NF-κB p105 degrader-1
Based on 1 publication(s) in Google Scholar
NF-κB p105 degrader-1 is a non-covalent, selective Molecular glue-like degrader targeting the NF-κB p105 subunit. NF-κB p105 degrader-1 induces proteasome-mediated degradation via the Cullin-RING ligase SCFβTrCP. NF-κB p105 degrader-1 inhibits LPS-induced production of NO and TNF-α. NF-κB p105 degrader-1 can be used in inflammation-related research.
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- Pureté : 99.92%
- Formule: C21H18O4
- Masse moléculaire:334.37
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NF-κB p105 degrader-1
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Activité biologique
Description
IC50 & Target
[1]|
p105 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
5.40 μM
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Inhibition of LPS-induced nitric oxide production in murine macrophage RAW 264.7 cells.
Inhibition of LPS-induced nitric oxide production in murine macrophage RAW 264.7 cells.
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40378174 |
| RAW264.7 | IC50 |
2.02 μM
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Inhibition of LPS-induced tumor necrosis factor-α production in murine macrophage RAW 264.7 cells.
Inhibition of LPS-induced tumor necrosis factor-α production in murine macrophage RAW 264.7 cells.
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40378174 |
In Vitro
NF-κB p105 degrader-1 (Compound MD-1) (0.1-10 μM; 1-50 μM) potently inhibits LPS-induced NO and TNF-α production in RAW 264.7 cells with IC50 values of 5.40 μM and 2.02 μM, respectively, and is non-cytotoxic at concentrations up to 20 μM[1].
NF-κB p105 degrader-1 (1-10 μM) selectively suppresses LPS-induced NF-κB p65 phosphorylation in RAW 264.7 cells, with no significant impact on MAPK pathway kinase phosphorylation[1].
NF-κB p105 degrader-1 (1-10 μM; 24 h) induces proteasome-mediated degradation of NF-κB1 p105 and its processed p50 subunit in RAW 264.7 cells without affecting p100 or p52 levels, and does not regulate p105 at the transcriptional level[1].
NF-κB p105 degrader-1 (10 μM; 24 h) requires the SCFβTrCP E3 ubiquitin ligase for induced degradation of NF-κB1 p105 and p50 in RAW 264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine macrophage RAW 264.7 cells
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Concentration:10 μM
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Incubation Time:24 h (MD-1 treatment post 24 h siRNA transfection)
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Result:Stimulated p105 and p50 degradation in control siRNA-transfected cells, but this degradation was completely abrogated in βTrCP knockdown cells.
Chemical Information
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Appearance Solid
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Masse moléculaire 334.37
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Formule C21H18O4
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Color Off-white to light yellow
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SMILES
O=C1OC2=C(C=C(C=C2C=C1C3=CC=CC=C3)OC)C(/C=C(C)\C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Food Chem Toxicol
Polystyrene microplastics drive chondrotoxicity in osteoarthritis through inducing ER stress and apoptosis via NFKB1 activation. [Abstract]2026 Sep:215:116166. PMID: 42162659
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (299.07 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 (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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.48 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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. * 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.
Pureté et documentation
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Fiche technique (291 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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Instruction de manipulation (2659 KB)
Références
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 | 2.9907 mL | 14.9535 mL | 29.9070 mL | 74.7675 mL |
| 5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL | 14.9535 mL | |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9907 mL | 7.4767 mL | |
| 15 mM | 0.1994 mL | 0.9969 mL | 1.9938 mL | 4.9845 mL | |
| 20 mM | 0.1495 mL | 0.7477 mL | 1.4953 mL | 3.7384 mL | |
| 25 mM | 0.1196 mL | 0.5981 mL | 1.1963 mL | 2.9907 mL | |
| 30 mM | 0.0997 mL | 0.4984 mL | 0.9969 mL | 2.4922 mL | |
| 40 mM | 0.0748 mL | 0.3738 mL | 0.7477 mL | 1.8692 mL | |
| 50 mM | 0.0598 mL | 0.2991 mL | 0.5981 mL | 1.4953 mL | |
| 60 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2461 mL | |
| 80 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9346 mL | |
| 100 mM | 0.0299 mL | 0.1495 mL | 0.2991 mL | 0.7477 mL |
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