I-BET-151 is a BET bromodomain (BRD) inhibitor that inhibits BRD2, BRD3, and BRD4. I-BET-151 exhibits anticancer chemotherapeutic and anti-inflammatory activities. In vitro and in vivo, this compound induces apoptosis and inhibits cellular proliferation in various cancer models. I-BET-151 inhibits recruitment of the P-TEFb component of cyclin-dependent kinase 9 (CDK9) to chromatin, causing transcriptional regression of Myc. I-BET-151 also inhibits bacteria-induced inflammation and sepsis in animal models.