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NRX-252114
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。
NRX-252114 Chemical Structure
CAS No. : 2763260-39-3
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100 mg |
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250 mg |
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500 mg |
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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, 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].
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IC50 & Target |
EC50: 6.5 nM (β-catenin:β-TrCP Interaction)[1] Kd: 0.4 nM (β-catenin:β-TrCP Interaction)[1]
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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.
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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