Kinesore is a cell penetrant and potent activator of kinesin-1 that induces kinesin light chain tetratricopeptide repeat domain-dependent kinesin-1 activation in the absence of organelle cargo-adaptor engagement. It inhibits kinesin-1 interaction with peptide fragment of organelle-specific cargo adaptors. Kinesore induces kinesin light chain conformational switch that causes remodeling of the microtubule network in cells.