ML-243 is an inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 2.0 μM) over a control (mammary epithelial) cell line (EC50 = 64 μM). It weakly antagonizes the adenosine A2A receptor (IC50 = 10 μM) and has no effect on 68 other targets commonly used in drug discovery for lead profiling.