NRX-2663 |
| Catalog No.GC64832 |
NRX-2663은 β-카테닌과 그 동족 E3 리가제인 SCFβ-TrCP 사이의 상호작용을 강화하는 역할을 합니다. NRX-2663은 22.9μM의 EC50 및 54.8nM의 Kd로 β-TrCP에 대한 β-카테닌 펩타이드의 결합을 향상시킵니다.
Products are for research use only. Not for human use. We do not sell to patients.
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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