Bromodomain-containing protein 4 (BRD4) is an epigenetic regulator that promotes transcription of oncogenic drivers such as MYC and contributes to tumor growth and therapy resistance in colorectal cancer, making it a promising therapeutic target. Researchers from Hangzhou Kexing Biochem Co. Ltd. described the discovery and preclinical characterization of compound [I], a potent BRD4 inhibitor.