2. PROTAC NF-κB Apoptosis
  3. PROTACs NF-κB Apoptosis
  4. JP-163-16

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: RelA/p65 Ligand (HY-174865); Blue: CRBN Ligand (HY-A0003); Black: Linker; CRBN Ligand+Linker (HY-160241)).

For research use only. We do not sell to patients.

JP-163-16

JP-163-16 Chemical Structure

CAS No. : 3100147-70-1

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JP-163-16 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

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Description

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: RelA/p65 Ligand (HY-174865); Blue: CRBN Ligand (HY-A0003); Black: Linker; CRBN Ligand+Linker (HY-160241))[1].

IC50 & Target[1]

Cereblon

 

p65

 

In Vitro

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.

JP-163-16 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.1-5 μM
Incubation Time: 48 h
Result: Significantly increased the apoptosis rate of cells.
Molecular Weight

777.86

Formula

C42H47N7O8
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2856 mL 6.4279 mL 12.8558 mL
5 mM 0.2571 mL 1.2856 mL 2.5712 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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
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JP-163-16 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JP-163-163100147-70-1PROTACsNF-κBApoptosisNuclear factor-κBNuclear factor-kappaBPROTACRelA/p65cancerapoptosisInhibitorinhibitorinhibit

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