L-Canaline treatment inhibits the proliferation of PBMCs after stimulation by phorbol 12-myristate-13-acetate (PMA) or via the mixed lymphocyte reaction. The greatest effect is seen with PMA-stimulated cells, where L-canaline has an IC50 of 0.26 mM. L-Canaline is slightly less toxic to PBMCs stimulated via the mixed lymphocyte reaction (IC50 of 0.54 mM).
L-canaline inhibits L-lysine flux competitively (Ki of 4.6 mM) in astrocytes and astrocytoma cells.