MS049
Based on 1 publication(s) in Google Scholar
MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
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- Purity: 98.0%
- CAS No.: 1502816-23-0
- 화학식: C15H24N2O
- 분자량:248.36
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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- References
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Publications Citing Use of MedChemExpress (MCE) MS049
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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PRMT4 34 nM () |
PRMT6 43 nM () |
PRMT8 1600 nM () |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.97 μM
Compound: 17; MS049
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Inhibition of wild-type FLAG-tagged PRMT6 (unknown origin) expressed in HEK293 cells assessed as reduction in H3R2me2a level measured after 20 hrs by western blot analysis
Inhibition of wild-type FLAG-tagged PRMT6 (unknown origin) expressed in HEK293 cells assessed as reduction in H3R2me2a level measured after 20 hrs by western blot analysis
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[PMID: 27584694] |
| HEK293 | IC50 |
1.4 μM
Compound: 17; MS049
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Inhibition of PRMT4 in HEK293 cells assessed as reduction in Med12-Rme2a level measured after 72 hrs by western blot analysis
Inhibition of PRMT4 in HEK293 cells assessed as reduction in Med12-Rme2a level measured after 72 hrs by western blot analysis
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[PMID: 27584694] |
| MT4 | IC50 |
34 nM
Compound: 17; MS049
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Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with protein followed by addition of biotin labeled histone H3 (1 to 25) peptide as substrate and [3H]-SAM measur
Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with protein followed by addition of biotin labeled histone H3 (1 to 25) peptide as substrate and [3H]-SAM measur
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[PMID: 27584694] |
MS049 (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM)[1].
MS049 (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells[1].
MS049 is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:20 hours
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Result:Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM).
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Cell Line:HEK293 cells
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Concentration:0.1, 1, 10, 100 μM
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Incubation Time:72 hours
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Result:Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells.
Chemical Information
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CAS No. 1502816-23-0
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Appearance Solid
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분자량 248.36
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화학식 C15H24N2O
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Color Light yellow to yellow
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SMILES
CNCCN1CCC(OCC2=CC=CC=C2)CC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175
용액&용해도
H2O : ≥ 100 mg/mL (402.64 mM)
DMSO : ≥ 31 mg/mL (124.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (10.07 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 (10.07 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (402.64 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (270 KB)
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SDS (479 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.0264 mL | 20.1321 mL | 40.2641 mL | 100.6603 mL |
| 5 mM | 0.8053 mL | 4.0264 mL | 8.0528 mL | 20.1321 mL | |
| 10 mM | 0.4026 mL | 2.0132 mL | 4.0264 mL | 10.0660 mL | |
| 15 mM | 0.2684 mL | 1.3421 mL | 2.6843 mL | 6.7107 mL | |
| 20 mM | 0.2013 mL | 1.0066 mL | 2.0132 mL | 5.0330 mL | |
| 25 mM | 0.1611 mL | 0.8053 mL | 1.6106 mL | 4.0264 mL | |
| 30 mM | 0.1342 mL | 0.6711 mL | 1.3421 mL | 3.3553 mL | |
| 40 mM | 0.1007 mL | 0.5033 mL | 1.0066 mL | 2.5165 mL | |
| 50 mM | 0.0805 mL | 0.4026 mL | 0.8053 mL | 2.0132 mL | |
| 60 mM | 0.0671 mL | 0.3355 mL | 0.6711 mL | 1.6777 mL | |
| 80 mM | 0.0503 mL | 0.2517 mL | 0.5033 mL | 1.2583 mL | |
| 100 mM | 0.0403 mL | 0.2013 mL | 0.4026 mL | 1.0066 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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