LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC , that inhibits LSD1 , HDAC1 , HDAC2 , HDAC3 , HDAC6 , and HDAC8 , with IC 50 s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity.