MLN4924 | NEDD8 activating enzyme inhibitor
NMR (Conforms)
Available Options
| size : | Price | Quantity | |
|---|---|---|---|
| 1 mg | $60.00 | ||
| 5 mg | $220.00 |
MLN4924 (905579-51-3) 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.
References/Citations:
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
MLN4924 (905579-51-3) 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.
References/Citations:
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
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