Potent and selective KV11.1 (hERG) channel blocker. Selective for KV11.1 over a panel of 14 other potassium channels. Dose-dependently prolongs QTc interval in isolated rabbit heart.
CAT No: R1045
CAS No:524962-01-4
Synonyms/Alias:524962-01-4;L-Phenylalanine,L-arginyl-L-prolyl-L-threonyl-L-a-aspartyl-L-isoleucyl-L-lysyl-L-cysteinyl-L-seryl-L-a-glutamyl-L-seryl-L-tyrosyl-L-glutaminyl-L-cysteinyl-L-phenylalanyl-L-prolyl-L-valyl-L-cysteinyl-L-lysyl-L-seryl-L-arginyl-L-phenylalanylglycyl-L-lysyl-L-threonyl-L-asparaginylglycyl-L-arginyl-L-cysteinyl-L-valyl-L-asparaginylgl;BeKm 1;BeKm1;BeKm-1;ZVA96201;AKOS027470315;DA-61566;PD080272;
BeKm 1 is a peptide toxin originally isolated from the venom of the scorpion *Buthus eupeus*, and it is recognized for its highly selective inhibitory activity against specific potassium ion channels, particularly the hERG (human Ether-à-go-go-Related Gene) channel. As a member of the scorpion toxin family, BeKm 1 is structurally characterized by a compact, disulfide-rich framework that imparts exceptional stability and target specificity. Its unique pharmacological properties have made it a valuable molecular tool in ion channel research, where it enables the precise interrogation of channel function, gating mechanisms, and toxin-channel interactions. The peptide's selectivity and mechanism of action have positioned it as an indispensable resource for advancing the understanding of potassium channel physiology and pharmacology.
Ion channel research: BeKm 1 is extensively utilized as a molecular probe in the study of voltage-gated potassium channels, with particular emphasis on the hERG subtype. Its high affinity and specificity allow researchers to dissect the functional roles of these channels in excitable cells, elucidate gating kinetics, and investigate the molecular determinants underlying channel modulation. By providing a means to selectively block hERG channels, the peptide supports studies aimed at understanding cardiac electrophysiology, neuronal signaling, and the broader implications of potassium channel activity in health and disease models.
Electrophysiological assay development: The selective inhibitory action of this peptide toxin makes it an essential reagent for patch-clamp electrophysiology and related bioassays. It is frequently employed to validate hERG channel expression in heterologous systems, characterize channel pharmacodynamics, and benchmark the effects of novel modulators. Its use enhances assay sensitivity and reproducibility, facilitating high-quality data acquisition for both academic research and pharmaceutical screening programs targeting ion channel modulators.
Structure-function analysis: BeKm 1 serves as a model ligand for probing the structural basis of toxin-channel interactions. By leveraging its known binding interface and mutational variants, researchers can map critical contact residues on both the peptide and the channel, enabling detailed structure-activity relationship (SAR) studies. These investigations contribute to the rational design of next-generation channel modulators and inform the engineering of peptide analogues with tailored selectivity profiles.
Peptide engineering and synthetic biology: The well-defined structure and potent bioactivity of this scorpion-derived peptide make it a valuable template for peptide engineering efforts. It is frequently used as a scaffold for the development of novel bioactive peptides, either through site-directed mutagenesis or chemical modification, to generate analogues with enhanced stability, altered selectivity, or improved pharmacokinetic properties. Such engineered peptides are of significant interest in both basic research and the development of advanced molecular tools for ion channel modulation.
Toxin-based biosensor development: The high specificity of BeKm 1 for particular potassium channels underpins its utility in the design of biosensors and diagnostic platforms. By immobilizing or functionalizing surfaces with the peptide, researchers can create sensitive detection systems for monitoring channel activity, screening for channelopathies, or evaluating the effects of environmental toxins and pharmacological agents. These biosensors benefit from the robust and selective binding properties of the peptide, enabling precise and reliable measurements in diverse research and analytical contexts.
The toxin BeKm-1 isolated from scorpion Buthus eupeus is singled out of other characterized α-KTxs by selectively inhibiting HERG channels, which are voltage-gated K+ channels, coded by the humanether-a-go-go-related gene. The interest in the HERG channels has increased due to the important role these channels play in different tissues, mainly in shaping the action potential in the heart). The HERG channels specify one component of the delayed rectifier that contributes to the repolarization phase of cardiac action potential. One form of inherited long QT syndrome, LQT2, results from genetic defects in herg1 gene and predisposes affected individuals to potentially lethal arrhythmias. However most often the same sickness is derived from the nonspecific blockade of cardiac HERG current by various commonly used medications, such as class III antiarrhythmics, antihistaminics, or antipsychotics. This undesirable side effect is a major hurdle in the development of new and safe drugs, which may be overcome by the resolution of HERG channel pore structure.
New Binding Site on Common Molecular Scaffold Provides HERG Channel Specificity of Scorpion Toxin BeKm-1*210
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