USP28-IN-3
Based on 1 Customer Validation
USP28-IN-3 is a USP28 inhibitor (IC50=0.1 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-3 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-3 also decreases the ankyrase-1/2 level in vitro. USP28-IN-3 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331).
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 : 98.26%
- CAS 番号: 2931509-14-5
- 分子式: C23H20Cl2N2O3S
- 分子量:475.39
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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DUB-IN-3Deubiquitinase Inhibitor -
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HBX 19818USP7 Inhibitor -
HY-16709
USP7-IN-1
生物活性
製品説明
IC50 & Target
[1]|
USP28 0.1 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
24.25 μM
Compound: 9o
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Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 3 days by SRB assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 3 days by SRB assay
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[PMID: 37075624] |
| LS174T | IC50 |
19.9 μM
Compound: 9o
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Antiproliferative activity against human LS174T cells assessed as cell growth inhibition incubated for 3 days by SRB assay
Antiproliferative activity against human LS174T cells assessed as cell growth inhibition incubated for 3 days by SRB assay
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[PMID: 37075624] |
体外実験
USP28-IN-3 (compound 9o) (10 μM, 15 μM; 3 d) inhibits colony formation of human colorectal cancer cells HCT116 (15 μM) and Ls174T (10 μM)[1].
USP28-IN-3 (20-80 μM; 24 h) down-regulates the level of c-Myc by enhancing its degradation via ubiquitin-proteasome system (UPS)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human colorectal cancer cells HCT116 and Ls174T
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Concentration:20 μM, 30 μM, 50 μM, and 60 μM, for Ls174T; 30 μM, 50 μM, 60 μM and 80 μM for HCT116
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Incubation Time:24 h
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Result:Dose-dependently down-regulated the cellular level of c-Myc.
化学情報
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CAS 番号 2931509-14-5
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性状 Solid
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分子量 475.39
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分子式 C23H20Cl2N2O3S
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Color White to off-white
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SMILES
CS(=O)(C1=CC=C(C(Cl)=C1)C(NC2=CC=C(C(C3=CC4=C(CNCC4)C=C3)=C2)Cl)=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
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (210.35 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)
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 (5.26 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.26 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
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データシート (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.1035 mL | 10.5177 mL | 21.0354 mL | 52.5884 mL |
| 5 mM | 0.4207 mL | 2.1035 mL | 4.2071 mL | 10.5177 mL | |
| 10 mM | 0.2104 mL | 1.0518 mL | 2.1035 mL | 5.2588 mL | |
| 15 mM | 0.1402 mL | 0.7012 mL | 1.4024 mL | 3.5059 mL | |
| 20 mM | 0.1052 mL | 0.5259 mL | 1.0518 mL | 2.6294 mL | |
| 25 mM | 0.0841 mL | 0.4207 mL | 0.8414 mL | 2.1035 mL | |
| 30 mM | 0.0701 mL | 0.3506 mL | 0.7012 mL | 1.7529 mL | |
| 40 mM | 0.0526 mL | 0.2629 mL | 0.5259 mL | 1.3147 mL | |
| 50 mM | 0.0421 mL | 0.2104 mL | 0.4207 mL | 1.0518 mL | |
| 60 mM | 0.0351 mL | 0.1753 mL | 0.3506 mL | 0.8765 mL | |
| 80 mM | 0.0263 mL | 0.1315 mL | 0.2629 mL | 0.6574 mL | |
| 100 mM | 0.0210 mL | 0.1052 mL | 0.2104 mL | 0.5259 mL |
USP28-IN-3 関連分類
HY-149229 関連分類
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