HDAC1/MAO-B-IN-1 has the potential to be used in the Alzheimer’s disease research. HDAC1/MAO-B-IN-1 is a potent and selective inhibitor of HDAC1/MAO-B that can cross the blood-brain barrier. The IC50 values of HDAC1/MAO-B-IN-1 for HDAC1 and MAO-B are 21.4 nM and 99.0 nM, respectively [1].

HDAC1/MAO-B-IN-1 (compound 1f) inhibits hMAO-B, hMAO-A, and hHDAC1 with IC50 values of 99.0 nM, 9923.0 nM, and 21.4 nM, respectively [1]. At 50 μM over 24 hours, it shows neuroprotective effects and reduces reactive oxygen species (ROS) production in PC12 cells, as confirmed by a Cell Viability Assay [1].

Administered intragastrically (i.g.) at 20 mg/kg, HDAC1/MAO-B-IN-1 demonstrates favorable permeability across the blood-brain barrier (BBB) [1]. When administered intraperitoneally (i.p.) at 15 mg/kg for 15 consecutive days, it enhances the learning and memory functionalities in ICR mice, both male (6-8 weeks old) and female (20-25 g) models [1].