GsMTx4

Name: GsMTx4
Brand: Tocris Bioscience
SKU: 4912
Rating: 4 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4912

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Citations (75)

COA / SDS

TRPC1 and TRPC6 inhibitor; inhibits mechanosensitive ion channels

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Technical Data
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Product Description
Licensing Information
Product Specifications
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Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

TRPC1 and TRPC6 inhibitor; inhibits mechanosensitive ion channels

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Product Description

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

Product Specifications

Molecular Weight

4095.86

Formula

C₁₈₅H₂₇₃N₄₉O₄₅S₆

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.

Solubility

Soluble to 1mg/ml in water

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Background References

References are publications that support the biological activity of the product.

Pathak Stretch-activated ion channel Piezo1 directs lineage choice in human neural stem cells. Proc.Natl.Acad.Sci.U.S.A. 2014 PMID: 25349416
Acheva Adipokine leptin co-operates with mechanosensitive Ca^{2 +}-Channels and triggers actomyosin-mediated motility of breast epithelial cells. Front.Cell.Dev.Biol. 2021 PMID: 33490070
Velasco-Estevez Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia 2020 PMID: 31596529
Beaulieu-Laroche TACAN is an ion channel involved in sensing mechanical pain. Cell 2020 PMID: 32084332
Bae The mechanosensitive ion channel Piezo1 is inhibited by the peptide GsMTx4. Biochemistry 2011 PMID: 21696149
Drew High-threshold mechanosensitive ion channels blocked by a novel conopeptide mediate pressure-evoked pain. PLoS One 2007 PMID: 17565368
Suchyna Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J.Gen.Physiol. 2000 PMID: 10779316
Bowman Mechanosensitive ion channels and the peptide inhibitor GsMTx-4: history, properties, mechanisms and pharmacology. Toxicon. 2007 PMID: 17157345