2. Vitamin D Related/Nuclear Receptor
  3. Nuclear Hormone Receptor 4A/NR4A
  4. NR4A agonist-2

NR4A agonist-2 是基于 Vidofludimus (HY-14908) 设计的、选择性泛 NR4A 激动剂 (对 NR4A1 的 Kd=0.10 μM)，对Nur77、Nurr1、NOR-1 的 EC50 分别为 0.098 μM、0.092 μM、0.09 μM。NR4A agonist-2 对 DHODH 的选择性达 47 倍，且在浓度高达 10 μM 时无细胞毒性活性。NR4A agonist-2 通过结合 Nurr1 配体结合域的特定表面口袋，抑制 Nurr1 同源二聚体形成，激活 NBRE、NurRE、DR5 等响应元件，进而强效诱导 BDNF、SOD2 等神经保护基因表达，发挥神经保护活性。NR4A agonist-2 可用于帕金森病、痴呆、多发性硬化症等神经退行性疾病的研究。

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NR4A agonist-2

NR4A agonist-2 Chemical Structure

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NR4A agonist-2 相关抗体

Top Publications Citing Use of Products

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

查看所有亚型
Nur77/NR4A1 Nurr1/NR4A2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis[1].

IC50 & Target

Nur77/NR4A1

0.098 μM (EC50)

Nurr1/NR4A2

0.092 μM (EC50)

体外研究
(In Vitro)

NR4A agonist-2 (compound 53) (0.3-1 μM; 20 h) 可在采用 N27 大鼠多巴胺能神经元的 qPCR 实验中，呈剂量依赖性诱导 BDNF、FLRT2 和 SOD2 等神经保护基因的 mRNA 表达[1]。

NR4A agonist-2 (10 μM; 2 h) 在 HTRF 实验中显著抑制 Nurr1 配体结合域同源二聚体的形成，抑制率约为 9 倍[1]。
NR4A agonist-2 (0.1-10 μM; 24 h) 对 HEK293T 细胞的多种毒性检测中，对细胞汇合度和代谢活性均无显著影响，也不会诱导细胞坏死[1]。

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

NR4A agonist-2 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: HEK293T
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Did not significantly affect cell confluence, metabolic activity, or induce necrosis in HEK293T cells, showing no obvious cytotoxicity at all tested concentrations.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: N27 rat dopaminergic neurons
Concentration: 0.3 μM, 0.6 μM, 1 μM
Incubation Time: 20 h
Result: Dose-dependently induced the mRNA expression of neuroprotective genes including BDNF, FLRT2, NRP-1, CRMP4, Sesn3, CCND2, XIAP, and SOD2, with more potent effects than Vidofludimus (HY-14908) at 1 μM.
分子量

421.78

Formula

C20H14ClF2NO5
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

NR4A agonist-2 相关分类

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Help & FAQs
  • 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:

NR4A agonist-2Nuclear Hormone Receptor 4A/NR4ANuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorDHODHpan-NR4AInhibitorinhibitorinhibit

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