An analog of adenosine 5'-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM) and disrupts CRL-mediated protein turnover leading to apoptosis in cancer cells by deregulating S-phase DNA synthesis

MLN4924 – 1 mg

Brand:
Cayman
CAS:
905579-51-3
Storage:
-20
UN-No:
Non-Hazardous - /

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 with roles relevant to cellular processes important for cancer cell survival. Neddylation of CRLs is initiated by NEDD8-activating enzyme (NAE), which has become a novel target in cancer therapeutic research.{24455} MLN4924 is an analog of adenosine 5’-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM).{24454} At much higher concentrations, MLN4924 inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2 μM, respectively.{24454} At 0.3 μM, MLN4924 has been shown to disrupt CRL-mediated protein turnover leading to apoptosis in HCT116 cells by deregulating S-phase DNA synthesis.{24454} In vivo, 30-60 mg/kg MLN4924 dose-dependently suppresses the growth of human tumor xenografts in mice.{24454}  

 

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Description

An analog of adenosine 5′-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM) and disrupts CRL-mediated protein turnover leading to apoptosis in cancer cells by deregulating S-phase DNA synthesis

Formal name: sulfamic acid, [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl ester

Synonyms:  Pevonedistat

Molecular weight: 443.5

CAS: 905579-51-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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