NRX 252114

Pricing Availability   Qty
Description: Molecular glue Degrader of mutant β-catenin
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
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for NRX 252114

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.

Technical Data for NRX 252114

M. Wt 510.31
Formula C22H12Cl2F3N3O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2763260-39-3
PubChem ID 162640509
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for NRX 252114

Solvent Max Conc. mg/mL Max Conc. mM
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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.96 mL 9.8 mL 19.6 mL
5 mM 0.39 mL 1.96 mL 3.92 mL
10 mM 0.2 mL 0.98 mL 1.96 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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References for NRX 252114

References are publications that support the biological activity of the product.

Simonetta et al (2019) Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction. Nat.Commun. 10 1402 PMID: 30926793

If you know of a relevant reference for NRX 252114, please let us know.

Keywords: NRX 252114, NRX 252114 supplier, NRX252114, e3, ligase, molecular, glue, proximity, inducer, beta, catenin, mutant, S37A, ubiquitination, degradation, degrader, Molecular, Glues, 7990, Tocris Bioscience

Citations for NRX 252114

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Targeted Protein Degradation Research Product Guide

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