1. Stem Cell/Wnt
  2. β-catenin
  3. NRX-252114

NRX-252114 

Cat. No.: HY-111836
Handling Instructions

NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation.

For research use only. We do not sell to patients.

NRX-252114 Chemical Structure

NRX-252114 Chemical Structure

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Description

NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation[1].

IC50 & Target

EC50: 6.5 nM (β-catenin:β-TrCP Interaction)[1]
Kd: 0.4 nM (β-catenin:β-TrCP Interaction)[1]

In Vitro

NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of wild-type doubly-phosphorylated peptide. NRX-252114 further enhances the ubiquitylation of pSer33/S37A β-catenin peptide to form long ubiquitin chains[1].
The non-phosphorylated Ser33/Ser37 peptide binds β-TrCP with very weak affinity (>100 μM); however, in the presence of 20 μM NRX-252114 that binding affinity is enhanced to 180 nM. NRX-252114 also potentiates the ubiquitylation of unphosphorylated Ser33/S37A β-catenin peptides by the SCFβ-TrCP complex[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

510.32

Formula

C₂₂H₁₂Cl₂F₃N₃O₂S

SMILES

N#CC1=CC=CC2=C1CN(C(C3=C(SC4=C(Cl)C=CC=C4Cl)C=C(C(F)(F)F)NC3=O)=O)C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

NRX-252114NRX252114NRX 252114β-cateninBeta cateninE3ligasedegradationmutantSCFβ-TrCPPPISer33Ser37Inhibitorinhibitorinhibit

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Product Name:
NRX-252114
Cat. No.:
HY-111836
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