| Field | Specification |
|---|---|
| Mfr No | |
| Accession Number | |
| Activity | |
| Alternative Names | Dalazatide, ShK-186 [SL5] |
| Cas No. | |
| Concentration | |
| Form | Lyophilized |
| Formulation | |
| Gene ID | |
| Molecular Weight | |
| Product Type | |
| Purity | |
| Reconstitution | |
| 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. |
| Source | Synthetic peptide |
| Species | |
| Storage | |
| Target |
Overview
ShK-186 is a research-grade protein/peptide reagent used in research settings. It is commonly applied as a tool reagent related to Kv1.3 biology and/or assay development. It is supplied in Lyophilized format to support flexible downstream use in RUO workflows. Researchers commonly pair it with applications such as Electrophysiology, Electrophysiology.
Key elements and design rationale
- Molecular identity: CAS: 1081110-69-1, MW: 4441 Da, Formula: C184H296N57O55S7P1.
- Source / origin: Stichodactyla helianthus (Sun anemone) (Stoichactis helianthus).
- Quality attributes: Purity: ≥98% (HPLC); Bioassay tested: Yes; Sterile / endotoxin-free: No.
Modifications
Disulfide bonds between: Cys3-Cys35, Cys12-Cys28 and Cys17-Cys32 Cys35- C-terminal amidation L-phosphotyrosine attached to the Arg1 at N-terminus via an AEEA linker (2-aminoethoxy-2-ethoxy acetic acid; mini-PEG).
When used as a biochemical or pharmacological tool, results are best interpreted relative to the experimental system (species, expression level, and assay readout) and with appropriate negative and competition-style controls where relevant. This product is intended for research use only.
Biological background
ShK-186 is a synthetic analog of ShK (#STS-400), a native 35 amino acid peptidyl toxin originally isolated from the nematocyst of the sea anemone Stichodactyla helianthus1. Native ShK blocks the voltage-gated potassium (KV)1.3, KV1.1, KV1.4, and KV1.6 at subnanomolar concentrations2. Its synthetic analog, ShK-186, is a highly specific Kv1.3 blocker with picomolar affinity and exhibited greater than 100-fold selectivity for Kv1.3 over Kv1.1 and other channels3,4. ShK-186 contains negatively charged amino acid L-phosphotyrosine attached to the N terminus via an AEEA (mini-PEG) hydrophilic linker and is amidated at C-terminus4.Kv channels play key roles in human physiology and pathology. The Kv1.3 channel in T lymphocytes is a validated therapeutic target for diverse autoimmune diseases5. This channel maintains the membrane potential of a sub-set of T lymphocytes known as effector memory (TEM) T cells, that mediate and play a major role in the pathogenesis of autoimmune diseases such as multiple sclerosis (MS), type 1 diabetes mellitus, rheumatoid arthritis (RA), and psoriasis4,6. ShK-186 (a.k.a. dalazatide) has been shown to be effective against autoimmune diseases in several models and being advanced as a treatment for multiple diseases, including inclusion body myositis, lupus, ANCA vasculitis, MS, psoriasis, psoriatic arthritis, RA, type 1 diabetes, inflammatory bowel diseases, and asthma. Moreover, proof of concept has been demonstrated for dalazatide therapy in a phase 1b psoriasis study 7-9.
Research relevance and current trends
- Using high-specificity ligands, toxins, and engineered peptides to dissect closely related receptor/channel subtypes and signaling microdomains.
- Pairing labeled (e.g., fluorescent) proteins/peptides with advanced imaging to map surface expression, trafficking, and nanoscale organization.
- Increasing emphasis on reproducibility through standardized characterization (identity, purity, and lot QC) and transparent reporting of reagent attributes.
Common research applications
- Electrophysiology: commonly used to compare signal, binding, or functional readouts across conditions without implying a specific protocol.
- Electrophysiology: commonly used to compare signal, binding, or functional readouts across conditions without implying a specific protocol.
Across these use cases, changes in signal or functional readout are generally interpreted as evidence of differences in target abundance, accessibility, or engagement, but alternative explanations (matrix effects, off-target interactions, or assay artifacts) should be considered.
Notes for experimental interpretation
- Assay context matters: binding assays, functional modulation, and detection workflows can yield different readouts even for the same target system.
- Target complexity: closely related family members, splice variants, and post-translational modifications can influence apparent specificity and potency.
- Matrix and sample effects: buffer composition, detergents, and biological matrices may alter stability or apparent activity; interpret with appropriate controls.
- Control concepts: include negative controls and orthogonal validation (e.g., genetic perturbation or alternative reagents) to support robust interpretation.
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