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Potent, selective and cell permeable inhibitor of Nedd8 E1 Activating Enzyme (NAE) (IC50=4.7nM). NEDD8 is an ubiquitin-like protein whose activity is required to activate cullin-RING ubiquitin E3 ligases (CRLs) responsible for the ubiquitination and proteasome-dependent turnover of certain substrates relevant to cancer cell survival.
Anticancer agent with in vitro and in vivo activity. By inhibiting the Neddylation pathway this molecule disrupts cullin-RING ligase activity, leading to inhibition of proliferation or apoptotic death of various human tumor cells through the deregulation of S-phase DNA synthesis.
Inhibits related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2μM, respectively.
Angiogenesis inhibitor and autophagy inducer.
Antiviral agent. Exhibited pronounced antiviral activity against mouse and human cytomegalovirus, herpes simplex virus (HSV)- 1 (including multi-drug resistant clinical isolates), HSV-2, adeno and influenza viruses.
Product References
Targeting NEDD8-activated cullin-RING ligases for the treatment of cancer: T.A. Soucy, et al.; Clin. Cancer Res. 15, 3912 (2009)
An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer: T.A. Soucy, et al.; Nature 458, 732 (2009)
Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ: J.E. Brownell, et al.; Mol. Cell. 37, 102 (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: M.A. Milhollen, et al.; Blood 116, 1515 (2010)
NEDD8-targeting drug MLN4924 elicits DNA rereplication by stabilizing Cdt1 in S phase, triggering checkpoint activation, apoptosis, and senescence in cancer cells: J.J. Lin, et al.; Cancer Res. 70, 10310 (2010)
The Nedd8-activating enzyme inhibitor MLN4924 induces autophagy and apoptosis to suppress liver cancer cell growth: Z. Luo, et al.; Cancer Res. 72, 3360 (2012)
MLN4924: a novel first-in-class inhibitor of NEDD8-activating enzyme for cancer therapy: S.T. Nawrocki, et al.; Expert. Opin. Investig. Drugs 21, 1563 (2012) (Review)
Inactivation of the Cullin (CUL)-RING E3 ligase by the NEDD8-activating enzyme inhibitor MLN4924 triggers protective autophagy in cancer cells: Z. Luo, et al.; Autophagy 8, 1677 (2012)
MLN4924, an NAE inhibitor, suppresses AKT and mTOR signaling via upregulation of REDD1 in human myeloma cells: Y. Gu, et al.; Blood 123, 3269 (2014)
Suppression of tumor angiogenesis by targeting the protein neddylation pathway: W.T. Yao, et al.; Cell Death Dis. 5, e1059 (2014)
MLN4924, a Novel NEDD8-activating enzyme inhibitor, exhibits antitumor activity and enhances cisplatin-induced cytotoxicity in human cervical carcinoma: in vitro and in vivo study: W.C. Lin, et al.; Am. J. Cancer Res. 5, 3350 (2015)
Broad and potent antiviral activity of the NAE inhibitor MLN4924: V.T. Le-Trilling, et al.; Sci. Rep. 6, 19977 (2016)
NEDD8-activating enzyme inhibitor, MLN4924 (Pevonedistat) induces NOXA-dependent apoptosis through up-regulation of ATF-4: X. Liu, et al.; BBRC 488, 1 (2017)
Targeting the protein ubiquitination machinery in melanoma by the NEDD8-activating enzyme inhibitor pevonedistat (MLN4924): K.M. Wong, et al.; Invest. New Drugs 35, 11 (2017)
Mechanism of Resistance to the WDR5 Inhibitor in MLL-Rearranged Leukemia: L. Liu, et al.; ACS Chem. Biol. ahead of print (2023)
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