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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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