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HDAC1/6-IN-1 is a potent multi-target inhibitor of GLP (IC50: 1.3 nM), HDAC6 (IC50: 13 nM) and HDAC1 (IC50: 89 nM). HDAC1/6-IN-1 inhibits the methylation and deacetylation of H3K9 at the protein level. HDAC1/6-IN-1 can block the cell cycle of cancer cells in G0/G1 phase, induce apoptosis and prevent cancer cell migration and invasion.