ADWX 1

Cat. No.: HY-P1409: FAQs
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ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC₅₀ value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases.

For research use only. We do not sell to patients.

ADWX 1 Chemical Structure

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References
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Description

IC₅₀ & Target^[1]

Kv1.3

1.89 pM (IC₅₀)

Kv1.1

0.65 nM (IC₅₀)

In Vitro

ADWX 1 (1,10 nM, 1 h) inhibits IL-2 and IFN-γ productions, and inhibits humans CD4⁺ CCR7^- T_EM cells activation selectively^[2].
ADWX 1 (1,10 nM, 50 min) reduces [Ca²⁺] in activated CD4⁺ CCR7^- T_CM cells from EAE rats^[2].
ADWX 1 (1,10 nM, 1 h) reduces NF-κB activation and suppresses Kv1.3 expression at both mRNA and protein levels preferentially in myelin basic protein (MBP) (HY-P77995)-stimulated CD4⁺ CCR7^- T cells from EAE rats^[2].
ADWX 1 (1,10 nM, 3 days) suppresses Th17 activation but not differentiation in CD4⁺ CCR7^- T cells^[2].

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

RT-PCR^[2]

Cell Line:	CD4⁺ CCR7^- T cells from EAE rats
Concentration:	1, 10 nM
Incubation Time:	1 h
Result:	Suppressed Kv1.3 gene mRNA expression preferentially.

Western Blot Analysis^[2]

Cell Line:	CD4⁺ CCR7^- T cells from EAE rats
Concentration:	1, 10 nM
Incubation Time:	1 h
Result:	Suppressed Kv1.3 protein expression preferentially.

In Vivo

ADWX 1 (100 μg/kg/day, s.c., 3 days) ameliorates the disease through the inhibition of IL-2 and IFN-γ productions and CCR7^- T_EM proliferation in experimental autoimmune encephalomyelitis (EAE) of Sprague-Dawley rats^[2].
ADWX 1 (5/10 mg/kg, s.c., 2 weeks) induces no pathological changes in the behavior or tissues of the rats (acute toxicity assay)^[2].

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

Animal Model:	Stable symptoms of acute experimental autoimmune encephalomyelitis (EAE) were induced by immunizing Sprague-Dawley rats^[2].
Dosage:	100 μg/kg/day, 3 days
Administration:	subcutaneous injection (s.c.)
Result:	Reduced neurological scores compared with vehicle-treated rats on days 10, 11, 12, 13 and 14. Reduced in inflammatory infiltrates and demyelination in the affected spinal cord significantly. Inhibited IL-2 and IFN-γ productions. Inhibited the T cell proliferation triggered by high and low concentrations of myelin antigen in a dose-dependent manner. Decreased CD4⁺ CCR7^- T_EM cells.

Molecular Weight

4071.85

Formula

C₁₆₉H₂₈₁N₅₇O₄₆S₇

Sequence

Val-Gly-Ile-Asn-Val-Lys-Cys-Lys-His-Ser-Arg-Gln-Cys-Leu-Lys-Pro-Cys-Lys-Asp-Ala-Gly-Met-Arg-Phe-Gly-Lys-Cys-Thr-Asn-Gly-Lys-Cys-His-Cys-Thr-Pro-Lys (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34)

Sequence Shortening

VGINVKCKHSRQCLKPCKDAGMRFGKCTNGKCHCTPK (Disulfide bonds: Cys7-Cys27, Cys13-Cys32, Cys17-Cys34)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Han S, et al. Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease. J Biol Chem. 2008 Jul 4;283(27):19058-65. [Content Brief]

[2]. Li Z, et al. Selective inhibition of CCR7(-) effector memory T cell activation by a novel peptide targeting Kv1.3 channel in a rat experimental autoimmune encephalomyelitis model. J Biol Chem. 2012 Aug 24;287(35):29479-94. [Content Brief]

ADWX 1 Related Classifications

Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ADWX 1ADWX1ADWX-1Potassium ChannelKcsAT cellEAEAutoimmune DiseaseInhibitorinhibitorinhibit

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