Conjugated molecules(CMs) exhibit distinctive advantages of tunable optoelectronic properties,intrinsic bioactivities, and flexible assembly characteristics, providingvarious opportunities for the regulation of Ca2+ channels.In this Outlook, we introduce the CM-based external-light-reliableor -free photodynamic, the first/second near-infrared (NIR-I/II) light-enabledphotothermal, and supramolecular regulations of Ca2+ channelsfor modulating biological functions, including cancer and thrombolysistherapy, remote neurostimulation, and glycemic management. This evidence concerns the gene CA2 and cancer.