Ebio3

Ebio3 (10 pM-10 μM) inhibits potassium currents in a dose-dependent manner in CHO-K1 cells overexpressing human KCNQ2 (IC₅₀ = 1.2 nM) and produces a non-blocking inactivation phenotype^[4].
Ebio3 (10 μM) alters the gating of Kv7.2 L307A/L307V mutant channels and does not affect cardiac Kv7.1 channels^[2].
Ebio3 binds to the S6_I/S5_II/S6_II pocket of the Kv7.2 pore domain, contacts L299, I300, F304, L307, V225, W236, F240, F305, and L312, and forms hydrogen bonds with S303 and W236^[2].
Ebio3 (100 nM) is a selective KCNQ2 inhibitor in CHO-K1/HEK293T/stable cell line electrophysiology, with approximately 10-fold selectivity for KCNQ3/4/5, and shows no significant activity against the tested non-KCNQ channels at 100 nM^[4].
Ebio3 (10 nM) potently inhibits and rescues excessive outward currents in CHO-K1 cells expressing KCNQ2 pathogenic gain-of-function mutants (R75C, I238L, R144Q, R198Q, R201C, N79K, V175L, G239S), reducing outward currents by at least 60%-80%^[4].