NRX 252114

Name: NRX 252114
Brand: Tocris Bioscience
SKU: 7990

Tocris Bioscience, part of Bio-Techne | Catalog # 7990

COA / SDS

Molecular glue Degrader of mutant β-catenin

Key Product Details

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)
Molecular Weight:	510.31

View Full Technical Details for NRX 252114

Technical Data
Citations

Biological Activity for NRX 252114

NRX-252114 is a potent enhancer of the interaction between S37A mutant β-catenin, and its cognate E3 ligase, SCF^β-TrCP (EC₅₀ = 6.5 nM; K_d = 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
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.

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

Solubility for NRX 252114

	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 will 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

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References for NRX 252114

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