BRD0639
Based on 1 publication(s) in Google Scholar
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.
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- Pureza: 98.04%
- No. CAS: 2760881-74-9
- Fòrmula: C21H22ClN5O4S
- Peso molecular:475.95
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Almacenamiento: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
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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
Publications Citing Use of MedChemExpress (MCE) BRD0639
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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PRMT5 |
BRD0639 is a first-in-class PBM-competitive small molecule that can support studies of PBM dependent PRMT5 activities and the development of novel PRMT5 inhibitors that selectively target these functions. BRD0639 can engage the cellular target and effectively outcompete binding between full-length PRMT5 and RIOK1 proteins with an IC50 of 7.5 uM and 16 uM in permeabilized and living cells, respectively. BRD0639 reduces SDMA in the same subset of proteins also affected by genetic perturbation of the PRMT5 binding motif (PBM) binding site[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2760881-74-9
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Appearance Solid
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Peso molecular 475.95
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Fòrmula C21H22ClN5O4S
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Color Light yellow to brown
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SMILES
C[C@H](N1C(C=C(Cl)C=N1)=O)C(NC2=CC=C(C)C(S(=O)(NCCC3=NC=CC=C3)=O)=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Biol Chem
Protein arginine methyltransferase 5 is essential for oncogene product EWSR1-ATF1-mediated gene transcription in clear cell sarcoma. [Abstract]2022 Oct;298(10):102434. PMID: 36041632
Solvente y solubilidad
DMSO : 250 mg/mL (525.27 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: ≥ 2.08 mg/mL (4.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureza y Documentación
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Ficha de datos (270 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 | 2.1011 mL | 10.5053 mL | 21.0106 mL | 52.5265 mL |
| 5 mM | 0.4202 mL | 2.1011 mL | 4.2021 mL | 10.5053 mL | |
| 10 mM | 0.2101 mL | 1.0505 mL | 2.1011 mL | 5.2527 mL | |
| 15 mM | 0.1401 mL | 0.7004 mL | 1.4007 mL | 3.5018 mL | |
| 20 mM | 0.1051 mL | 0.5253 mL | 1.0505 mL | 2.6263 mL | |
| 25 mM | 0.0840 mL | 0.4202 mL | 0.8404 mL | 2.1011 mL | |
| 30 mM | 0.0700 mL | 0.3502 mL | 0.7004 mL | 1.7509 mL | |
| 40 mM | 0.0525 mL | 0.2626 mL | 0.5253 mL | 1.3132 mL | |
| 50 mM | 0.0420 mL | 0.2101 mL | 0.4202 mL | 1.0505 mL | |
| 60 mM | 0.0350 mL | 0.1751 mL | 0.3502 mL | 0.8754 mL | |
| 80 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6566 mL | |
| 100 mM | 0.0210 mL | 0.1051 mL | 0.2101 mL | 0.5253 mL |
BRD0639 Related Classifications
HY-132309 Related Classifications
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