MAO-B-IN-33 (compound C3) is a potent, reversible and selective monoamine oxidase-B (MAO-B) inhibitor with an IC50 of 0.021 μM and 26.805 μM for MAO-B and MAO-A, respectively. The selectivity of MAO-B-IN-33 is attributed to the steric clash arising from the residue differences between Phe208 (MAO-A) and Ile199 (MAO-B). MAO-B-IN-33 inhibits cerebral MAO-B activity and alleviates MPTP (HY-15608)-induced dopaminergic neuronal loss in the mouse. MAO-B-IN-33 has the potential for Parkinson's disease research[1].
C3 is an inhibitor of monoamine oxidase B (MAO-B; IC50 = 0.021 μM).1 It is selective for MAO-B over MAO-A (IC50 = 26.8 μM). C3 (0.1, 1, and 3 mg/kg) prevents MPTP-induced decreases in brain dopamine levels in mice.
MAO-B: 0.021 μM (IC50); MAO-A: 26.805 μM (IC50)
1.Jin, C.-F., Wang, Z.-Z., Chen, K.-Z., et al.Computational fragment-based design facilitates discovery of potent and selective monoamine oxidase-B (MAO-B) inhibitorJ. Med. Chem.63(23)15021-15036(2020)