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Applications: Useful for inhibition of the NEDD8 and NEDD8-dependent pathways.
CAS Number: 905579-51-3
Description: Containing the active ingredient of MLN4924 which acts as a substrate-assisted inhibitor of the NEDD8-activating enzyme (NAE). NAE activates NEDD8 (Neural precursor cell expressed, developmentally down-regulated 8) for conjugation to a variety of ubiquitin E3 ligases. NAE inhibitor binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival. This cell permeable compound selectively inhibits NAE activity and results in inhibition of the NEDD8 pathway. Treatment of cells with MLN4924 results in inhibition of the NEDD8 pathway, making MLN4924 a new approach to targeting the UPS for the treatment of cancer.
Format: White powder
Purity: ≥98%
Solubility: Soluble in DMSO (10 mg/ml)
Warnings: Protect from moisture.
Biosafety Level: Not applicable (BSL-1)
References: 1. Brownell, J.E. et al. Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8 - AMP mimetic in situ. Molecular Cell 2010. 37:102-111.
2. Milhollen, M.A. et al. MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF-κB-dependent lymphoma. Blood, 2010. 116:1515-1523.
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