MLN4924

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MLN4924

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Cat No: 15217

Biochemicals - Small Molecule Inhibitors

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 impor...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

NEDD8 NEDD 8 selective inhibitor inhibit activating enzyme MLN 4924 cancer cell biology ubiquitin-proteasome ubiquitin-proteasome biochemical HCT-116

Product Overview:
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}

Size	1 mg
Shipping	dry ice
CAS Number	905579-51-3
Molecular Formula	C₂₁H₂₅N₅O₄S
SMILES	O[C@H]([C@H](COS(N)(=O)=O)C1)C[C@@H]1N2C=CC3=C(N[C@@H]4C(C=CC=C5)=C5CC4)N=CN=C23
Molecular Weight	443,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2930.90
UNSPSC code	12352100

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MSDS

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Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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