GsMTx4

Pricing Availability   Qty
Description: TRPC1 and TRPC6 inhibitor; inhibits mechanosensitive ion channels
Purity: ≥95% (HPLC)
Datasheet
Citations (10)
Reviews (1)

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

Certificate of Analysis / Product Datasheet
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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


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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:

Beaulieu-Laroche et al (2020) TACAN is an ion channel involved in sensing mechanical pain. Cell 180 956 PMID: 32084332

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

Sun et al (2019) The mechanosensitive Piezo1 channel is required for bone formation. Elife 8 PMID: 31290742

Yuri et al (2021) Selective Chemical Activation of Piezo1 in Leukemia Cell Membrane: Single Channel Analysis. Int J Mol Sci 22 PMID: 34360605

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

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

Dela Paz (2018) Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun 497 220 PMID: 29428723


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Reviews for GsMTx4

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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.