NRX-103094 | 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-103094

NRX-103094 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/Ser37 β-catenin 与 β-TrCP 的结合，EC₅₀ 为 62 nM，K_d 为 0.6 nM。

NRX-103094 Chemical Structure

CAS No. : 2763260-36-0

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250 mg		询价
500 mg		询价

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生物活性	NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF^β-TrCP. NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC₅₀ of 62 nM and a K_d of 0.6 nM^[1].
IC₅₀ & Target	EC50: 62 nM (β-catenin:β-TrCP Interaction)^[1] Kd: 0.6 nM (β-catenin:β-TrCP Interaction)^[1]
体外研究 (In Vitro)	NRX-103094 shows high potency with pSer33/Ser37 β-catenin peptide (EC₅₀ of 457 nM). NRX-103094 potentiates the ubiquitylation of pSer33/S37A β-catenin peptide to levels greater than wild-type pSer33/pSer37 levels at 250 nM^[1]. NRX-103094 enhances the S33E/S37A phosphomimetic peptide binding affinity for β-TrCP from >5 μM in the absence of compound to 22 nM in the presence of 40 μM compound. In the presence of 20 μM NRX-103094, robust time-dependent ubiquitylation of S33E/S37A β-catenin peptide is observed. Likewise, the full-length S33E/S37A β-catenin protein is strongly ubiquitylated in the presence of 20 μM NRX-103094, with the ubiquitylation levels approaching that of WT full-length β-catenin protein^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	503.28
Formula	C₂₀H₁₁Cl₂F₃N₂O₄S
CAS 号	2763260-36-0
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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