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  3. MLN4924 (Pevonedistat)

MLN4924 (Pevonedistat) #85923

Western blot analysis of extracts from K-562 cells, untreated (-) or treated with MLN4924 (Pevonedistat) (300 nM, 24 hr; +), using NEDD8 (19E3) Rabbit mAb #2754 (upper) or α-Actinin (D6F6) XP® Rabbit mAb #6487 (lower).
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Product Information

Product Usage Information

MLN4924 (Pevonedistat) is supplied as a lyophilized powder. For a 5 mM stock, reconstitute 1 mg of powder in 451.2 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 443.2 g/mol
Purity >98%
Molecular Formula C21H25N5O4S
CAS 905579-51-3
Solubility Soluble in DMSO at 10 mg/ml.

Background

MLN4924 (Pevonedistat) is a potent and selective inhibitor of NEDD8-activating enzyme (NAE) (1). The NAE is part of the NEDD8 conjugation pathway that involves the ubiquitin-like NEDD8 protein and cullin-RING ligases (CRL). The NAE is responsible for the covalent attachment of NEDD8 to cullin proteins, termed neddylation, resulting in a conformational change within the CRL, analogous to ubiquitination. This is a reversible, multi-step process responsible for cell cycle progression and survival pathways in cancer cells (2). The inhibition of NAE by MLN4924 (Pevonedistat) induces apoptosis in human tumor cells and reduces human tumor xenograft growth in mice (IC50 = 4.7 nM) (1-3).

限制使用

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For Research Use Only. Not For Use In Diagnostic Procedures.
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