Smartox Biotechnology
 
작성일 : 13-09-06
[Smartox Biotechnology] 화학합성의 Potassium Channel Blocker Peptide Toxin(3)
Agitoxin-2 / (Dap22)-ShK / ADWX-1
 
화학합성의 각종 Potassium Channel Blocker Peptide Toxin (3)
 
Potassium channel 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
 
 
Agitoxin-2, Blocker of Kv1.1 and Kv1.3 channels
 
Agitoxin-2 is a potent and selective blocker of the Shaker type voltage-gated Kv1.3 and Kv1.1 channels. Agitoxin-2
inhibits Kv1.3 with an IC50 value of around 200 pM and Kv1.1 with an IC50 value of around 140 pM. This peptide toxin
was originally isolated from the venom of the Israeli scorpion L. quinquestriatus hebraeus
 
Details
AA sequence:
 
Gly-Val-Pro-Ile-Asn-Val-Ser-Cys8-Thr-Gly-Ser-Pro-Gln-Cys14-Ile-Lys-Pro-Cys18-Lys-Asp-Ala-Gly-Met-Arg-Phe-Gly-Lys-Cys28-Met-Asn-Arg-Lys-Cys33-His-Cys35-Thr-Pro-Lys-OH
 
 
Cys8-Cys28, Cys14-Cys33 and Cys18-Cys35
Length (aa):
 
38
Formula:
C169H278N54O48S8
Molecular Weight:
 
4090.89 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
Source:
Synthetic
Purity rate:
 
> 97%
 
References
1. Anangi R., et al. (2012) Recombinant Expression of Margatoxin and Agitoxin-2 in Pichia pastoris: An Efficient
   Method for production of KV1.3 Channel Blockers. PLoS ONE
2. Garcia, M.L. et al. (1994) Purification and characterization of three inhibitors of voltage-dependent K+ channels
   from Leiurus quinquestriatus var. hebraeus venom. Biochemistry
 
 
(Dap22)-ShK (Stichodactyla toxin), Selective blocker of Kv1.3
 
(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 voltage-gated Kv1.1, Kv1.3, Kv1.4 and Kv1.6 channels at equal subnanomolar
concentrations. In (Dap22)-ShK, lysine22 has been replaced by a diaminopropionic acid (Dap) residue that greatly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.
 
Details
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
 
 
Cys3-Cys35, Cys12-Cys28 and Cys17-Cys32
Length (aa):
 
35
Formula:
C166H268N57O48S7
Molecular Weight:
 
4012.8 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
CAS number:
220384-25-8
Source:
 
Synthetic
Purity rate:
 
>97%
 
References
1. Robbins JR., et al. (2005) Hypoxia modulates early events in T cell receptor-mediated activation in human T
   lymphocytes via Kv1.3 channels. J Physiol. PubMed link
2. Norton RS., et al. (2004) Potassium channel blockade by the sea anemone toxin ShK for the treatment of multiple
   sclerosis and other autoimmune diseases. Curr Med Chem. PubMed link
3. Middleton RE., et al. (2003) Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a
   novel pharmacological profile. Biochemistry. PubMed link
4. Lanigan MD., et al. (2002) Mutating a critical lysine in ShK toxin alters its binding configuration in the pore-vestibule
   region of the voltage-gated potassium channel, Kv1.3. Biochemistry. PubMed link
5. Beeton C., et al. (2001) Selective blockade of T lymphocyte K(+) channels ameliorates experimental autoimmune
   encephalomyelitis, a model for multiple sclerosis. Proc Natl Acad Sci USA. PubMed link
6. Kalman K, et al. (1998) ShK-Dap22, a potent Kv1.3-specific immunosuppressive polypeptide. J Biol Chem.
 
 
ADWX-1, Kv1.3 channel blocker
 
ADWX-1 is an optimised synthetic analog of the scorpion peptide BmKTx. ADWX-1 is known to block voltage gated
Kv1.3 channel with a high affinity (IC50 = 1.89 pM) and selectivity (340 fold greater affinity than for voltage-
dependent ). ADWX1 is an interesting therapeutic candidate to treat auto-immune disorders such as multiple
sclerosis, type-1 diabetes, rheumatoid arthritis and psoriasis. This peptide is a valuable tool for studying the
structure-function of Kv1.3 channel and auto-immunity pathways.
 
Details
AA sequence:
 
Val-Gly-Ile-Asn-Val-Lys-Cys7-Lys-His-Ser-Arg-Gln-Cys13-Leu-Lys-Pro-Cys17-Lys-Asp-Ala-Gly-
Met-Arg-Phe-Gly-Lys-Cys27-Thr-Asn-Gly-Lys-Cys32-His-Cys34-Thr-Pro-Lys-OH
 
 
(Disulfide bonds between Cys7-Cys27, Cys13-Cys32 and Cys17-Cys34)
Length (aa):
 
37
Formula:
C169H281N57O46S7
Molecular Weight:
 
4071.90 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
Source:
Synthetic
Purity rate:
 
>98
 
References
1. Song Han , et al. (2008) Structural Basis of a Potent Peptide Inhibitor Designed for Kv1.3 Channel, a Therapeutic
   Target of Autoimmune Disease. JBC PubMed link
2. Zhi Li, et al.(2012) Selective Inhibition of CCR7− Effector Memory T Cell Activation by a Novel Peptide Targeting
   Kv1.3 Channel in a Rat Experimental Autoimmune Encephalomyelitis Model. JBC PubMed link
3. Yin SJ (2008) Different residues in channel turret determining the selectivity of ADWX-1 inhibitor peptide between
   Kv1.1 and Kv1.3 channels. Journal of proteome research PubMed link
 
 
Ordering informations
 
Catalog No.
Product Name
Size
13AGI002
Agitoxin-2
0.1mg, 0.5mg & 1.0mg
13SHD001
(Dap22)-ShK
0.01mg, 5 x 0.01mg & 0.1mg
13ADW001
ADWX-1
0.1mg, 0.5mg & 1.0mg
 
* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
 
 
* 관련 제품
 
Iberiotoxin (IbTx) / Charybdotoxin / Leiurotoxin 1 / Tamapin / Guangxitoxin 1E / ShK (Stichodactyla toxin)
 
Margatoxin / HsTx1 / Apamin / TERTIAPIN-Q / Maurotoxin / Kaliotoxin-1   
 
 
▣ 관련 페이지 ; Smartox Biotechnology
 
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• 화학 합성의 각종 Calcium Channel Blocker Peptide Toxin
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  conotoxin MVIIA )
 
• 화학 합성의 각종 Potassium Channel Blocker Peptide Toxin
  Agitoxin-2 / (Dap22)-ShK / ADWX-1
  Iberiotoxin (IbTx) / Charybdotoxin / Leiurotoxin 1 / Tamapin / Guangxitoxin 1E / ShK (Stichodactyla toxin)/
  Margatoxin / HsTx1 / Apamin / TERTIAPIN-Q / Maurotoxin / Kaliotoxin-1
 
• 화학 합성의 각종 Sodium Channel Blocker Peptide Toxin
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  Protoxin II (ProTx II) / Huwentoxin IV / Huwentoxin I / μ Conotoxin PIIIA  (mu conotoxin PIIIA)