N-Hydroxyapiosporamide was first isolated from Cytospora sp. associated with an ant colony by Clardy and coworkers, Cornell University, USA in 1996. N-Hydroxyapiosporamide is a pyridone with moderate activity against cholesteryl ester transfer protein (CTEP) implicated in atherosclerosis. N-Hydroxyapiosporamide shows significant cytotoxicy against a range of tumor cell lines, binding to the nuclear receptor RORγ in a small cell lung cancer model. More recently, N-hydroxyapiosporamide was shown to inhibit the NF-κB signaling pathway by blocking the interaction of the TAK1-TRAF6 complex in a colorectal cancer cell line.