Dalazatide  (Synonyms: ShK-186)

Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease^[1][2][3].

Dalazatide (ShK-186) (0-1000 pM) blocks the Kv1.3 current in the Ova-specific GFP+ effector memory T (Tem) cells in a dose-dependent manner with a K_d of 65 ± 5 pM^[3].
Dalazatide (0-100 nM; 3 days) inhibits CCR7⁻ T cell proliferation in a dose-dependent manner^[3].
Dalazatide (100 nM; 30 min) immobilizes effector memory T (Tem) cells at inflammatory sites by suppressing calcium signaling and thereby preventing β1 integrin activation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dalazatide (ShK-186) (100 μg/kg; s.c.; once) inhibits delayed-type hypersensitivity and suppresses the in vivo motility and activation of Tem cells in rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

4442.10

C₁₈₄H₂₉₆N₅₇O₅₅PS₇

1081110-69-1

Solid

White to off-white

H-{pY}-{AEEA}-Arg-Ser-Cys-Ile-Asp-Thr-Ile-Pro-Lys-Ser-Arg-Cys-Thr-Ala-Phe-Gln-Cys-Lys-His-Ser-Met-Lys-Tyr-Arg-Leu-Ser-Phe-Cys-Arg-Lys-Thr-Cys-Gly-Thr-Cys-NH2 (disulfide bridge:Cys5-Cys37,Cys14-Cys30,Cys19-Cys34)

H-{pY}-{AEEA}-RSCIDTIPKSRCTAFQCKHSMKYRLSFCRKTCGTC-NH2 (disulfide bridge:Cys5-Cys37,Cys14-Cys30,Cys19-Cys34)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Olsen C, et al. Dalazatide (ShK-186), a first-in-class peptide inhibitor of Kv1. 3 potassium channels, demonstrates safety, tolerability and proof of concept of efficacy in patients with active plaque psoriasis. J. Invest. Dermatol., 2016, 136(8).

  [2]. Stevens A M, et al. Thu0285 Dalazatide, an Inhibitor of the KV1. 3 Channel on Activated Effector Memory T Cells, Has Immunotherapy Potential in Systemic Lupus Erythematosus. 2016.

  [3]. Matheu MP, et al. Imaging of effector memory T cells during a delayed-type hypersensitivity reaction and suppression by Kv1.3 channel block. Immunity. 2008 Oct 17;29(4):602-14.  [Content Brief]