Pevonedistat
Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice[1].
Product Specifications
CAS Number
[905579-51-3]
Product Name Alternative
MLN4924
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; NEDD8-activating Enzyme
Type
Reference compound
Related Pathways
Apoptosis; Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/MLN4924.html
Concentration
10mM
Purity
99.98
Solubility
DMSO : 62.5 mg/mL (ultrasonic)
Smiles
O=S(OC[C@@H]1C[C@@H](N2C3=NC=NC(N[C@H]4CCC5=C4C=CC=C5)=C3C=C2)C[C@@H]1O)(N)=O
Molecular Formula
C21H25N5O4S
Molecular Weight
443.52
Precautions
H302, H315, H319, H335
References & Citations
[1]Soucy TA, et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature. 2009 Apr 9;458 (7239) :732-6.|[2]F S Wolenski, et al. The NAE inhibitor pevonedistat (MLN4924) synergizes with TNF-α to activate apoptosis. Cell Death Discovery 1, Article number: 15034 (2015)
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Citation 01
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