ERGi-USU-6

ERGi-USU-6 is a potent small molecule inhibitor specifically designed to target ERG-positive prostate cancers. Approximately 50% of primary prostate tumors and 35% of metastatic castration-resistant prostate cancers harbor the oncogenic TMPRSS2-ERG gene fusion. ERGi-USU-6, particularly its salt derivative 7b, selectively inhibits the growth of ERG-positive tumor cells and organoids while sparing normal endothelial cells that express endogenous ERG. Its mechanism of action involves the downregulation of ERG and RIOK2 protein levels, leading to programmed cell death via ferroptosis, an iron-dependent pathway. The induction of the ATF3 gene is also implicated in its cancer-selective activity. The compound was developed through a collaboration involving the Uniformed Services University of the Health Sciences (USUHS), the Center for Prostate Disease Research (CPDR), and Oregon Health and Science University (OHSU).

Other names

ERGi-USU-6 salt derivativeERGi-USU6 salt derivativeERGi-USU 6 salt derivative