화학합성의 Potasisum Channel Blocker Peptide Toxin(1)
본문
화학합성의 각종 Potassium Channel Blocker Peptide Toxin (1)
Potassium channel 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
Iberiotoxin (IbTx)
Iberiotoxin (IbTx) is a toxin that was originally isolated from Buthus tamulus scorpion venom. Iberiotoxin inhibits
selectively the high conductance Ca2+-activated K+ channel (KCa1.1). This toxin does not affect other types of voltage-
dependent K+ channels which are sensitive to the Charybdotoxin. Iberiotoxin is a valuable tool to study specifically Maxi-K
channels.
Details
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AA sequence: |
|
pGlu-Phe-Thr-AspVal-Asp-Cys-Ser-Val-Ser-Lys-GIu-Cys-Trp-Ser-Val-Cys-Lys-Asp-Leu-Phe-Gly-Val-Asp-Arg-Gly-Lys-Cys-Met-Gly-Lys-Lys-Cys-Arg-Cys-Tyr-GIn-OH |
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Disulfide bridges: |
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Cys7-Cys28, Cys13-Cys33, Cys17-Cys35 |
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Length (aa): |
|
37 |
|
Formula: |
|
C179H274N50O55S7 |
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Molecular Weight: |
|
4230.8 Da |
|
Appearance: |
|
White lyophilized solid |
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Solubility: |
|
Water and saline buffer |
|
CAS number: |
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129203-60-7 |
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Source: |
|
Synthetic |
|
Purity rate: |
|
> 95 % |
References
1. Galvez A, et al. Purification and characterization of a unique, potent, peptidyl probe for the high conductance calcium-
activated potassium channel from venom of the scorpion Buthus tamulus. J Biol Chem.
2. Giangiacomo KM, et al. Mechanism of iberiotoxin block of the large-conductance calcium-activated potassium channel
from bovine aortic smooth muscle. Biochemistry.
3. Kaczorowski GJ, et al. High-conductance calcium-activated potassium channels; structure, pharmacology, and function.
J Bioenerg Biomembr.
4. Garcia ML, et al. Use of toxins to study potassium channels. J Bioenerg Biomembr.
5. Candia S., et al. Mode of action of iberiotoxin, a potent blocker of the large conductance Ca(2+)-activated K+
channel. Biophys J.
Charybdotoxin
Charybdotoxin is a 37 amino acid peptide isolated from the venom of the scorpion Leiurus quinquestriatus hebraeus that
blocks voltage gated and Ca2+ activated K+ channels. This blockade causes hyperexcitability of the nervous system.
The toxin reversibly blocks channel activity by interacting at the external pore of the channel protein with an apparent
Kd of 2.1 nM. ChTX also blocks Kv1.2 (Kd 14 nM) and Kv1.3 (Kd 2.6nM) channels.
Details
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AA sequence: |
|
H-Pyr-Phe-Thr-Asn-Val-Ser-Cys7-Thr-Thr-Ser-Lys-Glu-Cys13-Trp-Ser-Val-Cys17-Gln-Arg-Leu-
His-Asn-Thr-Ser-Arg-Gly-Lys-Cys28-Met-Asn-Lys-Lys-Cys33-Arg-Cys35-Tyr-Ser-OH |
|
|
|
(Disulfide bonds between Cys7-Cys28, Cys13-Cys33, and Cys17-Cys35) |
|
Length (aa): |
|
37 |
|
Formula: |
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C176H277N57O55S7 |
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Molecular Weight: |
|
4295.90 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Water and saline buffer |
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CAS number: |
|
95751-30-7 |
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Source: |
|
Synthetic |
|
Purity |
|
> 97% |
References
1. Gimenez-Gallego G., et al. (1988) Purification, sequence, and model structure of charybdotoxin, a potent selective
inhibitor of calcium-activated potassium channels. Proc. Natl. Acad. Sci. U.S.A. PubMed link
2. Goldstein SA, Miller C. (1993) Mechanism of charybdotoxin block of a voltage-gated K+ channel. Biophys J.
3. Goldstein SA, et al. (1994) The charybdotoxin receptor of a Shaker K+ channel: peptide and channel residues
mediating molecular recognition. Neuron. PubMed link
Leiurotoxin 1
Leiurotoxin 1 (scyllatoxin) is a neurotoxin that was originally isolated from Leiurus quinquestriatus hebraeus. Leuirotoxin
binds to the SK channels (small conductance Ca2+-activated K+ channels) in the brain and spinal cord and inhibits them.
Details
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AA sequence: |
|
H-Ala-Phe-Cys3-Asn-Leu-Arg-Met-Cys8-Gln-Leu-Ser-Cys12-Arg-Ser-Leu-Gly-Leu-Leu-Gly-Lys-
Cys21-Ile-Gly-Asp-Lys-Cys26-Glu-Cys28-Val-Lys-His-NH2 |
|
|
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(Disulfide bonds between Cys3-Cys21, Cys8-Cys26, and Cys12-Cys28) |
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Length (aa): |
|
31 |
|
Formula: |
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C142H237N47O39S7 |
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Molecular Weight: |
|
3421.1 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Water and saline buffer |
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CAS number: |
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116235-63-3 |
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Source: |
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Synthetic |
|
Purity rate: |
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> 95% |
References
1. Chicchi, G. G.,et al. (1988) Purification and characterization of a unique, potent inhibitor of apamin
binding from Leiurus quinquestriatus hebraeus venom, J Biol Chem.
2. Auguste, P., et al. (1990) Leiurotoxin I (scyllatoxin), a peptide ligand for Ca2(+)-activated K+ channels.
Chemical synthesis, radiolabeling, and receptor characterization, J Biol Chem.
3. Martins, J. C., et al. (1990) Solution conformation of leiurotoxin I (scyllatoxin) by 1H nuclear magnetic
resonance. Resonance assignment and secondary structure, FEBS Lett.
Tamapin
Tamapin is a peptide toxin isolated from the venom of the Indian red scorpion Mesobuthus Tamulus. Tamapin is amidated at its C-terminal tyrosine residue (contrary to recombinant tamapin, Smartox’ tamapin is amidated). It binds to small
conductance Ca2+-activated K+ channels (SK channels) with high affinity and inhibits SK channel-mediated currents in
pyramidal neurons of the hippocampus as well as in cell lines expressing distinct SK channel subunits. Tamapin is an
excellent toxin to discriminate among SK channel subtypes because it presents different affinities for SK1 (42 nM),
SK2 (24 pM) and SK3 (1.7 nM) channels. This toxin is also the most potent SK2 channel blocker characterized so far (IC50 for SK2 channels = 24 pM).
Details
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AA sequence: |
|
Ala-Phe-Cys3-Asn-Leu-Arg-Arg-Cys8-Glu-Leu-Ser-Cys12-Arg-Ser-Leu-Gly-Leu-Leu-Gly-Lys-
Cys21-Ile-Gly-Glu-Glu-Cys26-Lys-Cys28-Val-Pro-Tyr-NH2 |
|
|
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(Disulfide bridges: Cys3-Cys21, Cys8-Cys26, and Cys12-Cys28) |
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Length (aa): |
|
31 |
|
Formula: |
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C146H237N44O41S6 |
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Molecular Weight: |
|
3459.00 Da |
|
Appearance: |
|
White lyophilized solid |
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Solubility: |
|
Water and saline buffer |
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CAS number: |
|
Not available |
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Source: |
|
Synthetic |
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Purity rate: |
|
> 97 % |
References
1. Pedarzani P et al. (2002) Tamapin, a venom peptide from the Indian red scorpion (Mesobuthus tamulus) that targets
small conductance Ca2+-activated K+ channels and afterhyperpolarization currents in central neurons. J. Biol Chem.
Guangxitoxin 1E
GxTx-1E was isolated from the venom of Chilobrachys jingzhao (Chinese earth tiger tarantula). It was shown to block Kv2.1/KCNB1, Kv2.2/KCNB2 and Kv4.3/KCND3 channels without significant effect on Kv1.2/KCNA2, Kv1.3/KCNA3, Kv1.5/KCNA5, Kv3.2/KCNC2, Cav1.2/CACNA1C, Cav2.2/CACNA1B, Nav1.5/SCN5A, Nav1.7/SCN9A or Nav1.8/SCN10A channels.
GxTx-1E inhibits Kv2.1 with an IC50 value of 1 nM and Kv2.2 with an IC50 value of 3 nM. Block of Kv4.3 occurs at
10-20 fold higher concentrations. It acts as a gating modifier since it shifts the voltage-dependence of Kv2.1 K+ currents
towards depolarized potentials. In pancreatic b cells, it enhances glucose-stimulated insulin secretion by broadening the
cell action potential and enhancing calcium oscillations.
Therapeutic area
Diabetes type 2
Details
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AA sequence: |
|
H-Glu-Gly-Glu-Cys4-Gly-Gly-Phe-Trp-Trp-Lys-Cys11-Gly-Ser-Gly-Lys-Pro-Ala-Cys18-Cys19-Pro-
Lys-Tyr-Val-Cys24-Ser-Pro-Lys-Trp-Gly-Leu-Cys31-Asn-Phe-Pro-Met-Pro-OH |
|
|
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(Presumed disulfide bridge pattern-but unsolved Cys4-Cys19, Cys11-Cys24 and Cys18-Cys31) |
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Length (aa): |
|
36 |
|
Formula: |
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C178H249N44O45S7 |
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Molecular Weight: |
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3948.7 Da |
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Appearance: |
|
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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Not available |
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Source: |
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Synthetic |
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Purity rate: |
|
> 95 % |
References
1. Herrington J. (2009) Gating modifier peptides as probes of pancreatic beta-cell physiology. Toxicon.
2. Zhuang GQ, et al. (2009) SNAP-25(1-180) enhances insulin secretion by blocking Kv2.1 channels in rat
pancreatic islet beta-cells. Biochem Biophys Res Commun.
3. Herrington J, et al. (2006) Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-
dependent insulin secretion. Diabetes
ShK (Stichodactyla toxin)
ShK (Stichodactyla toxin) has been isolated from the venom of the Carribean sea anemone Stoichactis helianthus. This
toxin inhibits voltage-dependent potassium channels. It blocks Kv1.3 (KCNA3) potently and also Kv1.1 (KCNA1), Kv1.4
(KCNA4), and Kv1.6 (KCNA6) respectively with 11 pM,16 pM and 165 pM.
Details
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AA sequence: |
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H-Arg-Ser-Cys3-Ile-Asp-Thr-Ile-Pro-Lys-Ser-Arg-Cys12-Thr-Ala-Phe-Gln-Cys17-Lys-His-Ser-Met-Lys-Tyr-Arg-Leu-Ser-Phe-Cys28-Arg-Lys-Thr-Cys32-Gly-Thr-Cys35-OH |
|
|
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(Disulfide bonds between Cys3-Cys35, Cys12-Cys28, and Cys17-Cys32) |
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Length (aa): |
|
35 |
|
Formula: |
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C169H274N54O48S7 |
|
Molecular Weight: |
|
4054.85 Da |
|
Appearance: |
|
White lyophilized solid |
|
Solubility: |
|
Water and saline buffer |
|
CAS number: |
|
165168-50-3 |
|
Source: |
|
Synthetic |
|
Purity rate: |
|
> 97 % |
References
1. Tudor, J. E., et al. (1996) Solution structure of ShK toxin, a novel potassium channel inhibitor from a sea
anemone, Nat Struct Biol.
2. Pennington, M. W., et al. (1995) Chemical synthesis and characterization of ShK toxin: a potent
potassium channel inhibitor from a sea anemone, Int J Pept Protein Res.
3. Castaneda, O., et al. (1995) Characterization of a potassium channel toxin from the Caribbean Sea anemone
Stichodactyla helianthus, Toxicon.
Ordering information
|
Catalog No. |
Product Name |
Size |
|
12IBX001 |
Iberiotoxin |
0.1mg, 0.5mg
& 1.0mg |
|
11CHA001 |
Charybdotoxin |
0.05mg, 0.1mg,
0.5mg & 1.0mg |
|
10LEI001 |
Leiurotoxin 1 |
0.1mg, 0.5mg
& 1.0mg |
|
10TAM001 |
Tamapin |
0.1mg, 0.5mg
& 1.0mg |
|
11GUA002 |
Guangxitoxin 1E |
0.05mg, 5 x 0.05mg,
0.1mg & 0.5mg |
|
08SHK001 |
ShK |
0.1mg
& 0.5mg |
* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
* 관련 제품
Margatoxin / HsTx1 / Apamin / TERTIAPIN-Q / Maurotoxin / Kaliotoxin-1
▣ 관련 페이지 ; Smartox Biotechnology
• 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
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
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
- 이전글화학합성의 Potassium Channel Blocker Peptide Toxin(2) 13.05.16
- 다음글화학합성의 Sodium Channel Blocker Peptide Toxin(2) 13.05.10
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