BeKm 1

Product Name:BeKm 1

CAS No:524962-01-4

Purity:95%

Molar Mass:4091.65

Chemical Formula:C174H261N51O52S6

Storage:Store at -20 degrees Celsius

Sequence:RPTDIKCSESYQCFPVCKSRFGKTNGRCVNGFCDCF

Target:HERG

Application:

BeKm-1 is a peptide toxin derived from the venom of the scorpion Buthus eupeus. It is a potent and selective blocker of the hERG (human ether-??-go-go-related gene) potassium channels, which play a crucial role in regulating the electrical activity of the heart. By inhibiting hERG channels, BeKm-1 can prolong the action potential duration in cardiac cells, which makes it a valuable tool for studying cardiac electrophysiology and for researching conditions like long QT syndrome, where abnormal hERG channel activity leads to arrhythmias. This peptide is also used in drug development to evaluate the potential cardiotoxicity of new compounds.

Current Research:

BeKm-1 is a peptide toxin derived from the venom of the Central Asian scorpion Buthus eupeus. It functions as a selective inhibitor of the human ether-??-go-go-related gene (hERG) potassium channels, which are crucial for cardiac electrical activity.
Structural Characteristics
BeKm-1 is a 36-amino-acid peptide with a molecular weight of approximately 4 kDa. Its structure includes six cysteine residues forming three disulfide bridges, contributing to its stability. The peptide comprises an alpha-helix and three beta-strands arranged in a twisted antiparallel beta-sheet. This configuration is characteristic of scorpion venom potassium channel blockers.
Mechanism of Action
BeKm-1 selectively inhibits hERG potassium channels by binding to their outer vestibule. This interaction suppresses potassium ion currents, leading to prolonged cardiac action potentials. The inhibition occurs with an IC?? of approximately 3.3 nM, indicating high potency.
Physiological Implications
Inhibition of hERG channels by BeKm-1 can prolong the QT interval on an electrocardiogram, a condition associated with an increased risk of arrhythmias. This effect underscores the importance of hERG channels in maintaining normal cardiac rhythm.
Research Applications
BeKm-1 is utilized in electrophysiological studies to investigate hERG channel function and to screen for potential cardiotoxicity of new drugs. Its specificity makes it a valuable tool for understanding cardiac electrophysiology and for developing safer pharmaceuticals.
Conclusion
As a potent and selective hERG channel inhibitor, BeKm-1 provides significant insights into cardiac ion channel physiology and aids in the assessment of drug-induced cardiac risks.

Reference:

Yi, H., Cao, Z., Yin, S., Dai, C., Wu, Y., & Li, W. (2007). Interaction simulation of hERG K+ channel with its specific BeKm-1 peptide: insights into the selectivity of molecular recognition. Journal of proteome research, 6(2), 611-620.