2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. Nuclear Hormone Receptor 4A/NR4A RAR/RXR
  4. Nurr1/RXR agonist 1

Nurr1/RXR dual agonist 1 是 Nurr1 (EC50 = 2.6 µM) 与 RXR 的双重激活剂，其 Ks 值分别为 0.6 和 1.1 µM。Nurr1/RXR dual agonist 1选择性破坏 Nurr1 同源二聚体的稳定性并稳定 Nurr1:RXR 异源二聚体，从而特异性激活异源二聚体反应元件 DR5。在神经元细胞中，Nurr1/RXR dual agonist 1 可增强特定神经保护性 Nurr1 靶基因子集的表达，同时避免诱导与潜在脱靶效应相关的基因。Nurr1/RXR dual agonist 1可用于神经退行性疾病的研究。

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Nurr1/RXR agonist 1

Nurr1/RXR agonist 1 Chemical Structure

CAS No. : 2231746-53-3

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Nurr1/RXR agonist 1 相关抗体

Top Publications Citing Use of Products

查看 Nuclear Hormone Receptor 4A/NR4A 亚型特异性产品:

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Nur77/NR4A1 Nurr1/NR4A2

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RXRα RXRβ RXRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR with K[1]s of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research[1].

IC50 & Target[1]

Nurr1/NR4A2

 

体外研究
(In Vitro)

Nurr1/RXR agonist 1 (compound 2) (15 h) 介导了相当显著的 3.3 倍 Nurr1 激活，并对 Nurr1 和 RXR 均有效[1]。
Nurr1/RXR agonist 1 (10 μM) 能减少 Nurr1 同源二聚体的形成，同时保持 Nurr1:RXR 异源二聚体完整[1]。
Nurr1/RXR agonist 1 (0.3-30 μM) 可增强 DR5 依赖性转录，但不激活 NBRE或 NurRE[1]。
Nurr1/RXR agonist 1 (3-30 μM，24 h) 在 HEK293T 细胞中未表现出毒性效应[1]。
Nurr1/RXR agonist 1 (10 μM，21 h)在大鼠多巴胺能神经元中实现了对下游基因表达程序的差异化调控或功能选择性激活[1]。
Nurr1/RXR agonist 1 所诱导的基因，在其启动子区含有 DR5 元件的经验概率更高[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Nurr1/RXR agonist 1 相关抗体:

Real Time qPCR[1]

Cell Line: rat dopaminergic neurons
Concentration: 10 μM
Incubation Time: 21 h
Result: Induced the expression of tyrosine hydroxylase (TH), fibronectin leucine rich transmembrane protein 2 (FLRT2), brain-derived neurotrophic factor (BDNF) and collapsin response mediator protein 4 (CRMP4; Dpysl3 in rat).
Did not induced X-linked inhibitor of apoptosis protein (XIAP), sestrin 3 (SESN3), cyclin D2 (CCND2), baculoviral inhibitor of apoptosis repeat-containing 5 (BIRC5), and superoxide dismutase 2 (SOD2).
分子量

319.35

Formula

C18H19F2NO2
CAS 号
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.
纯度 & 产品资料
参考文献

Nurr1/RXR agonist 1 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nurr1/RXR agonist 12231746-53-3Nuclear Hormone Receptor 4A/NR4ARAR/RXRNuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorRetinoic acid receptorsRetinoid X receptorsNurr1RXRNurr1:RXR heterodimerneurodegenerative diseasesDR5Inhibitorinhibitorinhibit

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