JP-163-16
Based on 1 Customer Validation
JP-163-16 is a NF-κB RelA/p65 PROTAC degrader that recruits CRBN. JP-163-16 selectively induces RelA/p65 degradation via the ubiquitin-proteasome pathway, exerts cytotoxicity and induces apoptosis in cancer cells, while showing low toxicity to non-malignant lymphocytes. JP-163-16 can be used for the research of chronic lymphocytic leukemia, triple-negative breast cancer and multiple myeloma.
(Pink: p65 and RelA ligand (HY-174865); Blue: Cereblon ligand (HY-A0003); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.20%
- No. CAS: 3100147-70-1
- Fòrmula: C42H47N7O8
- Peso molecular:777.86
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Almacenamiento:
-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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
p65 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MEC1 | LC50 |
0.14 μM
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Apoptosis induction in human MEC-1 chronic lymphocytic leukaemia cells assessed by FITC annexin V and 7-AAD staining followed by flow cytometry after 48 hrs of incubation.
Apoptosis induction in human MEC-1 chronic lymphocytic leukaemia cells assessed by FITC annexin V and 7-AAD staining followed by flow cytometry after 48 hrs of incubation.
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40443648 |
| RPMI-8226 | LC50 |
0.70 μM
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Apoptosis induction in human RPMI-8226 cereblon-deficient myeloma cells assessed by FITC annexin V and 7-AAD staining followed by flow cytometry after 48 hrs of incubation.
Apoptosis induction in human RPMI-8226 cereblon-deficient myeloma cells assessed by FITC annexin V and 7-AAD staining followed by flow cytometry after 48 hrs of incubation.
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40443648 |
| MDA-MB-231 | LC50 |
2.9 μM
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Apoptosis induction in human MDA-MB-231 triple-negative breast cancer cells assessed by FITC annexin V and 7-AAD staining followed by flow cytometry after 48 hrs of incubation.
Apoptosis induction in human MDA-MB-231 triple-negative breast cancer cells assessed by FITC annexin V and 7-AAD staining followed by flow cytometry after 48 hrs of incubation.
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40443648 |
In Vitro
JP-163-16 (compound 15d) (0.0625-1 μM; 48 h) potently induces apoptosis in MEC-1 chronic lymphocytic leukemia (CLL) cells, with an LC50 of 0.14 μM[1].
JP-163-16 (0.0625-1 μM; 48 h) exerts proapoptotic effects on MEC-1 chronic lymphocytic leukemia (CLL) cells, and this effect is proteasome-dependent[1].
JP-163-16 (0.0625-1 μM; 48 h) induces apoptosis in primary chronic lymphocytic leukemia (CLL) cells with an LC50 of 0.23 μM[1].
JP-163-16 (48 h) exhibits two orders of magnitude lower toxicity toward normal primary B lymphocytes (LD50: 19.1 μM) and T lymphocytes (LD50: 36.4 μM) than toward malignant chronic lymphocytic leukemia (CLL) cells[1].
JP-163-16 (10 nM-1 μM; 48 h) exhibits a five-fold reduction in cytotoxic potency in cereblon-deficient RPMI-8226 myeloma cells, with an LC50 of 0.70 μM, indicating that its activity is dependent on cereblon[1].
JP-163-16 (0.0625-1 μM; 48 h) induces apoptosis in MDA-MB-231 triple-negative breast cancer cells, with an LC50 of 2.9 μM[1].
JP-163-16 (0.0625-1 μM; 48 h) exerts proteasome-dependent proapoptotic effects on MDA-MB-231 triple-negative breast cancer cells[1].
JP-163-16 (10 μM) does not interact significantly with AT-rich DNA[1].
JP-163-16 (0.5-1 μM; 24 h) selectively depletes RelA/p65 expression in MEC-1 chronic lymphocytic leukemia (CLL) cells, with no persistent effect on RelB or cRel[1].
JP-163-16 (0.5-1 μM; 24 h) reduces the expression level of RelA/p65 in triple-negative breast cancer cells MDA-MB-231, and this effect is proteasome-dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MEC-1 chronic lymphocytic leukaemia cells
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Concentration:0.0625, 0.125, 0.25, 0.5, 1 μM
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Incubation Time:48 h
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Result:Induced dose-dependent apoptosis, with a mean LC50 value of 0.14 μM.
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Cell Line:MEC-1 CLL cells
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Concentration:0.0625, 0.125, 0.25, 0.5, 1 μM
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Incubation Time:48 h
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Result:Showed significantly reduced cytotoxicity when co-treated with proteasome inhibitor MG-132, with an increased mean LC50 value relative to JP-163-16 alone.
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Cell Line:RPMI-8226 cereblon-deficient myeloma cells
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Concentration:10, 100, 1000 nM
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Incubation Time:48 h
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Result:Showed a five-fold reduction in potency, with an LC50 of 0.70 μM (compared to 0.14 μM in MEC-1 cells).
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Research Protocol for Inflammation-related Diseases
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 3100147-70-1
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Appearance Solid
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Peso molecular 777.86
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
In Vitro:
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)
In Vivo:
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.
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. * 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.
Pureza y Documentación
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Ficha de datos (282 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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Instrucciones de manejo (2659 KB)
Referencias
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 Related Classifications
HY-174864 Related Classifications
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