- Strøbæk, D. et al. (2013) Br. J. Pharmacol. 168, 432.
- Alomone Labs NS-6180 blocks KCa3.1 currents expressed in HEK 293T cells.A. Time course of KCa3.1 current amplitude without and with 100 nM NS-6180 (#N-230). Currents were elicited by application of voltage ramp from -120 mV to +60 mV (150 msec), delivered every 10 seconds, holding potential of -80 mV. B. Superimposed example traces of current responses before and during perfusion of 100 nM NS-6180 as indicated.
The benzothiazinone NS-6180 is a potent and selective KCa3.1 channel blocker1.
The Ca2+-activated K+ channel, KCa3.1, plays a major role in the controlled expression of essential genes orchestrating proliferation, migration and cytokine production by participating in the regulation of calcium entry. A highly regulated and sustained increase in cytosolic Ca2+ is critical in these processes thus, the KCa3.1 channel is a potential target for therapy of immune disease1.
Inhibition of KCa3.1 channel by NS-6180 demonstrates IC50 value of 14 nM in human, 9 nM in rat and 15 nM in mouse. NS6180 also has the ability to inhibit KCa1.1, KV1.3 and KV11.1 channels with IC50s above 10 µM2.
NS-6180 (#N-230) is a highly pure, synthetic, and biologically active compound.