2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Nuclear Hormone Receptor 4A/NR4A Apoptosis
  4. Nur77 antagonist 1

Nur77 antagonist 1(Compound ja) 是一种选择性的 Nur77 拮抗剂 。Nur77 antagonist 1 能诱导癌细胞凋亡。Nur77 antagonist 1 对三阴性乳腺癌 (TNBC) 细胞表现出良好的抗肿瘤活性。

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Nur77 antagonist 1 Chemical Structure

Nur77 antagonist 1 Chemical Structure

CAS No. : 2378780-25-5

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Nur77 antagonist 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells[1].

IC50 & Target

Nur77/NR4A1

 

体外研究
(In Vitro)

Nur77 antagonist 1(Compound ja) 对来自不同组织的肿瘤细胞具有选择性，与人类正常乳腺细胞系相比（MCF-10A 的 IC50为48.01 ± 2.86），ja对所有测试的TNBC细胞系（MDA-MB-231, HCC-1806和BT549的IC50分别为0.40 ± 0.03、0.38 ± 0.08和2.12 ± 0.15）具有高度选择性的抗增殖活性[1]。
Nur77 antagonist 1 (0-2 μM, 6 h) 以Nur77依赖性方式诱导MDA-MB-231-sictr细胞凋亡[1]。
Nur77 antagonist 1 (0-5 μM, 6 h) 通过介导MDA-MB-231细胞中的TP53磷酸化途径，诱导Nur77依赖性细胞周期阻滞和凋亡[1]。

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

Nur77 antagonist 1 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0-5 μM
Incubation Time: 6 h
Result: Induced extrinsic Nur77 degradation.
Induced PARP cleavage in a dose- and time-dependent manner in MDA-MB-231 cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.32-5 μM
Incubation Time: 5 h
Result: Exhibited the apoptotic cells accounted for 15.10, 25.38, 40.01, 54.83, and 74.62% at 0.32, 0.63, 1.25, 2.5, and 5.0 μM.
体内研究
(In Vivo)

Nur77 antagonist 1(Compound ja) (10 mg/kg, 腹腔注射) 在乳腺癌MDA-MB-231异种移植裸鼠模型中具有良好的抗肿瘤效果和良好的体内耐受性[1]。
Nur77 antagonist 1 (1.25-5 μM) 在斑马鱼胚胎模型中具有良好的体内安全性[1]。

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

Animal Model: the breast cancer MDA-MB-231 xenograft nude mice model[1]
Dosage: 10 mg/kg
Administration: i.p
Result: Reduced tumor weight and volume with tumor growth inhibition (TGI) of 99.95%.
Increased cleaved caspase 3 and decreased the proliferation marker Ki67 expression in tumor tissues.
分子量

492.64

Formula

C25H32N8OS
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

Nur77 antagonist 1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Nur77 antagonist 12378780-25-5Nuclear Hormone Receptor 4A/NR4AApoptosisNerve Growth Factor IB-like ReceptorNur77 AntagonistTNBCAnticancerMDA-MB-231HCC-1806BT549Inhibitorinhibitorinhibit

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