NVP-2 is a potent and selective inhibitor of the NEDD8-activating enzyme (NAE), which plays a key role in the neddylation pathway. This pathway regulates the activity of cullin-RING ligases (CRLs), major E3 ubiquitin ligases involved in protein degradation. By inhibiting NAE, NVP-2 disrupts CRL function, leading to the accumulation of CRL substrate proteins that control cell cycle progression, DNA damage response, and apoptosis. Due to this mechanism, NVP-2 has been widely used in cancer research to study the effects of neddylation inhibition on tumor cell viability. It shows potent anti-proliferative activity in various cancer cell lines, particularly in hematological malignancies and solid tumors. NVP-2 induces cell cycle arrest and apoptosis, making it a valuable tool compound for validating the therapeutic potential of targeting the neddylation pathway. In preclinical studies, NVP-2 has demonstrated synergy with other anticancer agents, including DNA-damaging drugs and proteasome inhibitors, suggesting its potential use in combination therapies. Its application is primarily confined to laboratory research, where it helps elucidate the biological consequences of neddylation blockade and supports the development of related clinical candidates.