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Calmidazolium chloride is a calmodulin (CaMK) antagonist (Kd = 3 nM), antagonizing CaM-dependent phosphodiesterase(IC50 = 0.15 μM) and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase(IC50 = 0.35 μM). Calmidazolium chloride also induces apoptosis in certain cancer cell lines.