NRX-252114

NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation[1].

Product Specifications

CAS Number

[2763260-39-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Molecular Glues; β-catenin

Type

Reference compound

Related Pathways

PROTAC; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/nrx-252114.html

Purity

99.43

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

N#CC1=CC=CC2=C1CN(C(C3=C(SC4=C(Cl)C=CC=C4Cl)C=C(C(F)(F)F)NC3=O)=O)C2

Molecular Formula

C22H12Cl2F3N3O2S

Molecular Weight

510.32

Precautions

H302, H315, H319

References & Citations

[1]Kyle R Simonetta, et al. Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction. Nat Commun. 2019 Mar 29;10 (1) :1402.