LSD1/HDAC-IN-2 (Compound 20c) acts as an inhibitor targeting both LSD1 and several HDACs, specifically HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50 values of 39.0, 1.4, 1.0, 1.3, 2.9, and 16.0 nM, respectively. This compound effectively inhibits the proliferation of cancer cells, notably colorectal cancer cells. LSD1/HDAC-IN-2 induces cell cycle arrest at the G2/M phase, inhibits cell migration, and triggers apoptosis in HCT-116 and HT-29 cells. Additionally, it demonstrates antitumor activity in mouse models without causing significant toxicity at a dose of 20 mg/kg.

KDM1/LSD1:39.0 nM, HDAC2:1.0 nM, HDAC1:1.4 nM, HDAC6:2.9 nM, HDAC8:16.0 nM, HDAC3:1.3 nM