EN450
Based on 1 Customer Validation
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
For research use only. We do not sell to patients.
- Purity: 98.59%
- CAS No.: 793719-01-4
- Formula: C11H13ClN2O3S
- Molecular Weight:288.76
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
EN450 (50 μM; 24 h) significantly inhibits the proliferation of HAP1 leukemia cancer cells and HEK293T cells, and significantly reduces the levels of the p105 and p50 subunits of the oncogenic transcription factor NFκB1[1].
EN450 (50 μM; 1 h) enhances the ubiquitination of NFκB1 mediated by UBE2D1 in the presence of the full CUL4A/RBX1/NEDD8 complex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HAP1 and HEK293T cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Significantly inhibited HAP1 cell proliferation.
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Cell Line:HAP1 and HEK293T cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Showed a significant reduction in the levels of NFκB1 p105 and p50 subunits.
Chemical Information
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CAS No. 793719-01-4
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Appearance Solid
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Molecular Weight 288.76
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Formula C11H13ClN2O3S
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Color White to off-white
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SMILES
O=C(NC1=CC(S(=O)(N(C)C)=O)=CC=C1Cl)C=C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (346.31 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. 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. 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 (8.66 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.66 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
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 (274 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Portuguese - PT (644 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. 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 | 3.4631 mL | 17.3154 mL | 34.6308 mL | 86.5771 mL |
| 5 mM | 0.6926 mL | 3.4631 mL | 6.9262 mL | 17.3154 mL | |
| 10 mM | 0.3463 mL | 1.7315 mL | 3.4631 mL | 8.6577 mL | |
| 15 mM | 0.2309 mL | 1.1544 mL | 2.3087 mL | 5.7718 mL | |
| 20 mM | 0.1732 mL | 0.8658 mL | 1.7315 mL | 4.3289 mL | |
| 25 mM | 0.1385 mL | 0.6926 mL | 1.3852 mL | 3.4631 mL | |
| 30 mM | 0.1154 mL | 0.5772 mL | 1.1544 mL | 2.8859 mL | |
| 40 mM | 0.0866 mL | 0.4329 mL | 0.8658 mL | 2.1644 mL | |
| 50 mM | 0.0693 mL | 0.3463 mL | 0.6926 mL | 1.7315 mL | |
| 60 mM | 0.0577 mL | 0.2886 mL | 0.5772 mL | 1.4430 mL | |
| 80 mM | 0.0433 mL | 0.2164 mL | 0.4329 mL | 1.0822 mL | |
| 100 mM | 0.0346 mL | 0.1732 mL | 0.3463 mL | 0.8658 mL |
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