chemical

ShK-186

STS-390

STS-390_0.1 mg

ShK-186

Non Antibodies

Proteins

P29187

https://www.uniprot.org/uniprotkb/P29187/entry

Electrophysiology

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

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.

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.

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.

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

Stichodactyla helianthus (Sun anemone) (Stoichactis helianthus)

Synthetic peptide

KCNA3

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.

Alomone Labs

Kv1.3

A Potent Blocker of KV1.3

A Potent Blocker of KV1.3

4441 Da

Dalazatide, ShK-186 [SL5]

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).

C184H296N57O55S7P1

0.05 - 0.1 nM

ShK-186 is a potent and selective blocker of Kv1.3 voltage-gated K+ channels1.

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.

1-2 Business Days

Israel/IL

≥98% (HPLC)

1081110-69-1

Lyophilized

Contact Alomone Labs for technical support and product customization

L-pTyr-AEEA -RSCIDTIPKSRCTAFQCKHSMKYRLSFCRKTCGTC-NH2

Yes

12352202

yes

no

Electrophysiology