MLN4924

MLN4924 inhibits cullin neddylation by directly targeting the NEDD8-activating enzyme that is essential for the activity of cullin-RING ligase (CRL) (Nawrocki et al.). The components of CRL are frequently up-regulated in human cancers (Zhao & Sun), and MLN4924 was reported to suppress the growth of human tumor xenografts in mice (Soucy et al.).


GENOME EDITING
· In combination with other small molecules (“CRISPY” mix), MLN4924 has been reported to increase precise CRISPR-Cas9 genome editing in human pluripotent stem cells (Riesenberg & Maricic).

CANCER RESEARCH
· By blocking NAE and proteasome, MLN4924 together with bortezomib inhibits AKT and mTOR and induces apoptosis in multiple myeloma cell lines (Gu et al.).