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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $67 | In Stock | |
5 mg | $163 | In Stock | |
10 mg | $289 | In Stock | |
25 mg | $578 | In Stock | |
50 mg | $913 | In Stock | |
100 mg | $1,370 | In Stock |
Description | 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. |
Targets&IC50 | β-catenin-β-TrCP:0.6 nM(Kd), β-catenin-β-TrCP:62 nM(EC50) |
In vitro | RX-103094 demonstrates high potency against the pSer33/Ser37 β-catenin peptide with an EC50 of 457 nM. At 250 nM, NRX-103094 enhances the ubiquitylation of the pSer33/S37A β-catenin peptide to levels surpassing those of the wild-type pSer33/pSer37.[1] NRX-103094 significantly enhances the binding affinity of the S33E/S37A phosphomimetic peptide for β-TrCP, reducing it from >5 μM in the absence of the compound to 22 nM in the presence of 40 μM NRX-103094. In the presence of 20 μM NRX-103094, we observe robust, time-dependent ubiquitylation of the S33E/S37A β-catenin peptide. Similarly, when 20 μM NRX-103094 is present, the full-length S33E/S37A β-catenin protein undergoes strong ubiquitylation, with ubiquitylation levels approaching those of the WT full-length β-catenin protein.[1] |
Alias | NRX103094, NRX 103094 |
Molecular Weight | 503.28 |
Formula | C20H11Cl2F3N2O4S |
Cas No. | 2763260-36-0 |
Smiles | 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 |
Storage | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (79.48 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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