(Syn. : Potassium channel toxin ShK, kappa-stichotoxin-She3a, kappa-SHTX-She3a)
ShK (Stichodactyla Toxin) | Product ID | L8527-100UG |
| Name | ShK (Stichodactyla Toxin) |
| Molecular formula | C169H280N54O48S7 |
| Description |
A 35 amino-acids peptide with 3 disulfide bridges , synthetic, initially isolated from the venom of the Sun anemone Stichodactyla helianthus. |
| Biological activity | Kappa-stichotoxin-She3a (ShK) inhibits voltage-dependent potassium channels. It blocks Kv1.3 (KCNA3) potently and also Kv1.1 (KCNA1), Kv1.4 (KCNA4) and Kv1.6 (KCNA6) respectively with a Kd of 11 pM, 16 pM, 312 pM and 165 pM. Less potently blocks Kv1.4/KCNA4 (IC50=0.31 nM), and Kv1.6/KCNA6 (IC50=0.16 nM). It shows moderate activity on Kv1.2/KCNA2 (IC50=9 nM), Kv1.7/KCNA7 (IC50=11.5 nM), and KCa3.1/KCNN4 (Kd=0.03-30 nM). It Blocks Kv channels by binding to a shallow vestibule at the outer entrance to the ion conduction pathway and occluding the entrance to the pore (PubMed:10419508, PubMed:9830012). Interestingly, it was also demonstrated that ShK potently inhibits the hKv3.2b channel with an IC50 value of approximately 0.6 nM. ShK does not show or very weak activity on Kv1.5/KCNA5, Kv3.1/KCNC1, and Kv3.4/KCNC4 (IC50>100 nM). |
Packaging and Prices
| Packaging | Price (€) | Quantité | Buy Now |
|---|---|---|---|
| 1 Unité(s) | 340.00 | ||
| 5 Unité(s) | 1 360.00 | ||
| For quotation of big quantities, please Contact us | |||
Product Technical Documents
 | Safety Data Sheet Available on request, please Contact us Ref. SDS_L8527-100UG : unit price : free of charge |
Chemical and Physical Properties
| Product code | L8527-100UG | Molecular weight | 4057.92 Da |
| Product name | ShK (Stichodactyla Toxin) | Physical form | White lyophilized solid |
| CAS No. | 172450-46-3 | Melting point | |
| RTECS | NA | Solubility | water and saline buffer |
| UNIPROT | P29187 | Optical Activity | |
| PubChem SID | |||
| PubChem CID | 131676658 | ||
| Purity | > 98 % | ||
| Toxicity(LD50) | No Data | ||
| Chemical Name | |||
| Storage & Reconstitution Recommandations |
Stable at room temperature, store preferably at 4°C |
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| Savety Recommandations | |||
Bibliographic References
| Product code | L8527-100UG |
| Product name | ShK (Stichodactyla Toxin) |
- 1. Beeton C., et al. (2005) Targeting effector memory T cells with a selective peptide inhibitor of Kv1.3 channels for therapy of autoimmune diseases. Mol Pharmacol. ;
2. Castaneda, O., et al. (1995) Characterization of a potassium channel toxin from the Caribbean Sea anemone Stichodactyla helianthus, Toxicon. ;
3. Chen R., et al. (2011) Modeling the binding of three toxins to the voltage-gated potassium channel (Kv1.3). Biophys J. ;
4. Gilhar A., et al. (2011) The beneficial effect of blocking Kv1.3 in the psoriasiform SCID mouse model. J Invest Dermatol. ;
5. Grgic I., et al. (2009) Blockade of T-lymphocyte KCa3.1 and Kv1.3 channels as novel immunosuppression strategy to prevent kidney allograft rejection. Transplant Proc. ;
6. Jin L, Wu Y. (2007) Molecular mechanism of the sea anemone toxin ShK recognizing the Kv1.3 channel explored by docking and molecular dynamic simulations. J Chem Inf Model. ;
7. Norton RS., et al. (2004) Potassium channel blockade by the sea anemone toxin ShK for the treatment of multiple sclerosis and other autoimmune diseases. Curr Med Chem. ;
8. Panyi G, et al. (2006) K+ channel blockers: novel tools to inhibit T cell activation leading to specific immunosuppression. Curr Pharm Des. ;
9. Pennington MW., et al. (1996) An essential binding surface for ShK toxin interaction with rat brain potassium channels. Biochemistry. ;
10. Tarcha EJ., et al. (2012) Durable pharmacological responses from the peptide ShK-186, a specific Kv1.3 channel inhibitor that suppresses T cell mediators of autoimmune disease. J Pharmacol Exp Ther. ;
11. Tudor, J. E., et al. (1996) Solution structure of ShK toxin, a novel potassium channel inhibitor from a sea anemone, Nat Struct Biol. ;
12. Yan L., et al. (2005) Stichodactyla helianthus peptide, a pharmacological tool for studying Kv3.2 channels. Mol Pharmacol,
Links
| Product code | L8527-100UG |
| Product name | ShK (Stichodactyla Toxin) |
| External Links |
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