ION Biosciences’ HEK293 KV11.1 (hERG) recombinant cell line stably expresses human KCNH2 and provides a robust, well-validated model for investigating KV11.1 channel function. This cell line is ideally suited for high-throughput screening of channel modulators, safety pharmacology assays, and mechanistic studies aimed at discovering novel inhibitors or activators of KV11.1. With excellent reproducibility and functional expression, these cells facilitate efficient evaluation of compound effects on KV11.1 currents using fluorescence-based assays.
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Size: 2 x 10^6M cells
Cells/vial: 2 x 10^6
Mycoplasma test: Pass
Species: Human
Guaranteed performance: > 10 passages
ION Biosciences’ HEK293 KV11.1 (hERG) recombinant cell line stably expresses human KCNH2 and provides a robust, well-validated model for investigating KV11.1 channel function. This cell line is ideally suited for high-throughput screening of channel modulators, safety pharmacology assays, and mechanistic studies aimed at discovering novel inhibitors or activators of KV11.1. With excellent reproducibility and functional expression, these cells facilitate efficient evaluation of compound effects on KV11.1 currents using fluorescence-based assays.
Voltage-gated potassium (KV) channels are integral membrane proteins that enable selective potassium ion permeation in response to changes in cellular membrane potential. These channels play critical roles in shaping action potentials, regulating cellular excitability, and maintaining ion homeostasis across diverse tissues. The human genome encodes 40 KV channels, categorized into 12 subfamilies (KV1–KV12), each exhibiting unique biophysical properties and tissue distribution.
KV11.1, also known as hERG (human Ether-à-go-go Related Gene), is a key member of the KV channel family encoded by the KCNH2 gene. This channel is predominantly expressed in cardiac myocytes and the central nervous system, where it is essential for repolarizing the cardiac action potential and regulating neuronal excitability. Dysfunction or pharmacological inhibition of KV11.1 channels leads to delayed cardiac repolarization, manifesting as drug-induced long QT syndrome—a potentially fatal arrhythmia of major concern in drug development. Because of this, regulatory agencies including the FDA mandate routine screening of new drug candidates for KV11.1 inhibition. Beyond cardiac physiology, KV11.1 channels have emerging roles in neurological disorders, tumor proliferation, and cellular migration, making them a valuable target for a broad range of therapeutic applications.
The biological function of the HEK293 Kv11.1 (hERG) recombinant cell line was validated using terfenadine, a well-characterized tool compound known to inhibit hERG function. Functional activity of hERG channels was measured using ION Biosciences’ Brilliant Thallium Gold Assay, Brilliant Thallium Gold Snapshot Assay, and Thallium-Free hERG Potassium Channel Assay kits. These kits use fluorescent ion indicators to detect the flow of thallium or potassium ions through the channel. HEK293 KV11.1 (hERG) recombinant cells were pre-incubated with the fluorescent ion indicators’ optimized loading conditions, followed by exposure to increasing concentrations of terfenadine. A dose-dependent change in fluorescence was observed upon addition of a membrane-depolarizing stimulus solution, reflecting inhibition of KV11.1-mediated ion flux. Fluorescence was recorded continuously following compound addition, and the resulting data were analyzed to determine IC50 values based on maximum velocity (Vmax) or area under the curve (AUC). The assay produced an IC50 consistent with literature values for terfenadine, confirming functional expression and pharmacological responsiveness of KV11.1 channels in the HEK293 cell line.
