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

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

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Nur77/NR4A1 Nurr1/NR4A2

  • 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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BT-549 IC50
2.12 μM
Compound: ja
Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
Bel-7402 IC50
38.33 μM
Compound: ja
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
HCC1806 IC50
0.38 μM
Compound: ja
Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
HCT-116 IC50
9.84 μM
Compound: ja
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
HT-29 IC50
47.16 μM
Compound: ja
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
HeLa IC50
1.99 μM
Compound: ja
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
HeLa IC50
9.15 μM
Compound: ja
Antiproliferative activity against human HeLa cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human HeLa cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
HepG2 IC50
53.72 μM
Compound: ja
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
MCF-10A IC50
48.01 μM
Compound: ja
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
MCF7 IC50
0.72 μM
Compound: ja
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
MDA-MB-231 IC50
0.4 μM
Compound: ja
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
SW-620 IC50
18.09 μM
Compound: ja
Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
T47D IC50
1.05 μM
Compound: ja
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
T47D IC50
6.34 μM
Compound: ja
Antiproliferative activity against human T47D cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay
Antiproliferative activity against human T47D cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay
[PMID: 37983615]
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/NR4AApoptosisNuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorNur77 AntagonistTNBCAnticancerMDA-MB-231HCC-1806BT549Inhibitorinhibitorinhibit

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