K67
Based on 1 publication(s) in Google Scholar
K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2.
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- 純度: 98.26%
- CAS 番号: 2046250-48-8
- 分子式: C29H30N2O7S2
- 分子量:582.69
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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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
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 K67
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生物活性
K67 (50 μM; 24-72 h) significantly inhibits the proliferation of Huh1 cells and Huh7 cells expressing phospho-mimetic p62 in cell viability assays1.
K67 (50 μM; 12-48 h) inhibits the expression of Nrf2 target genes in Huh1 cells1.
K67 (50 μM; 4-36 h respectively) significantly reduces the content of Nrf2 in the nucleus and cytoplasm of Huh1 cells and Keap1 accumulates in a time-dependent manner1.
K67 (50 μM; treated for 12 h) significantly inhibits the interaction between phosphorylated p62 and Keap1 and promotes the interaction between Nrf2 and Keap1 in immunoprecipitation assays in Huh1 cells1.
K67 (50 μM; treated for 4 h + 8 h (with the addition of the proteasome inhibitor lactacystin)) significantly promotes the ubiquitination of Nrf2 in Huh7 cells (expressing S351E)1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh1 cells
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Concentration:50 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Significantly inhibited the proliferation of Huh1 cells.
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Cell Line:Huh1 cells
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Concentration:50 μM
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Incubation Time:12 h, 24 h, 48 h
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Result:Inhibited the expression of Nrf2 target genes in Huh1 cells.
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Cell Line:Huh1 cells
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Concentration:50 μM
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Incubation Time:4 h, 12 h, 24 h, 36 h
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Result:Increased the content of Nrf2 in both nuclear and cytosolic fractions of Huh1 cells decreased significantly. Meanwhile, Keap1 accumulated in a time-dependent manner.
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Cell Line:Huh1 cells
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Concentration:50 μM
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Incubation Time:12 h
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Result:The interaction between phosphorylated p62 and Keap1 in Huh1 cells was significantly inhibited, while the interaction between Nrf2 and Keap1 was promoted.
化学情報
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CAS 番号 2046250-48-8
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性状 Solid
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分子量 582.69
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分子式 C29H30N2O7S2
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Color Off-white to light yellow
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SMILES
CC(CC1=CC(NS(C2=CC=C(C=C2)OCC)(=O)=O)=C3C=CC=CC3=C1NS(C4=CC=C(C=C4)OCC)(=O)=O)=O
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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 4°C 2 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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Adv Sci (Weinh)
2025 Apr;12(15):e2408763. PMID: 39985288
溶剤 & 溶解度
DMSO : 100 mg/mL (171.62 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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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取扱説明書 (2659 KB)
参考文献
[1]. Saito T, et al. p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming. Nat Commun. 2016 Jun 27;7:12030. [Content Brief]
[2]. Yasuda D, et al. Synthesis of Keap1-phosphorylated p62 and Keap1-Nrf2 protein-protein interaction inhibitors and their inhibitory activity. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5956-5959. [Content Brief]
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 | 1.7162 mL | 8.5809 mL | 17.1618 mL | 42.9045 mL |
| 5 mM | 0.3432 mL | 1.7162 mL | 3.4324 mL | 8.5809 mL | |
| 10 mM | 0.1716 mL | 0.8581 mL | 1.7162 mL | 4.2904 mL | |
| 15 mM | 0.1144 mL | 0.5721 mL | 1.1441 mL | 2.8603 mL | |
| 20 mM | 0.0858 mL | 0.4290 mL | 0.8581 mL | 2.1452 mL | |
| 25 mM | 0.0686 mL | 0.3432 mL | 0.6865 mL | 1.7162 mL | |
| 30 mM | 0.0572 mL | 0.2860 mL | 0.5721 mL | 1.4301 mL | |
| 40 mM | 0.0429 mL | 0.2145 mL | 0.4290 mL | 1.0726 mL | |
| 50 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8581 mL | |
| 60 mM | 0.0286 mL | 0.1430 mL | 0.2860 mL | 0.7151 mL | |
| 80 mM | 0.0215 mL | 0.1073 mL | 0.2145 mL | 0.5363 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1716 mL | 0.4290 mL |
K67 関連分類
HY-111126 関連分類
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