Bulk Inquiry
MLN4924
- Pevonedistat
Axon 2038
CAS:
905579-51-3
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C21H25N5O4S
- MW: 443.52
Description
MLN4924 (Pevonedistat) is a first-in-class, cell-permeable NEDD8-activating enzyme (NAE) inhibitor. It blocks cullin neddylation and inactivates Cullin-RING E3 ubiquitin ligases, leading to accumulation of CRL substrates.
Neddylation regulates protein turnover, DNA replication licensing, cell-cycle progression and stress responses. MLN4924 is useful for studying ubiquitin-proteasome pathway pharmacology and antitumor mechanisms linked to CRL inhibition.
Key Features
- First-in-class NAE inhibitor
- Blocks cullin neddylation
- Inactivates Cullin-RING E3 ligases
- Cell-permeable tool with antitumor activity in reported models
Applications
- Neddylation pathway assays
- Cullin-RING ligase research
- Ubiquitin-proteasome system studies
- Oncology pharmacology models
More Information
| Parent CAS No. | 905579-51-3 |
|---|---|
| Chemical Name | ((1S,2S,4R)-4-(4-((S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate |
| SMILES | S(N)(OC[C@@H]1C[C@@H](N2C3C(C=C2)=C(N[C@@H]2C4=C(C=CC=C4)CC2)N=CN=3)C[C@@H]1O)(=O)=O |&1:4,6,14,27,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H25N5O4S/c22-31(28,29)30-11-14-9-15(10-19(14)27)26-8-7-17-20(23-12-24-21(17)26)25-18-6-5-13-3-1-2-4-16(13)18/h1-4,7-8,12,14-15,18-19,27H,5-6,9-11H2,(H2,22,28,29)(H,23,24,25)/t14-,15+,18-,19-/m0/s1 |
| InChiKey | MPUQHZXIXSTTDU-QXGSTGNESA-N |
| CID | 16720766 |
| Short Description | NAE inhibitor |
References
- TA Soucy et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 2009, 458, 732-736.
- TA Soucy et al. Targeting NEDD8-Activated Cullin-RING Ligases for the Treatment of Cancer. Clin. Cancer Res. 2009, 15, 3912.
- Y Zhao et al. Targeting Cullin-RING ligases by MLN4924 induces autophagy via modulating the HIF1-REDD1-TSC1-mTORC1-DEPTOR axis. Cell Death and Disease 2012, 3, e386.
- JL Toth et al. A Gatekeeper Residue for NEDD8-Activating Enzyme Inhibition by MLN4924. Cell Reports, 2012, 1(4), 309-316.
Other Categories
Get a Quote for
Loading...