| Identification | Back Directory | [Name]
2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid | [CAS]
951950-33-7 | [Synonyms]
NAE Inhibitor, MLN4924 - CAS 951950-33-7 - Calbiochem
Glycine, N-[2-[(1,2,3,9-tetrahydro-9-oxopyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]glycyl-
2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid | [Molecular Formula]
C17H18N4O6 | [MOL File]
951950-33-7.mol | [Molecular Weight]
374.35 |
| Chemical Properties | Back Directory | [density ]
1.56±0.1 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
DMSO: 100mg/mL | [form ]
Light beige solid | [pka]
3.31±0.10(Predicted) | [color ]
light beige |
| Hazard Information | Back Directory | [Uses]
MLN4924 has been used as a neddylation inhibitor:
- to tre at cell lines stably expressing a GaLV/MLV chimera construct in order to study its effects on viral transduction and infectivity
- to study its effects on the accumulation of LCMT1, suggesting a potential role in regulating LCMT1 stability and degradation in LNCaP cells
- to study UBX-390-mediated degradation of androgen receptor (AR) via proteasomal action in a prostate cancer cell line
| [General Description]
A cell-permeable AMP mimetic that targets the NEDD8-activating E1 enzyme NAE nucleotide-binding site and undergoes a NAE-catalyzed covalent NEDD8 adduct formation, the adduct in turn acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7 nM), exhibiting much reduced or little potency against UAE/UBA1, UBA6/UBE1L2, SAE, ATG7, adenosine receptors A1/A2A/A2B/A3, or a panel of 12 cellular kinases. Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (ICmax = 90 nM in HCT-116 cultures in 24 h), resulting in cullin-RING ligases substrates elevation. Shown to inhibit the growth of various cancer cells both in cultures (IC50 from 50 nM to 1.03 μM) in vitro and in murine xenograft models (30 to 60 mg/kg via s.c.) in vivo via apoptosis induction. | [Biochem/physiol Actions]
Cell permeable: yes |
|
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
|