2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Necroptosis TrxR Reactive Oxygen Species (ROS)
  4. Necroptosis inducer 1

Necroptosis inducer 1 是一种坏死性凋亡 (Necroptosis) 诱导剂。Necroptosis inducer 1 可抑制硫氧还蛋白还原酶 (TrxR) 活性，提升细胞内 ROS 水平，触发 ROS 介导的坏死性凋亡，并诱导依赖坏死性凋亡的免疫原性细胞死亡。Necroptosis inducer 1 可抑制肿瘤生长、重塑肿瘤免疫微环境，且在动物模型中与 anti-PD-1 具有协同作用。Necroptosis inducer 1 可用于结肠癌的研究。

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Necroptosis inducer 1

Necroptosis inducer 1 Chemical Structure

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Necroptosis inducer 1 相关抗体

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TrxR1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Necroptosis inducer 1 is a necroptosis inducer. Necroptosis inducer 1 inhibits the activity of thioredoxin reductase (TrxR), elevates intracellular ROS levels, triggers ROS-mediated necroptosis, and induces necroptosis-dependent immunogenic cell death. Necroptosis inducer 1 inhibits tumor growth, remodels the tumor immune microenvironment, and exerts a synergistic effect with anti-PD-1 in animal models. Necroptosis inducer 1 is applicable to the research of colon cancer[1].

体外研究
(In Vitro)

Necroptosis inducer 1 (Compound Au-1) (48 h) 在多种癌细胞系中表现出强细胞毒性，对 CT-26 细胞的活性最强 (IC50 = 1.03 μM)[1]。
Necroptosis inducer 1 (0.5-2 μM; 24-48 h) 可在体外以浓度和时间依赖的方式抑制 CT-26 细胞中的 TrxR 活性[1]。
Necroptosis inducer 1 (0.5-2 μM; 24 h) 可在 CT-26 细胞中诱导浓度依赖性的细胞内 ROS 积累[1]。
Necroptosis inducer 1 (0.5-4 μM; 24-48 h) 可触发 ROS 介导的坏死性凋亡，作为 CT-26 细胞中占主导地位的细胞死亡途径，其特征为坏死性凋亡相关蛋白上调、Annexin V−/PI+细胞增加、PI 摄取及 LDH 释放[1]。
Necroptosis inducer 1 (1-2 μM; 24 h) 可在 CT-26 细胞中诱导坏死性凋亡依赖性的免疫原性细胞死亡 (ICD)，其特征为呈浓度依赖性的胞外钙网蛋白 (ecto-CRT) 暴露、ATP 释放以及 HMGB1 释放[1]。

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

Necroptosis inducer 1 相关抗体:
体内研究
(In Vivo)

Necroptosis inducer 1 (Compound Au-1) (10 mg/kg; i.v.; 两次; 每次间隔 48 小时) 对原位 CT-26 肿瘤的肿瘤生长抑制率 (IRT) 达 74.2%，对远端 CT-26 肿瘤的 IRT 达 83.9%，同时维持小鼠体重[1]。
Necroptosis inducer 1 (10 mg/kg; i.v.; 每隔两天一次共 24 天) 给药后 IRT 达 43.1%，与抗 PD-1 联合用药时的 IRT 达 66.2%；可通过激活 CD8+ 和 CD4+ 辅助 T 细胞、减少调节性 T 细胞来重塑肿瘤免疫微环境，同时维持小鼠体重[1]。

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

Animal Model: BALB/c (4-week-old, sex not specified, subcutaneously inoculated with CT-26 cells to establish primary and distant tumors)[1]
Dosage: 10 mg/kg
Administration: i.v.; twice with 48-hour interval
Result: Achieved a 74.2% inhibition rate of tumor growth (IRT) in primary tumors.
Achieved an 83.9% IRT in distant tumors.
Maintained stable body weight throughout the treatment period.
Animal Model: BALB/c (4-week-old, sex not specified, subcutaneously inoculated with CT-26 cells to establish tumors reaching ~50 mm3)[1]
Dosage: 10 mg/kg
Administration: i.v.; every 48 hours
Result: Achieved a 43.1% IRT as monotherapy.
Achieved a 66.2% IRT in combination with anti-PD-1.
Maintained stable body weight throughout the treatment period.
Increased tumor-infiltrating CD3+CD8+ T cells from 0.83% to 3.57%.
Increased proportions of CD3+CD8+CD38+ T cells from 10.03% to 37.68% and CD3+CD8+Ki67+ T cells from 30.44% to 48.20%.
Increased percentages of CD8+ T cells expressing TNF-α to 17.66%, IFN-γ to 38.00%, and granzyme B to 23.64%.
Increased tumor-infiltrating CD3+CD4+ T cells from 0.79% to 5.25%.
Increased helper T (CD4+CD185+) cells from 7.63% to 18.18%.
Decreased immunosuppressive regulatory T (CD3+CD4+Foxp3+) cells from 18.83% to 8.60%.
Observed elevated CD3+CD8+ T cell infiltration in spleens, lymph nodes, and peripheral blood.
分子量

794.56

Formula

C25H28AuF6N2O2PS2
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

Necroptosis inducer 1 相关分类

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Keywords:

Necroptosis inducer 1Necroptosis inducer1Necroptosis inducer-1NecroptosisTrxRReactive Oxygen Species (ROS)Thioredoxin Reductasethioredoxin reductaseanti-PD-1 therapyCD8+ T cellsCD4+ helper T cellsreactive oxygen speciescolon carcinomanecroptosisimmunogenic cell deathregulatory T cellsCT-26 cellsInhibitorinhibitorinhibit

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