JP-163-16
Based on 1 Customer Validation
JP-163-16 is a RelA/p65 PROTAC degrader. JP-163-16 selectively reduces the expression of RelA/p65 in a proteasome-dependent manner in cells. JP-163-16 can induce cell apoptosis by inhibiting the NF-κB signaling pathway. JP-163-16 can be used for research on RelA/p65-dependent tumours, such as chronic lymphocytic leukaemia (CLL).
(Pink: p65 ligand (HY-174865); Blue: Cereblon ligand (HY-A0003); Black: linker).
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: 99.20%
- CAS 番号: 3100147-70-1
- 分子式: C42H47N7O8
- 分子量:777.86
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Help & FAQs
PROTACs 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
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Cereblon |
p65 |
JP-163-16 (Compound 15d) (3.16-3162 nM, 48 h) has significant cytotoxicity in MEC-1 (LC50 = 0.14 μM) and primary CLL (LC50 = 0.23 μM) cells[1].
JP-163-16 (3.16-3162 nM, 48 h) relies on the expression of cereblon to exert cytotoxic effects and has a weaker inhibitory effect in RPMI-8226 cells (LC50 = 0.68 μM)[1].
JP-163-16 (0.1-5 μM, 48 h) significantly inhibits the growth and induces apoptosis of MDA-MB-231 (LC50 = 2.9 μM) cells by degrading the level of RelA/p65 in a proteasome-dependent manner[1].
JP-163-16 (48 h) is less toxic in primary B-lymphocytes (LD50 = 19.1 μM) and T-lymphocytes (LD50 = 36.4 μM)[1].
JP-163-16 (0-1 μM, 24 h) selectively degrades the level of RelA/p65, with little impact on RelB and cRel in MEC-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.1-5 μM
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Incubation Time:48 h
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Result:Significantly increased the apoptosis rate of cells.
化学情報
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CAS 番号 3100147-70-1
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性状 Solid
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分子量 777.86
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分子式 C42H47N7O8
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Color White to off-white
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SMILES
O=C(NC1=CC=C(NC(CCCOC2=C(OC)C=C3C(N=C[C@@](CCC4)([H])N4C3=O)=C2)=O)C=C1)CCCCCNC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=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
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (128.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (stored under nitrogen). 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 (stored under nitrogen). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.21 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- 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 (stored under nitrogen). 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 | 1.2856 mL | 6.4279 mL | 12.8558 mL | 32.1395 mL |
| 5 mM | 0.2571 mL | 1.2856 mL | 2.5712 mL | 6.4279 mL | |
| 10 mM | 0.1286 mL | 0.6428 mL | 1.2856 mL | 3.2139 mL | |
| 15 mM | 0.0857 mL | 0.4285 mL | 0.8571 mL | 2.1426 mL | |
| 20 mM | 0.0643 mL | 0.3214 mL | 0.6428 mL | 1.6070 mL | |
| 25 mM | 0.0514 mL | 0.2571 mL | 0.5142 mL | 1.2856 mL | |
| 30 mM | 0.0429 mL | 0.2143 mL | 0.4285 mL | 1.0713 mL | |
| 40 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8035 mL | |
| 50 mM | 0.0257 mL | 0.1286 mL | 0.2571 mL | 0.6428 mL | |
| 60 mM | 0.0214 mL | 0.1071 mL | 0.2143 mL | 0.5357 mL | |
| 80 mM | 0.0161 mL | 0.0803 mL | 0.1607 mL | 0.4017 mL | |
| 100 mM | 0.0129 mL | 0.0643 mL | 0.1286 mL | 0.3214 mL |
JP-163-16 関連分類
HY-174864 関連分類
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