NRX-2663|CAS 2763260-34-8|DC Chemicals

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.

Cat. No.	Product name	Field of application
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DC77784	UNC10013	UNC10013 is a SETDB1 allosteric modulator that forms a covalent bond with Cys385 in the 3TD domain, exhibiting negative allosteric regulatory activity. It has a kinact/KI value of 1.0 × 106 M-1*s-1. UNC10013 effectively disrupts SETDB1-mediated Akt methylation and holds potential value for research in cancer and neurodegenerative diseases.
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NRX2663