Overview
- Waschk, D.E. et al. (2011) Am. J. Physiol. Cell. Physiol. 300, C843.
Alomone Labs 1-EBIO activates KCa3.1 currents expressed in HEK 293T cells.A. Time course of KCa3.1 current amplitude and its activation by 50 µM 1-EBIO (#E-150). Currents were elicited by application of voltage ramp from -120 mV to +60 mV (150 msec), delivered every 10 seconds, holding potential of -80mV. B. Superimposed example traces of current responses before and during perfusion of 50 µM 1-EBIO as indicated.
1-EBIO is a potent KCa2/3 channel activator that activates the channels by increasing the Ca2+ sensitivity by stabilizing the interaction between calmodulin and the channels1,2, thus shifting the activation curve of the channels to the left. 1-EBIO activates KCa3.1 with an EC50 value of around 30 μM and all three KCa2 channels with EC50 value around 300 μM2.
The Ca2+-activated K+ channel, KCa3.1, plays a major role in the controlled expression of essential genes that are responsible for several physiological processes including- membrane potential, cell volume proliferation, migration and production of inflammatory mediators by participating in the regulation of calcium entry. A highly regulated and sustained increase in cytosolic Ca2+ is critical in these processes making KCa3.1 a potential target for therapy of several disease1,3.
