2. NF-κB Apoptosis Immunology/Inflammation Metabolic Enzyme/Protease Autophagy
  3. Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS) Atg8/LC3
  4. Nrf2-IN-4

Nrf2-IN-4 是一种 Nrf2 抑制剂。Nrf2-IN-4 通过抑制 NRF2 诱导铁死亡 (ferroptosis)。Nrf2-IN-4 破坏细胞铁稳态，促进铁蛋白降解，并最终触发铁死亡。Nrf2-IN-4 通过促进铁依赖性活性氧 (ROS) 产生和溶酶体酸化来诱导溶酶体激活。Nrf2-IN-4 显示出显著的抗肿瘤效果。Nrf2-IN-4 可用于乳腺癌研究。

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Nrf2-IN-4 Chemical Structure

Nrf2-IN-4 Chemical Structure

CAS No. : 2417486-06-5

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Nrf2-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nrf2-IN-4 is a Nrf2 inhibitor. Nrf2-IN-4 induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor efficacy. Nrf2-IN-4 can be used for the study of breast cancer[1].

体外研究
(In Vitro)

Nrf2-IN-4 (Compound PhcY) (0.01-10 μM, 72 h) 对多种癌细胞系表现出抑制作用，其 IC50 值分别为：MCF-7细胞 80 nM，HepG2 细胞 3.26 μM，T24 细胞 0.90 μM，HCT116 细胞 2.89 μM，L929 成纤维细胞 3.27 μM，以及HEK293人胚肾细胞 5.36 μM[1]。
Nrf2-IN-4 (40-160 nM) 使 MCF-7 细胞呈现“气球状”和圆形细胞形态，伴有细胞质液泡化[1]。
Nrf2-IN-4 (40-80 nM, 14 days) 以剂量依赖性方式抑制 MCF-7 细胞的克隆形成[1]。
Nrf2-IN-4 (80-160 nM, 24-48 h) 通过抑制 Nrf2 增加 MCF-7 细胞的游离铁池 (LIP) 和铁死亡[1]。
Nrf2-IN-4 (80-320 nM, 24 h) 通过促进铁依赖性活性氧 (ROS) 产生和溶酶体酸化诱导 MCF-7 细胞的溶酶体激活[1]。
Nrf2-IN-4 (40-320 nM, 0-12 h) 通过铁蛋白自噬诱导 MCF-7 细胞的铁蛋白降解[1]。
Nrf2-IN-4 (80-320 nM) 诱导氧化应激，导致 MCF-7 细胞线粒体膜电位显著下降，这一效应可被 Acetylcysteine (N-acetylcysteine) (NAC) (HY-B0215) 减轻[1]。
Nrf2-IN-4 (0.1-0.2 μM) 对肿瘤类器官生长的抑制作用显著优于 ML385 (HY-100523)[1]。

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

Nrf2-IN-4 相关抗体:

Immunofluorescence[1]

Cell Line: MCF-7 cells
Concentration: 80 nM
Incubation Time: 24 h
Result: Increased LIP and reversed the effect and the the effect was reversed by Nrf2knockdown.

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 80, 160 nM
Incubation Time: 48 h
Result: Increased cytotoxicity upon Nrf2 overexpression.
Induced dose-dependent cytotoxicity, which was inhibited by both 1,8-Diazafluoren-9-one (DFO) (HY-D0903) and Ferrostatin-1 (Fer-1) (HY-100579).

Immunofluorescence[1]

Cell Line: MCF-7 cells
Concentration: 80, 160, 320 nM
Incubation Time: 24 h
Result: Increased cathepsin B activity in a dose-dependent manner, which was inhibited by Chloroquine (CQ)(HY-17589A) or DFO.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0, 3, 6, 9, 12 h
Incubation Time: 24 h
Result: Showed a dose-dependent increase in Beclin-1, LC3-II, and ATG5 protein levels.
Reduced intracellular FTH and FTL levels, and this reduction was reversed by autophagy inhibitors(Bafilomycin A1(HY-100558) ,CQ) and the iron chelator DFO.
体内研究
(In Vivo)

Nrf2-IN-4 (Compound PhcY) (10 mg/kg，腹腔注射，每日一次，持续21天) 在 MCF-7 异种移植小鼠模型中展现出显著的肿瘤抑制效果[1]。

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

Animal Model: MCF-7 cells (5 × 106) were injected subcutaneously into each female adult athymic nude mouse [1]
Dosage: 10 mg/kg
Administration: i.p. daily for 21 days
Result: Led to the degradation of FTH and FTL, as well as the upregulation of P53 and LC3-II.
Did not cause notable body weight loss or other observable adverse effects in mice.
分子量

426.32

Formula

C20H13Cl2N5S
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

Nrf2-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Nrf2-IN-42417486-06-5Keap1-Nrf2FerroptosisReactive Oxygen Species (ROS)Atg8/LC3Autophagy-related 8| ferroptosisbreast cancerROSMCF-7 cellsInhibitorinhibitorinhibit

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