2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid
- CAS No.
- 951950-33-7
- Chemical Name:
- 2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid
- 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
- CBNumber:
- CB74208023
- Molecular Formula:
- C17H18N4O6
- Molecular Weight:
- 374.35
- MDL Number:
- MOL File:
- 951950-33-7.mol
- MSDS File:
- SDS
2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid price More Price(1)
2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid Chemical Properties,Uses,Production
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
2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid Preparation Products And Raw materials
Raw materials
Preparation Products
2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51456 | 80 |
Supplier | Advantage |
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Sigma-Aldrich | 80 |