HDAC8-IN-1 is an inhibitor of histone deacetylase 8 (HDAC8; IC50 = 27.2 nM). It is selective for HDAC8 over HDAC1-3, -4, -6, -10, and -11 (IC50s = ≥3,000 nM for all). HDAC8-IN-1 is cytotoxic to A549, H1299, and CL1-5 lung cancer cells (IC50s = 7.9, 7.2, and 7 μM, respectively).