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NRX-252114
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NRX-252114图片
CAS NO:2763260-39-3
包装:10mg
市场价:9000元

产品介绍
NRX-252114 是一种有效的 β-catenin 与 同源 E3 ligase SCFβ-TrCP 的相互作用增强剂,增强 pSer33/S37A β-catenin 与 β-TrCP 的结合,EC50 为 6.5 nM,Kd 为 0.4 nM。NRX-252114 能够促进突变体 β-catenin 的降解。
Cas No.2763260-39-3
分子式C22H12Cl2F3N3O2S
分子量510.32
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NRX-252114 is a potent enhancer of the interaction betweenβ-catenin, and its cognateE3 ligase, SCFβ-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with anEC50of 6.5 nM and aKdof 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].