NRX-252114( NRX 252114 | NRX252114 )

Catalog No. M17009 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

NRX-252114
Note

Research use only, not for human use.
Brief Description

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule enhancer of β-catenin-β-TrCP interaction, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).
Description

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule enhancer of β-catenin-β-TrCP interaction, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM); NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of WT doublyphosphorylated peptide in vitro, induces the degradation of an engineered mutant β-Catenin in a cellular system; inserts into a naturally occurring PPI interface, with contacts optimized for both the substrate and ligase within the same small molecule entity, which is distinct from PROTACs.
In Vitro

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In Vivo

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Synonyms

NRX 252114 | NRX252114
Pathway

Proteasome/Ubiquitin
Target

E3 Ubiquitin Ligase
Recptor

E3 Ubiquitin Ligase
Research Area

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Indication

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CAS Number

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Formula Weight

510.312
Molecular Formula

C22H12Cl2F3N3O2S
Purity

>98% (HPLC)
Solubility

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SMILES

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Chemical Name

2-(4-((2,6-dichlorophenyl)thio)-2-oxo-6-(trifluoromethyl)-1,2-dihydropyridine-3-carbonyl)isoindoline-4-carbonitrile

1. Simonetta KR, et al. Nat Commun. 2019 Mar 29;10(1):1402.

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