NRX-252114 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NRX-252114

NRX-252114 是一种有效的 β-catenin 与同源 E3 ligase SCF^β-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，K_d 为 0.4 nM。NRX-252114 能够促进突变体 β-catenin 的降解。

NRX-252114 Chemical Structure

CAS No. : 2763260-39-3

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生物活性	NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF^β-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC₅₀ of 6.5 nM and a K_d of 0.4 nM. NRX-252114 induces mutant β-catenin degradation^[1].
IC₅₀ & Target	EC50: 6.5 nM (β-catenin:β-TrCP Interaction)^[1] Kd: 0.4 nM (β-catenin:β-TrCP Interaction)^[1]
体外研究 (In Vitro)	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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	510.32
Formula	C₂₂H₁₂Cl₂F₃N₃O₂S
CAS 号	2763260-39-3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[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.

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