GsMTx-4 | Alomone Labs STG-100 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

GsMTx-4

catalog :

STG-100

more info or order :

Alomone Labs product webpage

citations: 18

Reference
Liu L, Zhang Q, Xiao S, Sun Z, Ding S, Chen Y, et al. Inhibition of Shear-Induced Platelet Aggregation by Xueshuantong via Targeting Piezo1 Channel-Mediated Ca2+ Signaling Pathway. Front Pharmacol. 2021;12:606245 pubmed publisher
He J, Fang B, Shan S, Xie Y, Wang C, Zhang Y, et al. Mechanical stretch promotes hypertrophic scar formation through mechanically activated cation channel Piezo1. Cell Death Dis. 2021;12:226 pubmed publisher
Wong S, Lenzini S, Bargi R, Feng Z, Macaraniag C, Lee J, et al. Controlled Deposition of 3D Matrices to Direct Single Cell Functions. Adv Sci (Weinh). 2020;7:2001066 pubmed publisher
Velasco Estevez M, Gadalla K, Liñan Barba N, Cobb S, Dev K, Sheridan G. Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia. 2020;68:356-375 pubmed publisher
Zhao C, Sun Q, Tang L, Cao Y, Nourse J, Pathak M, et al. Mechanosensitive Ion Channel Piezo1 Regulates Diet-Induced Adipose Inflammation and Systemic Insulin Resistance. Front Endocrinol (Lausanne). 2019;10:373 pubmed publisher
Pakshir P, Alizadehgiashi M, Wong B, Coelho N, Chen X, Gong Z, et al. Dynamic fibroblast contractions attract remote macrophages in fibrillar collagen matrix. Nat Commun. 2019;10:1850 pubmed publisher
Hennes A, Held K, Boretto M, De Clercq K, Van den Eynde C, Vanhie A, et al. Functional expression of the mechanosensitive PIEZO1 channel in primary endometrial epithelial cells and endometrial organoids. Sci Rep. 2019;9:1779 pubmed publisher
Wen L, Feil S, Wolters M, Thunemann M, Regler F, Schmidt K, et al. A shear-dependent NO-cGMP-cGKI cascade in platelets acts as an auto-regulatory brake of thrombosis. Nat Commun. 2018;9:4301 pubmed publisher
Mikolajewicz N, Zimmermann E, Willie B, Komarova S. Mechanically stimulated ATP release from murine bone cells is regulated by a balance of injury and repair. elife. 2018;7: pubmed publisher
dela Paz N, Frangos J. Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun. 2018;497:220-225 pubmed publisher
Maffioli E, Schulte C, Nonnis S, Grassi Scalvini F, Piazzoni C, Lenardi C, et al. Proteomic Dissection of Nanotopography-Sensitive Mechanotransductive Signaling Hubs that Foster Neuronal Differentiation in PC12 Cells. Front Cell Neurosci. 2017;11:417 pubmed publisher
Ilkan Z, Wright J, Goodall A, Gibbins J, Jones C, Mahaut Smith M. Evidence for shear-mediated Ca2+ entry through mechanosensitive cation channels in human platelets and a megakaryocytic cell line. J Biol Chem. 2017;292:9204-9217 pubmed publisher
Johansson S, Andersen X, Hansen R, Povlsen G, Edvinsson L. Cerebrovascular endothelin-1 hyper-reactivity is associated with transient receptor potential canonical channels 1 and 6 activation and delayed cerebral hypoperfusion after forebrain ischaemia in rats. Acta Physiol (Oxf). 2015;214:376-89 pubmed publisher
Vemana H, Karim Z, Conlon C, Khasawneh F. A critical role for the transient receptor potential channel type 6 in human platelet activation. PLoS ONE. 2015;10:e0125764 pubmed publisher
Li C, Rezania S, Kammerer S, Sokolowski A, DeVaney T, Gorischek A, et al. Piezo1 forms mechanosensitive ion channels in the human MCF-7 breast cancer cell line. Sci Rep. 2015;5:8364 pubmed publisher
Bressan M, Louie J, Mikawa T. Hemodynamic forces regulate developmental patterning of atrial conduction. PLoS ONE. 2014;9:e115207 pubmed publisher
Wang H, Tibbitt M, Langer S, Leinwand L, Anseth K. Hydrogels preserve native phenotypes of valvular fibroblasts through an elasticity-regulated PI3K/AKT pathway. Proc Natl Acad Sci U S A. 2013;110:19336-41 pubmed publisher
Arora P, Wang Y, Bresnick A, Dawson J, Janmey P, McCulloch C. Collagen remodeling by phagocytosis is determined by collagen substrate topology and calcium-dependent interactions of gelsolin with nonmuscle myosin IIA in cell adhesions. Mol Biol Cell. 2013;24:734-47 pubmed publisher

image

image 1 :

Alomone Labs GsMTx-4 inhibits NaV1.7 channel currents expressed inXenopusoocytes. - NaV1.7 currents were elicited by 100 ms voltage ramp from a holding potential of -100 mV to +30 mV applied every 10 sec using whole-cell voltage clamp technique. Left: Superimposed traces of NaV1.7 currents before (black) and during (green) application of 500 nMGsMTx-4(#STG-100). Right: GsMTx-4 dose response inhibition of NaV1.7 currents.

image 2 :

Inhibiting mechano-sensitive ion channels reduces valvular myofibroblast differentiation. - Immunocytochemical staining of VICs treated with the mechano-sensitve ion channel inhibitorGsMTX(#STG-100) at 5 ?M. ?SMA protein expression was reduced relative to the internal control GAPDH (not shown). Similarly ?SMA stress fibers (green) were inhibited by the inhibitor. Nuclei blue. (Scale bars 100 ?m.).Adapted fromWang H.et al.(2013) with permission of the National Academy of Sciences USA.

image 3 :

Expression of proNGF in mouse cortex - Immunohistochemical staining of perfusion-fixed mouse brain frozen sections using Guinea pigAnti-proNGFAntibody (#AGP-031) (1:400) followed by goat-anti-guinea pig-Cy3. proNGF staining (red) appears in the pyramidal layer (arrows). Nuclei were stained with DAPI (blue).

product information

cat :

STG-100

SKU :

STG-100_0.1 mg

Product Name :

GsMTx-4

Group Type :

Non Antibodies

Product Type :

Proteins

Accession :

Q7YT39

Accession Number :

https://www.uniprot.org/uniprotkb/Q7YT39/entry

Applications :

Electrophysiology

Formulation :

Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.

Storage After Reconstitution :

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Reconstitution and Solubility :

Centrifuge the vial (10,000 × g for 5 minutes) before adding solvent to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Gently tap, tilt, and roll the vial to aid dissolution. Avoid vigorous vortexing; light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.

Solubility :

Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.

Storage Before Reconstitution :

The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture.

Origin :

Grammostola rosea (Chilean rose tarantula) (Grammostola spatulata)

Source :

Synthetic peptide

Gene ID :

SCN9A, TRPC1, TRPC6, PIEZO1

Product Page - Scientific background :

GsMTx-4 is a 34 amino acid peptidyl toxin originally isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family1.This toxin inhibits different channels and in addition has antimicrobial activity. It blocks cation-selective mechanosensitive ion channels (strech-activated channels, SACs), without having an effect on whole-cell voltage-sensitive currents1. In addition, it inhibits atrial fibrillation2 as well as the membrane motor of outer hair cells3 at low doses. A medium toxicity on a large spectra of voltage-gated Na+ channels, namely NaV1.1, NaV1.2, NaV1.3, NaV1.4, NaV1.5, NaV1.6 and NaV1.7 was reported. GsMTx-4 also inhibits K+ channels KV11.1 and KV11.2, whereas it does not inhibit K+ channels KV1.1 (IC50 > 85 µM), KV1.4 (IC50 > 85 µM) and KV11.3 (IC50 = 53 µM)4. GsMTx-4 was also found to inhibit both TRPC1 and TRPC6 channels5,6, as well as Piezo1, the mechanosensitive channel7.Antimicrobial activity is shown against several Gram-positive and Gram-negative bacteria as well8.

Supplier :

Alomone Labs

Target :

NaV1.7 channels, TRPC1, TRPC6, Piezo1

Long Description :

A Blocker of NaV1.7, TRPC1, TRPC6 and Piezo1 Channels

Short Description :

A Blocker of NaV1.7, TRPC1, TRPC6 and Piezo1 Channels

MW :

4096 Da

Synonyms :

M-TRTx-Gr1a, M-theraphotoxin-Gr1a, GsMTx4

Modifications :

Disulfide bonds between: Cys2-Cys17, Cys9-Cys23, and Cys16-Cys30 Phe34 - C-terminal amidation

Molecular formula :

C185H273N49O45S6

Effective Concentration :

500 nM - 10 μM

Activity :

GsMTx-4 is an inhibitor of Na+ voltage-gated channels3 and cation-selective mechanosensitive channels1,2.

Storage of solutions :

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Purity :

≥98% (HPLC)

CAS No :

1209500-46-8

Form :

Lyophilized

Comment :

Contact Alomone Labs for technical support and product customization

Sequence :

GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2

Is Toxin :

Yes

UNSPSC :

12352202

Bioassay Tested :

yes

Steril endotoxin free :

more info or order :

Alomone Labs product webpage