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2763260-39-3

2763260-39-3 Structure

2763260-39-3 Structure
IdentificationBack Directory
[Name]

1H-Isoindole-4-carbonitrile, 2-[[4-[(2,6-dichlorophenyl)thio]-1,2-dihydro-2-oxo-6-(trifluoromethyl)-3-pyridinyl]carbonyl]-2,3-dihydro-
[CAS]

2763260-39-3
[Synonyms]

1H-Isoindole-4-carbonitrile, 2-[[4-[(2,6-dichlorophenyl)thio]-1,2-dihydro-2-oxo-6-(trifluoromethyl)-3-pyridinyl]carbonyl]-2,3-dihydro-
[Molecular Formula]

C22H12Cl2F3N3O2S
[MOL File]

2763260-39-3.mol
[Molecular Weight]

510.32
Chemical PropertiesBack Directory
[Boiling point ]

632.1±55.0 °C(Predicted)
[density ]

1.62±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[form ]

Solid
[pka]

5.41±0.10(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Description]

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].

NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of wild-type doubly-phosphorylated peptide. NRX-252114 further enhances the ubiquitylation of pSer33/S37A β-catenin peptide to form long ubiquitin chains[1].
The non-phosphorylated Ser33/Ser37 peptide binds β-TrCP with very weak affinity (>100 μM); however, in the presence of 20 μM NRX-252114 that binding affinity is enhanced to 180 nM. NRX-252114 also potentiates the ubiquitylation of unphosphorylated Ser33/S37A β-catenin peptides by the SCFβ-TrCP complex[1].

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