2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid

2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid Chemische Eigenschaften,Einsatz,Produktion Methoden

Allgemeine Beschreibung

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/A_2A/A_2B/A₃, or a panel of 12 cellular kinases. Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (IC_max = 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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51471	80

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• 2-[[2-[[2-[(9-oxo-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-7-yl)oxy]acetyl]amino]acetyl]amino]acetic acid
• 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-
• 951950-33-7