NRX-252114 | β-catenin degrader | Probechem Biochemicals

Chemical Structure : NRX-252114

CAS No.: 2763260-39-3

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NRX-252114 (NRX 252114, NRX252114)

货号: PC-36151Not For Human Use, Lab Use Only.

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule β-TrCP-based degrader of β-catenin, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).

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2 mg	￥2580	In stock
5 mg	￥4280	In stock
10 mg	￥7280	In stock
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100 mg		Get quote

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生物&药学活性

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule β-TrCP-based degrader of β-catenin, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).
NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of WT doublyphosphorylated peptide in vitro.
NRX-252114 induces the degradation of an engineered mutant β-Catenin in a cellular system.
NRX-252114 inserts into a naturally occurring PPI interface, with contacts optimized for both the substrate and ligase within the same small molecule entity, which is distinct from PROTACs.

物理化学性质&存储条件

分子量	510.312
分子式	C22H12Cl2F3N3O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(4-((2,6-dichlorophenyl)thio)-2-oxo-6-(trifluoromethyl)-1,2-dihydropyridine-3-carbonyl)isoindoline-4-carbonitrile

参考文献

1. Simonetta KR, et al. Nat Commun. 2019 Mar 29;10(1):1402.

NRX-252114 (NRX 252114, NRX252114)

生物&药学活性

物理化学性质&存储条件

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NRX-252114 (NRX 252114, NRX252114)

生物&药学活性

物理化学性质&存储条件

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