review.)
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a mechanosensitive channel blocker.
By
Hyun Choi on 02/19/2018
Assay Type: Ex Vivo
Species: Rat
Cell Line/Tissue: Applied to brain slices
It blocks mechanosensitive channels such as TRPC1 and 6.Dissolved in artificial cerebrospinal fluid (acsf) at 20 microM.