2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Keap1-Nrf2 Reactive Oxygen Species
  4. Nrf2-IN-3

Nrf2-IN-3 (化合物R16) 是一种小分子 Nrf2 抑制剂，增加活性氧 (reactive oxygen species) 产生。Nrf2-IN-3 选择性结合 KEAP1 突变体，并通过修复中断的 KEAP1/Nrf2 相互作用恢复其 Nrf2 抑制功能，导致细胞中蛋白酶体依赖的 Nrf2 降解。Nrf2-IN-3 使 KEAP1 突变的肿瘤细胞对顺铂 (HY-17394)、吉非替尼 (HY-50895) 和 KEAP1 G333C 突变的异种移植物对顺铂敏感。

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Nrf2-IN-3 Chemical Structure

Nrf2-IN-3 Chemical Structure

CAS No. : 6325-13-9

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10 mM * 1 mL in DMSO ￥2860
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5 mg ￥2600
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Nrf2-IN-3 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-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin [1].

体外研究
(In Vitro)

Nrf2-IN-3 (24小时) 选择性抑制 KEAP1 突变细胞 (A549、H1648和H322细胞) 中的 ARE-luc 活性，IC50s 分别为 6.5 μM (A549)、7.3 μM (H1648)、5.7 μM (H322)[1]。
Nrf2-IN-3 (0-10μM，24小时) 降解 A549、H1648 和 H322 细胞中 Nrf2 的表达，由蛋白酶体介导[1]。
Nrf2-IN-3 结合 KEAP1 突变体 (G333C、G364C 和 R460S 突变体) 并恢复其形成 mKEAP1/Nrf2 复合物的能力，但对 WT-KEAP1 没有影响[1]。
Nrf2-IN-3 (5，10μM，24小时) 降低了 A549(KEAP1 G333C 突变) 中 Nrf2 蛋白的表达并增加了活性氧 (ROS) 的产生，但对 A549 (WT-KEAP1) 细胞没有影响[1]。
Nrf2-IN-3 选择性地使 KEAP1 突变的 A549、H1648 或 H322 细胞对顺铂和吉非替尼敏感，但不使WT-KEAP1 细胞敏感[1]。

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

Nrf2-IN-3 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: A549,H1648, H3229 cells
Concentration: 0-10 μM
Incubation Time: 72 h
Result: The IC50 (µM) of Cisplatin and Gefitinib in the presence and absence of Nrf2-IN-3 for 72 h.
A549 (G33C) H1648 (G364C) H322 (R460S)
Cisplatin 0.81 1.33 4.6
Cisplatin + 0.1 µM Nrf2-IN-3 0.13 0.23 3.5
Cisplatin + 0.5 µM Nrf2-IN-3 0.07 0.17 0.9
Gefitinib 2.5 3.4 4.4
Gefitinib + 0.5 µM Nrf2-IN-3 0.36 0.67 0.92

Western Blot Analysis[1]

Cell Line: A549,H1648, H3229 cells
Concentration: 0,0.5, 1, 2, 5, 10 μM
Incubation Time: 24 h
Result: Resulted in a decrease of NRF2 protein, and cells co-exposure to Epoxomicin (HY-13821) (1 μM) and Nrf2-IN-3 (5 μM) restored NRF2 levels.
Had no effect on NRF2 mRNA levels at 5 and 10 μM.
Reduced the mRNA levels of NQO1 and GCLM, two target genes of NRF2.
体内研究
(In Vivo)

Nrf2-IN-3 3 (110 mg/kg i.p. 每周 5 天，6 周) 抑制肿瘤生长，并选择性地使 mKEAP1 A549ctl 异种移植物对顺铂敏感[1]。

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

Animal Model: Palpable tumors were generated by subcutaneous injection of a million A549ctl or A549(WT-KEAP1) cells in the flank of NOD-SCID mice[1].
Dosage: 110 mg/kg for Nrf2-IN-3 and 2 mg/kg for Cisplatin.
Administration: Combination of Cisplatin (2 mg/kg) and Nrf2-IN-3 (110 mg/kg). The treatment started on day 18 after subcutaneous injection of A549ctl cells. Mice were treated i.p. with R16 at 110 mg/kg daily for 5 consecutive days per week, Cisplatin at 2 mg/kg twice per week, or the combination of both, or the vehicle
Result: Combination of Cisplatin and Nrf2-IN-3 strongly inhibited the growth of A549ctl xenograft, while Cisplatin or Nrf2-IN-3 alone has no effect[1].
Cisplatin alone or in combination with Nrf2-IN-3 significantly inhibited the growth of A549(WT-KEAP1) xenograft, but Nrf2-IN-3 did not significantly enhance the efficacy of cisplatin against this WT-KEAP1 tumor[1].
Cisplatin alone caused slight, but significant, weight loss, Nrf2-IN-3 did not enhance Cisplatin toxicity.
Nrf2-IN-3 alone or in combination with Cisplatin significantly decreased the levels of the NRF2 protein in the A549ctl tumors but not in the A549 (WT-KEAP1) tumors.
分子量

442.53

Formula

C22H26N4O4S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 116.67 mg/mL (263.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2597 mL 11.2987 mL 22.5973 mL
5 mM 0.4519 mL 2.2597 mL 4.5195 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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动物溶解方案计算器
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工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Nrf2-IN-3 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2597 mL 11.2987 mL 22.5973 mL 56.4933 mL
5 mM 0.4519 mL 2.2597 mL 4.5195 mL 11.2987 mL
10 mM 0.2260 mL 1.1299 mL 2.2597 mL 5.6493 mL
15 mM 0.1506 mL 0.7532 mL 1.5065 mL 3.7662 mL
20 mM 0.1130 mL 0.5649 mL 1.1299 mL 2.8247 mL
25 mM 0.0904 mL 0.4519 mL 0.9039 mL 2.2597 mL
30 mM 0.0753 mL 0.3766 mL 0.7532 mL 1.8831 mL
40 mM 0.0565 mL 0.2825 mL 0.5649 mL 1.4123 mL
50 mM 0.0452 mL 0.2260 mL 0.4519 mL 1.1299 mL
60 mM 0.0377 mL 0.1883 mL 0.3766 mL 0.9416 mL
80 mM 0.0282 mL 0.1412 mL 0.2825 mL 0.7062 mL
100 mM 0.0226 mL 0.1130 mL 0.2260 mL 0.5649 mL
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:

Nrf2-IN-36325-13-9Keap1-Nrf2Reactive Oxygen SpeciesA549H1648H3229BT20H838drug-resistantKEAP1 mutationantitumorInhibitorinhibitorinhibit

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