USP10-IN-4
Based on 1 Customer Validation
USP10-IN-4 is a potent ubiquitin-specific protease 10 (USP10) inhibitor with an IC50 of 10.87 μM and a Kd of 365 nM. USP10-IN-4 effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the subsequent downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in HCC cells and inhibits the onset and progression of liver cancer. USP10-IN-4 can used for the study of hepatocellular carcinoma (HCC).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.70%
- 分子式: C28H26ClN3O3
- 分子量:487.98
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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
YAP アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
CDK4 |
体外実験
USP10-IN-4 (Compound LY-2) (0.1-10 μM) inhibits the proliferation of Huh-7 and Bel-7402 cells in a concentration-dependent manner with IC50s of 2.5 and 1.3 μM[1].
USP10-IN-4 (1-20 μM, 14 d) consistently inhibits Huh-7 cells colony formation[1].
USP10-IN-4 (5-40 μM, 24 h) induces apoptosis and G1 arrest in Huh-7 cells[1].
USP10-IN-4 (0-20 μM, 0-48 h) results in the decrease of YAP, p53, CDK4 and Cyclin B2 protein in Huh-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh-7 cells
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Concentration:5, 20 and 40 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells in the G1 phase from 45% to 68%.
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Cell Line:Huh-7 cells
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Concentration:0, 0.5, 1, 5, 10 and 20 μM
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Incubation Time:0, 6, 12, 24, 36, 48 h
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Result:Reduced the expression of YAP and p53 in a time- and concentration-dependent manner.
Reduced CDK4, and Cyclin B2 proteins.
化学情報
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性状 Solid
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分子量 487.98
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分子式 C28H26ClN3O3
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Color White to off-white
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SMILES
O=C(C(N(CC(NCCC1=CC=C(Cl)C=C1)=O)C2=C3C=CC(C)=C2)=CC3=O)NC4=CC=CC=C4C
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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
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (102.46 mM; ultrasonic and warming and heat to 60°C; 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)
体内:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
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.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (252 KB)
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- Portuguese - PT (252 KB)
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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 | 2.0493 mL | 10.2463 mL | 20.4926 mL | 51.2316 mL |
| 5 mM | 0.4099 mL | 2.0493 mL | 4.0985 mL | 10.2463 mL | |
| 10 mM | 0.2049 mL | 1.0246 mL | 2.0493 mL | 5.1232 mL | |
| 15 mM | 0.1366 mL | 0.6831 mL | 1.3662 mL | 3.4154 mL | |
| 20 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5616 mL | |
| 25 mM | 0.0820 mL | 0.4099 mL | 0.8197 mL | 2.0493 mL | |
| 30 mM | 0.0683 mL | 0.3415 mL | 0.6831 mL | 1.7077 mL | |
| 40 mM | 0.0512 mL | 0.2562 mL | 0.5123 mL | 1.2808 mL | |
| 50 mM | 0.0410 mL | 0.2049 mL | 0.4099 mL | 1.0246 mL | |
| 60 mM | 0.0342 mL | 0.1708 mL | 0.3415 mL | 0.8539 mL | |
| 80 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6404 mL | |
| 100 mM | 0.0205 mL | 0.1025 mL | 0.2049 mL | 0.5123 mL |