NRX-2663 |
| カタログ番号GC64832 |
NRX-2663 は、β-カテニンとその同種の E3 リガーゼである SCFβ-TrCP との間の相互作用のエンハンサーです。 NRX-2663 は、22.9 μM の EC50 と 54.8 nM の Kd で、β-TrCP に対する β-カテニン ペプチドの結合を強化します。
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Cas No.: 2763260-34-8
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
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