The small molecule inhibitor Rg5 effectively blocks NFKB2 binding with STAT2, resulting in decreased PD‐L1 transcription and increased immune surveillance, as evidenced by the enhanced proportion of CD8+ T cells in the tumor microenvironment and improved response to PD‐1 blockade immunotherapy in CRC‐bearing mice. This evidence concerns the gene CD274 and colorectal carcinoma.