화학합성의 Potassium Channel Blocker Peptide Toxin(3)
본문
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
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AA sequence: |
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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 |
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|
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Cys8-Cys28, Cys14-Cys33 and Cys18-Cys35 |
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Length (aa): |
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38 |
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Formula: |
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C169H278N54O48S8 |
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Molecular Weight: |
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4090.89 Da |
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Appearance: |
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White lyophilized solid |
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Solubility: |
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Water and saline buffer |
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Source: |
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Synthetic |
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Purity rate: |
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> 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
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AA sequence: |
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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 |
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Cys3-Cys35, Cys12-Cys28 and Cys17-Cys32 |
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Length (aa): |
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35 |
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Formula: |
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C166H268N57O48S7 |
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Molecular Weight: |
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4012.8 Da |
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Appearance: |
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White lyophilized solid |
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Solubility: |
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Water and saline buffer |
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CAS number: |
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220384-25-8 |
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Source: |
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Synthetic |
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Purity rate: |
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>97% |
References
1. Robbins JR., et al. (2005) Hypoxia modulates early events in T cell receptor-mediated activation in human T
2. Norton RS., et al. (2004) Potassium channel blockade by the sea anemone toxin ShK for the treatment of multiple
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
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
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AA sequence: |
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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 |
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(Disulfide bonds between Cys7-Cys27, Cys13-Cys32 and Cys17-Cys34) |
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Length (aa): |
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37 |
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Formula: |
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C169H281N57O46S7 |
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Molecular Weight: |
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4071.90 Da |
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Appearance: |
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White lyophilized solid |
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Solubility: |
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Water and saline buffer |
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Source: |
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Synthetic |
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Purity rate: |
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>98 |
References
1. Song Han , et al. (2008) Structural Basis of a Potent Peptide Inhibitor Designed for Kv1.3 Channel, a Therapeutic
2. Zhi Li, et al.(2012) Selective Inhibition of CCR7− Effector Memory T Cell Activation by a Novel Peptide Targeting
3. Yin SJ (2008) Different residues in channel turret determining the selectivity of ADWX-1 inhibitor peptide between
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
• 기타 각종 생리활성 Peptide
Morphiceptin / Lys-conopressin G / GsMTx4 / Obtustatin
• 화학 합성의 각종 Purinergic Receptor Blocker Peptide Toxin
Purotoxin 1
• 화학 합성의 각종 Acetylcholine Receptor Blocker Peptide Toxin
Waglerin 1 / α-Conotoxin MI / α-Conotoxin GI / α-Conotoxin IMI
• 화학 합성의 각종 TRP Channel Blocker Peptide Toxin
GsMTx4 / Vanillotoxin 3 (VaTx3)
• 화학 합성의 각종 ASIC Channel Blocker Peptide Toxin
Psalmotoxin-1 (PcTx1, Pi-theraphotoxin-Pc1a) / APETx2
• 화학 합성의 각종 Chloride Channel Blocker Peptide Toxin
GaTx1 / GaTx2 / Chlorotoxin
• 화학 합성의 각종 Calcium Channel Blocker Peptide Toxin
ω-agatoxin IVA / ω-CONOTOXIN GVIA(Omega conotoxin GVIA) / ω-Conotoxin MVIIC(Omega conotoxin MVIIC) /
SNX482 / Maurocalcine/Huwentoxin I/ω CONOTOXIN SO-3(Omega contoxin SO-3)/ω-Conotoxin MVIIA(Omega
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
Paurtx 3 /
Protoxin I (ProTx-1) / GsAF-I / GsAF-II / Jingzhaotoxin III / Biotinyl-Protoxin II (ProTx II) / Hainantoxin-IV /
Protoxin II (ProTx II) / Huwentoxin IV / Huwentoxin I / μ Conotoxin PIIIA (mu conotoxin PIIIA)
- 이전글각종 Acetylcholine Receptor Blocker Peptide Toxin(2) 13.10.15
- 다음글화학합성의 Sodium Channel Blocker Peptide Toxin(3) 13.08.12
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