α-NETA is a potent, irreversible and noncompetitive inhibitor of choline acetyltransferase (ChA) with an IC50 of 9 μM. It is also a potent antagonist of ALDH1A1, CMKLR1, and G9a histone methyltransferase with an IC50 of 0.04 µM, 0.38 µM, and 0.50 µM, respectively. It exhibits anti-cancer activity and may be beneficial in preventing or treating multiple sclerosis (MS).