Benzoic acid, 3-[[[1,2-dihydro-2-oxo-4-phenoxy-6-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-

Benzoic acid, 3-[[[1,2-dihydro-2-oxo-4-phenoxy-6-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]- Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 μM and a Kd of 54.8 nM[1]. NRX-2663 displays both improved potency in the binding assay with pSer33/Ser37 β-catenin (EC50 of 80 μM) and cooperativity of binding (13-fold). NRX-2663 also markedly enhances the ubiquitylation of the pSer33/Ser37 β-catenin peptide, with ubiquitin chain formation at ligand concentrations of 16 μM and above resembling ubiquitin chain formation on wild-type pSer33/pSer37 β-catenin peptide[1].

• Einzelnachweise

  [1]. Kyle R Simonetta, et al. Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction. Nat Commun. 2019 Mar 29;10(1):1402.

Benzoic acid, 3-[[[1,2-dihydro-2-oxo-4-phenoxy-6-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]- Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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