MLN4924
Nedd8 activating enzyme inhibitor / MLN4924 is a potent and selective NEDD8-activating enzyme (NAE) inhibitor.1 It disrupts cullin-RING ligase-mediated protein turnover leading to apoptosis in human tumor cells. Suppresses the growth of human tumor xenografts in mice.2 Upregulates PD-L1 expression and enhances the efficacy of immune checkpoint blockade in glioblastoma.3 Modulates tumor microenvironment.4 Blocks the neddylation of the DNA endonuclease CtIP, which promotes HDR in Cas9- and Cpf1-mediated gene editing. Part of the CRISPY mix for increasing precise gene editing.5 Cell permeable.
Biochemicals & reagents
905579-51-3
Pevonedistat
1) Soucy, et al. (2009), An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 458 732 2) Milhollen, et al. (2010) MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF-(kappa)B-dependent lymphoma. Blood, 116 1515 3) Zhou et al. (2019) Neddylation inhibition upregulates PD-L1 expression and enhances the efficacy of immune checkpoint blockade in glioblastoma; Int. J. Cancer, 145 763 4) Zhou et al. (2019) Neddylation: a novel modulator of the tumor microenvironment; Mol. Cancer 18 77 5) Riesenberg and Maricic (2018) Targeting repair pathways with small molecules increases precise genome editing in pluripotent stem cells; Nat. Commun. 9 2164
-20°C
TARGET: Neddylation -- PATHWAY: Apoptosis inducer -- RESEARCH AREA: CRISPR; Cell death; Neuroscience; Ubiquitin/Proteasome -- DISEASE AREA: Cancer; InflammationIschemia; Neurodegeneration