NRX-103094

Research use only, not for human use.

NRX-103094 is a potent enhancer of the interaction between β-catenin and the homologous E3 ligase SCFβ-TrCP, increasing the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

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.

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.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.

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Wnt/Notch/Hedgehog

Wnt/beta/catenin

Wnt/beta-catenin

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2763260-36-0

503.28

C20H11Cl2F3N2O4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (99.35 mM; Ultrasonic )

S(C1=C(C(NC2=CC(C(O)=O)=CC=C2)=O)C(=O)NC(C(F)(F)F)=C1)C3=C(Cl)C=CC=C3Cl

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(-20℃)

With Ice Pack

≥ 2 years