Figure 1

SP6616 is an inhibitor of Kv2.1 channel. (a) Chemical structure of SP6616. (b) CHO-Kv2.1 cells were incubated with 20 μM SP6616 or 100 nM ScTx-1 and membrane potential dye for 30 min, and then signal was recorded. These data were analyzed and shown as AUC. (c) Membrane potential assay in CHO cells was conducted as described in b. (d) Fifty percent inhibitive concentration (IC50, 2.58 μM) of SP6616 evaluated on the membrane potential assay. (e) Voltage-dependent outward K+ currents were recorded in CHO-Kv2.1 cells by whole-cell patch clamp from −80 mV to +120 mV. ScTx-1 (100 nM) effectively reduced K+ current amplitude. (f) SP6616 (10 μM) inhibited K+ current amplitude in the whole-cell patch clamp assay. (g) IC50 (6.44 μM) of SP6616 was evaluated on whole-cell patch clamp technique. All data were obtained from three independent experiments and shown as means±S.E.M. (*P<0.05, **P<0.01)