| MLN 4924 |
| 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 |
| (CAS 905579-51-3) |
 |
| Description： |
MLN4924 is a potent and selective small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50 = 4.7 nM).
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.MLN 4924 is an analog of adenosine 5’-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM).At much higher concentrations, MLN 4924 inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2 μM, respectively.At 0.3 μM, MLN 4924 has been shown to disrupt CRL-mediated protein turnover leading to apoptosis in HCT-116 cells by deregulating S-phase DNA synthesis.In vivo, 30-60 mg/kg MLN 4924 dose-dependently suppresses the growth of human tumor xenografts in mice.
|
| Product No. |
KT00578 |
| Product Name |
MLN 4924 |
| Synonyms |
Pevonedistat |
| 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 |
| CAS Number |
905579-51-3 |
| Molecular Formula |
C21H25N5O4S |
| Formula Weight |
443.52 |
| Formulation |
A crystalline solid |
| Purity |
98%min |
| Stability |
2 years |
| Storage |
-20°C |
| Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
| Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
| Price & Availability |
In Stock. Price Negotiated. |
|
| Related Products： |
P005091
WP1130
MLN4924 hydrochloride
|
|
