Smartox Biotechnology
 
작성일 : 13-12-05
[Smartox Biotechnology] 화학합성의 Potassium Channel Blocker Peptide Toxin(4)
Kaliotoxin-1 / Charybdotoxin / BeKm-1
 
화학합성의 각종 Potassium Channel Blocker Peptide Toxin (4)
 
Potassium channel 연구에 유용한 유독 생물 유래의 합성 peptide toxin 입니다. 화학합성 peptide이기 때문에
endotoxin 오염의 걱정이 없습니다.
 
 
Kaliotoxin-1
 
Kaliotoxin-1 (KTX1) has been isolated from the venom of the Scorpion Androctonus mauretanicus mauretanicus.
Kaliotoxin-1 shows a high structural affinity with Iberiotoxin and Charybdotoxin that inhibit KCa2+ channels activity.
According to several studies, it appears that Kaliotoxin-1 has a weak inhibitory effect on KCa2+ channels, but it is a
potent and selective inhibitor of voltage-activated potassium channel (Kv1.1, Kv1.2, Kv1.3).
 
Details
AA sequence:
 
Gly-Val-Glu-Ile-Asn-Val-Lys-Cys8-Ser-Gly-Ser-Pro-Gln-Cys14-Leu-Lys-Pro-Cys18-Lys-Asp-Ala-Gly-Met-Arg-Phe-Gly-Lys-Cys28-Met-Asn-Arg-Lys-Cys33-His-Cys35-Thr-Pro-Lys-OH
 
 
(Disulfide bonds between Cys8-Cys28, Cys14-Cys33 and Cys18-Cys35)
Length (aa):
 
38
Formula:
C171H283N55O49S6
Molecular Weight:
 
4149.89 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
Source:
Synthetic
Purity rate:
 
> 97%
 
References
1. Ladjel-Mendil A., et al. (2013) Neuropathophysiological effect and immuno-inflammatory response induced by
   kaliotoxin of androctonus scorpion venom. Neuroimmunomodulation. PubMed link
2. Bessone R., et al. (2004) Heterogeneous competition of Kv1 channel toxins with kaliotoxin for binding in rat brain:
   autoradiographic analysis. Neurochem Int. PubMed link
3. Kourrich S., et al.  (2001) Kaliotoxin, a Kv1.1 and Kv1.3 channel blocker, improves associative learning in rats.
   Behav Brain Res. PubMed link
4. Beeton C., et al. (2001) Selective blocking of voltage-gated K+ channels improves experimental autoimmune
   encephalomyelitis and inhibits T cell activation. J Immunol. PubMed link   
5. Mourre C, et al. (1999) Distribution in rat brain of binding sites of kaliotoxin, a blocker of Kv1.1 and Kv1.3
   alpha-subunits. J Pharmacol Exp Ther. PubMed link
6. Gairí M, et al. 3D structure of kaliotoxin: is residue 34 a key for channel selectivity? J Pept Sci. PubMed link
7. Rader RK, et al. (1997) T cell activation is regulated by voltage-dependent and calcium-activated potassium channels.
   J Immunol. PubMed link
8. Gribkoff VK. 1996) Effects of channel modulators on cloned large-conductance calcium-activated potassium channels.
   Mol Pharmacol. PubMed link
9. Eder C. (1997) Pharmacological properties of Ca2+activated K+ currents of ramified murine brain macrophages.
   Naunyn Schmiedebergs Arch Pharmacol. PubMed link
10.Crest M., et al. (1992) Kaliotoxin, a novel peptidyl inhibitor of neuronal BK-type Ca(2+)-activated K+ channels
   characterized from Androctonus mauretanicus mauretanicus venom. JBC. PubMed link  
 
 
Charybdotoxin
 
Charybdotoxin (ChTx) is a 37 amino acid peptide isolated from the venom of the scorpion Leiurus quinquestriatus
hebraeus that blocks voltage-gated and large conductance Ca2+ activated K+ channels KCa1.1 in nanomolar
concentrations (IC50~ 3 nM). 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 KCa3.1 (IC50 5 nM), Kv1.2 (IC50 14 nM), Kv1.3 (IC50 2.6 nM) and Kv1.6 (IC50 2 nM) channels.
 
Details
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:
C176H277N57O55S7
Molecular Weight:
 
4295.9 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
CAS number:
95751-30-7
Source:
 
Synthetic
Purity rate:
 
>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. PubMed link
3. Goldstein SA, et al. (1994) The charybdotoxin receptor of a Shaker K+ channel: peptide and channel residues
   mediating molecular recognition. Neuron. PubMed link
 
 
BeKm-1
 
BeKm-1 toxin is a peptide toxin that has been isolated from the venom of the Central Asian scorpion Buthus eupeus.
BeKm-1 toxin has been reported to be a highly selective inhibitor of the human ether-a-go-go ERG1 channel (hERG1).
BeKm-1 inhibits hERG1 channels expressed in HEK-293 cells with an IC50 of 3.3 nM, but has no effect at 100 nM on
human EAG, human SK1, rat SK2, human IK, human BK, KCNQ1/KCNE1, KCNQ2/KCNQ3, and KCNQ4 channels. It has also minimal effects on rat ELK1 channel. BeKm-1 inhibits the human ERG1 + KCNE1 combination transiently expressed in HEK-293 cells with an IC50 value in the range of 10 to 30 nM. BeKm-1 toxin preferentially blocks human ERG channel through the closed (resting) state, although some open channel blockade is also reported to occur.
 
Details
AA sequence:
 
Arg-Pro-Thr-Asp-Ile-Lys-Cys7-Ser-Glu-Ser-Tyr-Gln-Cys13-Phe-Pro-Val-Cys17-Lys-Ser-Arg-Phe-
Gly-Lys-Thr-Asn-Gly-Arg-Cys28-Val-Asn-Gly-Phe-Cys33-Asp-Cys35-Phe-OH
 
 
(Disulfide bonds between Cys7-Cys28, Cys13-Cys33 and Cys17-Cys35)
Length (aa):
 
36
Formula:
C174H261N51O52S6
Molecular Weight:
 
4091.7 Da
Appearance:
 
White lyophilized solid
Solubility:
 
Water and saline buffer
Source:
Synthetic
Purity rate:
 
>97
 
References
1. Milnes J., et al. (2003) Preferential closed channel blockade of HERG potassium currents by chemically synthesised
   BeKm-1 scorpion toxin. FEBS Letters. PubMed link
2. Korolkova Y., et al. (2002) New Binding Site on Common Molecular Scaffold Provides HERG Channel Specificity of
   Scorpion Toxin BeKm-1. JBC. PubMed link
3. Korolkova Y., et al. (2001) An ERG Channel Inhibitor from the Scorpion Buthus eupeus. JBC. PubMed link
 
 
Ordering informations
 
Catalog No.
Product Name
Size
08KTX002
Kaliotoxin-1
0.1mg, 0.5mg & 1.0mg
11CHA001
Charybdotoxin
0.05mg, 0.1mg, 0.5mg & 1mg
13BEK001
BeKm-1
0.1mg & 0.5mg
 
* 다른 사이즈나 bulk 공급도 가능하오니 별도로 문의하여 주십시오.
 
 
Iberiotoxin (IbTx) / Charybdotoxin / Leiurotoxin 1 / Tamapin / Guangxitoxin 1E / ShK (Stichodactyla toxin)
Margatoxin / HsTx1 / Apamin / TERTIAPIN-Q / Maurotoxin / Kaliotoxin-1   
Agitoxin-2 / (Dap22)-ShK / ADWX-1
 
 
▣ 관련 페이지 ; Smartox Biotechnology
 
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