PROTAC BRD4 Degrader-1
Based on 1 Customer Validation
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
(Pink: BRD4 BD1 ligand (HY-150941); Blue: Cereblon ligand (HY-10984); Black: linker (HY-108369)).
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 2133360-00-4
- Formula: C40H37N9O8
- Molecular Weight:771.78
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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BRD4 (BD1) 41.8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
0.81 μM
Compound: 21
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Antiproliferative activity against human THP1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
Antiproliferative activity against human THP1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
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[PMID: 31813613] |
PROTAC BRD4 Degrader-1 (compound 21) (2.5 μM; 24 hours) shows high inhibitory activity against the growth of human monocyte lymphoma cell line THP-1, with the IC50 value of 0.81 μM, and moderate activity against Raji and HL-60 cell lines[1]. PROTAC BRD4 Degrader-1 (1 μM; 24 hours) effectively induces the degradation of BRD4 protein and suppression of c-Myc, while pomalidomide couldn’t degrade BRD4 at the low concentration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60, Raji and THP-1 cell
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Concentration:2.5 μM
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Incubation Time:24 hours
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Result:Inhibited HL-60, Raji and THP-1 cell growth.
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Cell Line:THP-1 cell
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Concentration:1 μM
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Incubation Time:3 hours
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Result:Degraded BRD4 protein and suppressed c-Myc expression.
Chemical Information
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CAS No. 2133360-00-4
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Appearance Solid
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Molecular Weight 771.78
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Formula C40H37N9O8
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)COCCN4N=NC(CN5C(N(C)C6=C(C=C(C7=C(C)ON=C7C)C=C6)C5C8=CC=CC=C8)=O)=C4
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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 (129.57 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)
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.
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 (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 |
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| DMSO | 1 mM | 1.2957 mL | 6.4785 mL | 12.9571 mL | 32.3926 mL |
| 5 mM | 0.2591 mL | 1.2957 mL | 2.5914 mL | 6.4785 mL | |
| 10 mM | 0.1296 mL | 0.6479 mL | 1.2957 mL | 3.2393 mL | |
| 15 mM | 0.0864 mL | 0.4319 mL | 0.8638 mL | 2.1595 mL | |
| 20 mM | 0.0648 mL | 0.3239 mL | 0.6479 mL | 1.6196 mL | |
| 25 mM | 0.0518 mL | 0.2591 mL | 0.5183 mL | 1.2957 mL | |
| 30 mM | 0.0432 mL | 0.2160 mL | 0.4319 mL | 1.0798 mL | |
| 40 mM | 0.0324 mL | 0.1620 mL | 0.3239 mL | 0.8098 mL | |
| 50 mM | 0.0259 mL | 0.1296 mL | 0.2591 mL | 0.6479 mL | |
| 60 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5399 mL | |
| 80 mM | 0.0162 mL | 0.0810 mL | 0.1620 mL | 0.4049 mL | |
| 100 mM | 0.0130 mL | 0.0648 mL | 0.1296 mL | 0.3239 mL |
PROTAC BRD4 Degrader-1 Related Classifications
HY-133131 Related Classifications
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