SK2 Inhibitors

Chemical inhibitors of SK2 play diverse roles in inhibiting the function of this small conductance calcium-activated potassium channel. Apamin, a well-documented SK2 inhibitor, binds directly to the channels, effectively reducing their ability to conduct potassium ions, which is a critical function for the proper operation of these channels. Similarly, UCL 1684 engages with SK2 channels and diminishes their potassium ion conductance, directly inhibiting their physiological function. Both NS8593 hydrochloride and its non-hydrochloride form, NS8593, perturb the gating mechanism of SK2 channels, which is integral to their operation, resulting in a decreased flow of potassium ions through the channel.

Lei-Dab7 attaches to SK2 channels and modifies their gating properties. This interaction decreases the probability of the channels being in an open state, thereby reducing potassium ion conductance. Dequalinium chloride and BML-258 employ a similar inhibition strategy by binding directly to SK2 channels and obstructing the potassium ion flow. CyPPA, while also an inhibitor, achieves its effect by altering the channel's conformation, leading to a reduction in the channel's conductance of potassium ions. This alteration in channel conformation is a crucial aspect of SK2 channel inhibition. UCL 1848, for instance, targets SK2 channels with high specificity, binding to them and curtailing their ability to conduct potassium ions. This specific interaction is key to the inhibition process. Scyllatoxin exerts its inhibitory effect by obstructing the potassium ion passage through SK2 channels, directly hindering their functionality. Lastly, Candelalide A inhibits SK2 by altering the channel's structure upon binding. This change in structure is not merely a physical blockade but a functional alteration that results in reduced potassium ion conductance through the channel. Each of these chemicals interacts with the SK2 protein in a way that impedes its normal function, reducing its activity and therefore its contribution to the potassium ion conductance they are responsible for.