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

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.

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NRX-103094 Chemical Structure

NRX-103094 Chemical Structure

CAS No. : 2763260-36-0

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Based on 1 publication(s) in Google Scholar

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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].

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

Molecular Weight

503.28

Formula

C20H11Cl2F3N2O4S

CAS No.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (99.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9870 mL 9.9348 mL 19.8697 mL
5 mM 0.3974 mL 1.9870 mL 3.9739 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.89%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9870 mL 9.9348 mL 19.8697 mL 49.6741 mL
5 mM 0.3974 mL 1.9870 mL 3.9739 mL 9.9348 mL
10 mM 0.1987 mL 0.9935 mL 1.9870 mL 4.9674 mL
15 mM 0.1325 mL 0.6623 mL 1.3246 mL 3.3116 mL
20 mM 0.0993 mL 0.4967 mL 0.9935 mL 2.4837 mL
25 mM 0.0795 mL 0.3974 mL 0.7948 mL 1.9870 mL
30 mM 0.0662 mL 0.3312 mL 0.6623 mL 1.6558 mL
40 mM 0.0497 mL 0.2484 mL 0.4967 mL 1.2419 mL
50 mM 0.0397 mL 0.1987 mL 0.3974 mL 0.9935 mL
60 mM 0.0331 mL 0.1656 mL 0.3312 mL 0.8279 mL
80 mM 0.0248 mL 0.1242 mL 0.2484 mL 0.6209 mL
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NRX-103094 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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