MS4322
Based on 1 publication(s) in Google Scholar
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
(Pink: Histone Methyltransferase ligand (HY-173092); Blue: VHL ligand (HY-112078); Black: linker (HY-124780)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.14%
- No. CAS: 2375432-47-4
- Fòrmula: C55H76N10O12S
- Peso molecular:1101.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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
Publications Citing Use of MedChemExpress (MCE) MS4322
MoreVer todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
(Pink: Histone Methyltransferase ligand (HY-173092); Blue: VHL ligand (HY-112078); Black: linker (HY-124780)).
|
VHL |
Cereblon |
MDM2 |
SMYD2 |
SMYD3 |
EHMT1/GLP/KMT1D |
SETD7/KMT7 |
PRMT4 |
PRMT8 |
EZH1 |
SETDB1/KMT2G |
SETD8/KMT5A |
PRMT5 |
EZH2 |
SUV39H2/KMT1B |
SETD2/KMT3A |
PRMT1 |
PRMT6 |
DOT1L |
EHMT2/G9a/KMT1C |
NSD2 |
PRMT3 |
PRMT7 |
MS4322 (0.05-5 μM, 6 days) effectively reduces the PRMT5 protein level in a concentration dependent manner, with a Dmax of 74 % in MCF-7 cells[1].
MS4322 (5 μM, 7 days) degrades the PRMT5 protein through a PRMT5-, VHL-, and proteasome-dependent mechanism in MCF-7 cells[1].
MS4322 (0.1-10 μM, 6 days) exhibits antiproliferative effect mainly because of its PRMT5 degradation activity but not its PRMT5 inhibitory activity in MCF-7 cells[1].
MS4322 (5 μM, 6 days) also effectively reduces the PRMT5 protein level and inhibits growth in multiple cancer cell lines (HeLa, A549, A172, and Jurkat cells)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, HeLa, A549, A172, Jurkat cells
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Concentration:0.1, 0.3, 1, 3, 10 μM
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Incubation Time:6 days
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Result:Potently inhibited MCF-7 cell proliferation in a concentration-dependent manner.
Inhibited HeLa, A549, A172, Jurkat cells proliferation.
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Cell Line:MCF-7 cells
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Concentration:0.05-5 μM(6 days); 5 μM (0-8 days); 0-3 μM(6 days); 5 μM (7 days); 5 μM (6 days)
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Incubation Time:6 days; 0-8 days; 7 days;
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Result:Reduced the PRMT5 protein level (0.05-5 μM, 6 days).
Reduced the PRMT5 protein level in a time-dependent manner (5 μM, 0-8 days).
Inhibited SDMA(0-3 μM,6 days).
Reduced the PRMT5 protein level in MCF-7 cells in a PRMT5-, E3 ligase VHL-, and proteasome-dependent manner (5 μM, 7 days).
PRMT5 degradation was reversible (5 μM, 6 days).
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Cell Line:HeLa, A549, A172, Jurkat cells
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Concentration:5 μM
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Incubation Time:6 days
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Result:Significantly reduced PRMT5 protein levels in Hela (cervical cancer), A549 (lung adenocarcinoma), A172 (GBM), and Jurkat (leukemia) cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2375432-47-4
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Appearance Solid
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Peso molecular 1101.32
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Fòrmula C55H76N10O12S
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Color White to light yellow
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SMILES
O=C(C1=NC=NC(NC2CN(C(COCCOCCOCCOCCOCC(N[C@H](C(N3[C@H](C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)C[C@@H](O)C3)=O)C(C)(C)C)=O)=O)C2)=C1)NC[C@H](O)CN6CC7=C(C=CC=C7)CC6
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Synonyms
YS43-22
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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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Cancer Res Commun
PRMT5 Inhibitors Regulate DNA Damage Repair Pathways in Cancer Cells and Improve Response to PARP Inhibition and Chemotherapies. [Abstract]2023 Nov 6;3(11):2233-2243. PMID: 37861290
Solvente y solubilidad
DMSO : 100 mg/mL (90.80 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 (2.27 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.27 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 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 (276 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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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 |
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| DMSO | 1 mM | 0.9080 mL | 4.5400 mL | 9.0800 mL | 22.7000 mL |
| 5 mM | 0.1816 mL | 0.9080 mL | 1.8160 mL | 4.5400 mL | |
| 10 mM | 0.0908 mL | 0.4540 mL | 0.9080 mL | 2.2700 mL | |
| 15 mM | 0.0605 mL | 0.3027 mL | 0.6053 mL | 1.5133 mL | |
| 20 mM | 0.0454 mL | 0.2270 mL | 0.4540 mL | 1.1350 mL | |
| 25 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9080 mL | |
| 30 mM | 0.0303 mL | 0.1513 mL | 0.3027 mL | 0.7567 mL | |
| 40 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5675 mL | |
| 50 mM | 0.0182 mL | 0.0908 mL | 0.1816 mL | 0.4540 mL | |
| 60 mM | 0.0151 mL | 0.0757 mL | 0.1513 mL | 0.3783 mL | |
| 80 mM | 0.0114 mL | 0.0568 mL | 0.1135 mL | 0.2838 mL |
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