Nrf2-IN-3
Based on 1 publication(s) in Google Scholar
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 .
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- 純度: 98.10%
- CAS 番号: 6325-13-9
- 分子式: C22H26N4O4S
- 分子量:442.53
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Nrf2-IN-3
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生物活性
Nrf2-IN-3 selectively sensitizes KEAP1-mutated cells, but not WT-KEAP1 cells, to Cisplatin (HY-17394) and Gefitinib (HY-50895) respectively [1].
Nrf2-IN-3 (24 h) selectively inhibits ARE-luc activity in KEAP1-mutated cells (A549, H1648, and H322 cells), with IC50s of 6.5 μM (A549), 7.3 μM (H1648), 5.7 μM (H322), respectively[1].
Nrf2-IN-3 (0-10 μM, 24 h) degrades NRF2 expression in A549, H1648, and H322 cells, which is mediated by the proteasome[1].
Nrf2-IN-3 binds KEAP1 mutants (G333C, G364C, and R460S mutants) and restores their capability to form mKEAP1/NRF2 complexes but has no effect on WT-KEAP1[1].
Nrf2-IN-3 (5, 10μM, 24 h) decreases NRF2 protein and increases reactive oxygen species (ROS) production in A549 (KEAP1 G333C mutation), but not A549 (WT-KEAP1) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549,H1648, H3229 cells
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Concentration:0-10 μM
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Incubation Time:72 h
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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
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Concentration:0,0.5, 1, 2, 5, 10 μM
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Incubation Time:24 h
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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.
体内実験Nrf2-IN-3 (110 mg/kg i.p. daily for 5 days per week for six weeks) inhibits tumor growth and selectively sensitizes mKEAP1 A549ctl xenograft to Cisplatin (HY-17394)[1].MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:110 mg/kg for Nrf2-IN-3 and 2 mg/kg for Cisplatin.
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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
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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.
化学情報
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CAS 番号 6325-13-9
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性状 Solid
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分子量 442.53
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分子式 C22H26N4O4S
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Color White to off-white
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SMILES
O=C(CCCSCCCC(N/N=C/C1=C(O)C=CC=C1)=O)N/N=C/C2=C(O)C=CC=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Exp Mol Med
Machine learning-based integration of transcriptome and digital pathology for predicting chemoresistance in muscle-invasive bladder cancer. [Abstract]2026 May;58(5):1589-1607. PMID: 42104016
溶剤 & 溶解度
体外:DMSO : 116.67 mg/mL (263.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
View the Complete Stock Solution Preparation TablePreparing Stock SolutionsView the Complete Stock Solution Preparation TableConcentration Solvent Mass1 mg5 mg10 mgConcentrationSolventMass1 mM2.2597 mL11.2987 mL22.5973 mL5 mM0.4519 mL2.2597 mL4.5195 mL10 mM0.2260 mL1.1299 mL2.2597 mLPlease refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
モル濃度計算機Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)= × ×希釈計算機濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
×=×
純度とドキュメンテーション
バッチを選択:純度: 99.98%Assay: 99.98%ee.: 99.98%-
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent Concentration Solvent Mass 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 
Nrf2-IN-3 関連分類
HY-149508 関連分類
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