NRX 252114
Tocris Bioscience, part of Bio-Techne | Catalog # 7990
Molecular glue Degrader of mutant β-catenin
Key Product Details
Description
Molecular glue Degrader of mutant β-catenin
Product Description
NRX-252114 is a potent enhancer of the interaction between S37A mutant β-catenin, and its cognate E3 ligase, SCFβ-TrCP (EC50 = 6.5 nM; Kd = 0.4 nM). NRX-252114 is a molecular glue degrader that binds at the phosphoserine binding site on β-TrCP and induces mutant β-catenin ubiquitination and subsequent degradation.Product Specifications
Molecular Weight
510.31
Formula
C22H12Cl2F3N3O2S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
2-[[4-[(2,6-Dichlorophenyl)thio]-1,2-dihydro-2-oxo-6-(trifluoromethyl)-3-pyridinyl]carbonyl]-2,3-dihydro-1H-isoindole-4-carbonitrile
CAS Number
2763260-39-3
PubChem ID
162640509
InChI Key
BMQXGPBUQGPLOV-UHFFFAOYSA-N
SMILES
N#CC1=CC=CC2=C1CN(C2)C(C3=C(SC4=C(Cl)C=CC=C4Cl)C=C(C(F)(F)F)NC3=O)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.03 | 100 | |
| Ethanol | 5.1 | 10 |
Preparing Stock Solutions
for NRX 252114
The following data is based on the product molecular weight 510.31
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.96 mL | 9.80 mL | 19.60 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.92 mL |
| 10 mM | 0.20 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.20 mL | 0.39 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Simonetta Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction. Nat.Commun. 2019 PMID: 30926793
Product Specific Notices for NRX 252114
For research use only
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