(Dap22)-ShK

50 180 

(Dap22)-ShK is a highly selective Kv1.3 blocker

(Dap22)-ShK (ShK Dap22) peptide is a synthetic derivative of the well-known ShK toxin #08SHK001 (Stichodactyla helianthus neurotoxin) isolated from the venom of the Carribean sea anemone Stoichactis helianthus. Wild-type ShK blocks potently Kv1.3 (KCNA3), Kv1.1 (KCNA1), Kv1.4 (KCNA4), and Kv1.6 (KCNA6) respectively with a Kd of 11 pM,16 pM, 312 pM and 165 pM. In (Dap22)-ShK, lysine22 has been replaced by a diaminopropionic acid (Dap) residue that greatly improves the selectivity of the peptide for the voltage-gated potassium channel Kv1.3 (IC50 around 23 pM) against Kv1.1 (1.8 nM), Kv1.4 (37 nM) and Kv1.6 (10 nM) channels. The high selectivity of (Dap22)-Shk is achieved thanks to the strong binding between the Dap and His404 / Asp386 residues of Kv1.3 channel. (Dap22)-ShK inhibits T cell proliferation induced by anti-CD3 at subnanomolar concentrations.

Contact us
SKU: 13SHD001 Category: Tags: , ,

Description

AA sequence: Arg-Ser-Cys3-Ile-Asp-Thr-Ile-Pro-Lys-Ser-Arg-Cys12-Thr-Ala-Phe-Gln-Cys17-Lys-His-Ser-Met-Dap-Tyr-Arg-Leu-Ser-Phe-Cys28-Arg-Lys-Thr-Cys32-Gly-Thr-Cys35-OH
Disulfide bonds: Cys3-Cys35, Cys12-Cys28 and Cys17-Cys32
Length (aa): 35
Formula: C166H268N54O48S7
Molecular Weight: 4012.8 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number: 220384-25-8
Source: Synthetic
Purity rate: > 97%

Kaliotoxin-1MargatoxinHsTx1
MaurotoxinShK – Stichodactyla toxinADWX-1
Agitoxin-2TMR-ShK
Hypoxia modulates early events in T cell receptor-mediated activation in human T lymphocytes via Kv1.3 channels

Potassium channel blockade by the sea anemone toxin ShK for the treatment of multiple sclerosis and other autoimmune diseases

Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile

Mutating a critical lysine in ShK toxin alters its binding configuration in the pore-vestibule region of the voltage-gated potassium channel, Kv1.3

Selective blockade of T lymphocyte K(+) channels ameliorates experimental autoimmune encephalomyelitis, a model for multiple sclerosis

ShK-Dap22, a potent Kv1.3-specific immunosuppressive polypeptide

Sign Up to our Newsletter

    Placeholder

    (Dap22)-ShK

    50 180 Quote request