1. Stem Cell/Wnt
  2. β-catenin
  3. NRX-103094

NRX-103094 

Cat. No.: HY-141449
Handling Instructions

NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

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

NRX-103094 Chemical Structure

NRX-103094 Chemical Structure

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Description

NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM[1].

IC50 & Target

EC50: 62 nM (β-catenin:β-TrCP Interaction)[1]
Kd: 0.6 nM (β-catenin:β-TrCP Interaction)[1]

In Vitro

NRX-103094 shows high potency with pSer33/Ser37 β-catenin peptide (EC50 of 457 nM). NRX-103094 potentiates the ubiquitylation of pSer33/S37A β-catenin peptide to levels greater than wild-type pSer33/pSer37 levels at 250 nM[1].
NRX-103094 enhances the S33E/S37A phosphomimetic peptide binding affinity for β-TrCP from >5 μM in the absence of compound to 22 nM in the presence of 40 μM compound. In the presence of 20 μM NRX-103094, robust time-dependent ubiquitylation of S33E/S37A β-catenin peptide is observed. Likewise, the full-length S33E/S37A β-catenin protein is strongly ubiquitylated in the presence of 20 μM NRX-103094, with the ubiquitylation levels approaching that of WT full-length β-catenin protein[1].

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

Molecular Weight

503.28

Formula

C₂₀H₁₁Cl₂F₃N₂O₄S

SMILES

OC(C1=CC=CC(NC(C2=C(C=C(NC2=O)C(F)(F)F)SC3=C(C=CC=C3Cl)Cl)=O)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

NRX-103094NRX103094NRX 103094β-cateninBeta cateninE3ligasedegradationmutantSCFβ-TrCPPPISer33Ser37Inhibitorinhibitorinhibit

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Product Name:
NRX-103094
Cat. No.:
HY-141449
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