SML3140
GsMTx4 trifluoroacetate
≥95% (HPLC), powder, TRPC1 and TRPC6 inhibitor
Synonyme(s) :
1-amino-Cy5-glucose, Cyanine-based 1-amino-1-deoxy-β-glucose conjugate, Cy5-linked 1amino-glucose, GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2 trifluoroacetate(Disulfide: 2-17, 9-23, 16-30), Gly-Cys-Leu-Glu-Phe-Trp-Trp-Lys-Cys-Asn-Pro-Asn-Asp-Asp-Lys-Cys-Cys-Arg-Pro-Lys-Leu-Lys-Cys-Ser-Lys-Leu-Phe-Lys-Leu-Cys-Asn-Phe-Ser-Phe-NH2 trifluoroacetate (Disulfide: 2-17, 9-23, 16-30), Grammostola Mechanotoxin #4 trifluoroacetate, GsMTx-4 trifluoroacetate, L-GsMTx trifluoroacetate
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About This Item
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produits recommandés
product name
GsMTx4 trifluoroacetate, ≥95% (HPLC)
Niveau de qualité
Pureté
≥95% (HPLC)
Forme
powder
Couleur
white to beige
Température de stockage
−20°C
Description générale
Grammostola mechanotoxin #4 (GsMTx4), a gating modifier peptide, is obtained from spider venom. This 34-amino-acid peptide is a small (3-5 kD) amphipathic molecule built on a conserved inhibitory cysteine-knot (ICK) backbone. The structure of GsMTx4 has a belt of charged residues surrounding a hydrophobic patch. GsMTx4 acts as an inhibitor of cationic mechanosensitive channels (MSCs) belonging to the Piezoand transient receptor potential (TRP) channel families. It is different from other spider venom peptides because it can inhibit these channels regardless of their shape, and both its L- and D-forms can have this effect. GsMTx4 has a unique structure and carries a positive charge due to its six lysine residues which can affect membrane binding. This peptide has become a valuable tool in research to identify the roles of excitatory MSCs in normal physiology and pathology. It can also inhibit stretch-activated big potassium channels (SAKcaC). The presence of positively charged residues in GsMTx4 is thought to play a role in peptide channel-lipid interaction. It can effectively reduce arrhythmias by inhibiting stretch-activated channels (SACs) in the heart. GsMTx4 also serves as an inhibitor of histone acetylation inhibitor I-BET 762 and Piezo 1 inhibitor.
Application
GsMTx4 trifluoroacetate has been used in drug treatment as a supplement in cell culture medium to treat mouse hippocampal neurons to block cationic MSCs in cortical neurons. It has also been used as a specific inhibitor to incubate cementoblasts to study its effects on the response of cementoblasts to investigate if cementum repair was impaired by compression.
Actions biochimiques/physiologiques
GsMTx4 (Grammostola Mechanotoxin #4) is a tarantula venom-derived 34-mer amphipathic cysteine knot peptide that exerts its cationic mechanosensitive channels (MSCs; stretch-gated ion channels or SACs) modulatory activity by changing local membrane properties near the channels. GsMTx4 negatively regulates TRPC1/5/6 and Piexo1/2, while potentiating TREK-1 and TRPA1 activity. In addition, GsMTx4 can either hamper (2-4 μM) or facilitate (12-20 μM) the gating of prokaryotic E. coli cytoplasmic membrane MscS and MscK in a biphasic manner. GsMTx4 is also reported to inhibit Nav1.1 (SCN1A), Nav1.2 (SCN2A), Nav1.3 (SCN3A), Nav1.4 (SCN4A), Nav1.5 (SCN5A), Nav1.6 (SCN8A), Nav1.7 (SCN9A), hERG1/2/3 (KCNH2/6/7), but not hKV1.1 (KCNA1) or hKV1.4 (KCNA4).
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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Ana Gomis et al.
The Journal of physiology, 586(23), 5633-5649 (2008-10-04)
Transient receptor potential (TRP) channels mediate a wide array of sensory functions. We investigated the role of TRPC5, a poorly characterized channel widely expressed in the central and peripheral nervous system, as a potential osmosensory protein. Here we show that
Maria A Spassova et al.
Proceedings of the National Academy of Sciences of the United States of America, 103(44), 16586-16591 (2006-10-24)
The TRP family of ion channels transduce an extensive range of chemical and physical signals. TRPC6 is a receptor-activated nonselective cation channel expressed widely in vascular smooth muscle and other cell types. We report here that TRPC6 is also a
Kimberly Laskie Ostrow et al.
Toxicon : official journal of the International Society on Toxinology, 42(3), 263-274 (2003-10-16)
The peptide GsMTx4 from the tarantula venom (Grammostola spatulata) inhibits mechanosensitive ion channels. In this work, we report the cDNA sequence encoding GsMTx4. The gene is translated as a precursor protein of 80 amino acids. The first 21 amino acids
Elisa Redaelli et al.
The Journal of biological chemistry, 285(6), 4130-4142 (2009-12-04)
Venom-derived peptide modulators of ion channel gating are regarded as essential tools for understanding the molecular motions that occur during the opening and closing of ion channels. In this study, we present the characterization of five spider toxins on 12
Two types of peptides derived from the neurotoxin GsMTx4 inhibit a mechanosensitive potassium channel by modifying the mechanogate
Zhou N, et al.
The Journal of biological chemistry (2022)
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