EM12-FS
Based on 1 Customer Validation
EM12‑FS is a selective covalent molecular glue degrader of NTAQ1 that binds to CRBN with an IC50 of 256 nM. EM12‑FS covalently modifies the His353 residue of CRBN via chemical modification, reshapes the surface conformation of CRBN protein, selectively recruits NTAQ1 to form a ternary complex, and mediates the degradation of NTAQ1 protein in a CRL4CRBN E3 ubiquitin-proteasome pathway-dependent manner. EM12‑FS can be used in cancer-related research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.82%
- No. CAS: 2839138-44-0
- Fòrmula: C13H11FN2O6S
- Peso molecular:342.30
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
256 nM
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Cereblon engagement in human HEK293T cells measured by cellular cereblon engagement assay.
Cereblon engagement in human HEK293T cells measured by cellular cereblon engagement assay.
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d3cb00103b |
In Vitro
EM12-FS binds to cereblon in HEK293T cells with an IC50 of 256 nM; it covalently and specifically labels the His353 residue of recombinant CRBN in a cell-free biochemical system[1][2].
EM12-FS is a molecular glue degrader that selectively degrades the NTAQ1 protein in human leukemia cell lines MOLT4 and THP1[1][2].
EM12-FS exhibits high metabolic stability, with a half-life of 196 min in human plasma, >145 min in human liver microsomes, and >217 min in human hepatocytes[2].
EM12-FS (1-5 μM) mediates the degradation of endogenous and FLAG-tagged NTAQ1 in MOLT4 cells in a neddylation-dependent manner[2].
EM12-FS induces time-dependent dimerization of CRBN and NTAQ1 in a cell-free TR-FRET assay, and the degree of dimerization correlates with the level of covalent labeling of CRBN at the His353 site[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2839138-44-0
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Appearance Solid
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Peso molecular 342.30
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Fòrmula C13H11FN2O6S
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Color White to off-white
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SMILES
O=C1NC(C(CC1)N2C(C3=CC(OS(=O)(F)=O)=CC=C3C2)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (73.04 mM; ultrasonic and warming and heat to 60°C; 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)
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 (7.30 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.
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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 2.9214 mL | 14.6071 mL | 29.2141 mL | 73.0354 mL |
| 5 mM | 0.5843 mL | 2.9214 mL | 5.8428 mL | 14.6071 mL | |
| 10 mM | 0.2921 mL | 1.4607 mL | 2.9214 mL | 7.3035 mL | |
| 15 mM | 0.1948 mL | 0.9738 mL | 1.9476 mL | 4.8690 mL | |
| 20 mM | 0.1461 mL | 0.7304 mL | 1.4607 mL | 3.6518 mL | |
| 25 mM | 0.1169 mL | 0.5843 mL | 1.1686 mL | 2.9214 mL | |
| 30 mM | 0.0974 mL | 0.4869 mL | 0.9738 mL | 2.4345 mL | |
| 40 mM | 0.0730 mL | 0.3652 mL | 0.7304 mL | 1.8259 mL | |
| 50 mM | 0.0584 mL | 0.2921 mL | 0.5843 mL | 1.4607 mL | |
| 60 mM | 0.0487 mL | 0.2435 mL | 0.4869 mL | 1.2173 mL |
EM12-FS Related Classifications
HY-164891 Related Classifications
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