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).
For research use only. We do not sell to patients.
- Purity: 99.20%
- CAS No.: 3100147-70-1
- Formula: C42H47N7O8
- Molecular Weight:777.86
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Storage:
-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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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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.
Chemical Information
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CAS No. 3100147-70-1
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Appearance Solid
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Molecular Weight 777.86
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 |
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| 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 Related Classifications
HY-174864 Related Classifications
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