Cas No.: | 2763260-34-8 |
Chemical Name: | NRX2663 |
Synonyms: | NRX 2663 |
SMILES: | OC(C1=CC=CC(NC(C2=C(C=C(NC2=O)C(F)(F)F)OC3=CC=CC=C3)=O)=C1)=O |
Formula: | C20H13F3N2O5 |
M.Wt: | 418.32 |
Purity: | >98% |
Sotrage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
Publication: | [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. |
Target: | EC50: 22.9 µM (β-catenin:β-TrCP Interaction)[1] Kd: 54.8 nM (β-catenin:β-TrCP Interaction)[1] |
In Vitro: | NRX-2663 displays both improved potency in the binding assay with pSer33/Ser37 β-catenin (EC50 of 80 µM) and cooperativity of binding (13-fold). NRX-2663 also markedly enhances the ubiquitylation of the pSer33/Ser37 β-catenin peptide, with ubiquitin chain formation at ligand concentrations of 16 μM and above resembling ubiquitin chain formation on wild-type pSer33/pSer37 β-catenin peptide[1]. |
References: | [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. |