Potent and selective NEDD8-activating enzyme (NAE) inhibitor1. It disrupts cullin-RING ligase-mediated protein turnover leading to apoptosis in human tumor cells. Suppresses the growth of human tumor xenografts in mice2. Upregulates PD-L1 expression and enhances the efficacy of immune checkpoint blockade in glioblastoma3. Modulates tumor microenvironment4. Cell permeable.