MS117
Based on 1 Customer Validation
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.
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- Purity: 98.0%
- CAS No.: 2702280-86-0
- 화학식: C17H22N4O
- 분자량:298.38
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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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT6 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.3 μM
Compound: 4; MS117
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Inhibition of Flag-tagged PRMT6 (unknown origin) expressed in HEK293 cells incubated for 20 hrs assessed as reduction in H3R2me2a levels
Inhibition of Flag-tagged PRMT6 (unknown origin) expressed in HEK293 cells incubated for 20 hrs assessed as reduction in H3R2me2a levels
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[PMID: 32367723] |
| MCF7 | IC50 |
5.6 μM
Compound: 4; MS117
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Inhibition of PRMT1 in human MCF7 cells assessed as reduction in H4R3me2a levels incubated for 2 days by fluorescence based assay
Inhibition of PRMT1 in human MCF7 cells assessed as reduction in H4R3me2a levels incubated for 2 days by fluorescence based assay
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[PMID: 32367723] |
MS117 (Compound 4) inhibits the PRMT6 methyltransferase activity in a time-dependent manner[1].
MS117 (Compound 4) shows moderate selectivity (6-fold) for PRMT6 over PRMT1 (IC50 = 0.1 ± 0.025 μM) and PRMT8 (IC50 = 0.11 ± 0.01 μM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2702280-86-0
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Appearance Solid
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분자량 298.38
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화학식 C17H22N4O
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Color Light brown to brown
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SMILES
NCCN(C)CC1=CNC=C1C2=CC=CC(NC(C=C)=O)=C2
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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
용액&용해도
DMSO : 100 mg/mL (335.14 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, 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.
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.
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 (8.38 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 (8.38 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.
순도&문서
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Data Sheet (274 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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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 | 1 mM | 3.3514 mL | 16.7572 mL | 33.5143 mL | 83.7858 mL |
| 5 mM | 0.6703 mL | 3.3514 mL | 6.7029 mL | 16.7572 mL | |
| 10 mM | 0.3351 mL | 1.6757 mL | 3.3514 mL | 8.3786 mL | |
| 15 mM | 0.2234 mL | 1.1171 mL | 2.2343 mL | 5.5857 mL | |
| 20 mM | 0.1676 mL | 0.8379 mL | 1.6757 mL | 4.1893 mL | |
| 25 mM | 0.1341 mL | 0.6703 mL | 1.3406 mL | 3.3514 mL | |
| 30 mM | 0.1117 mL | 0.5586 mL | 1.1171 mL | 2.7929 mL | |
| 40 mM | 0.0838 mL | 0.4189 mL | 0.8379 mL | 2.0946 mL | |
| 50 mM | 0.0670 mL | 0.3351 mL | 0.6703 mL | 1.6757 mL | |
| 60 mM | 0.0559 mL | 0.2793 mL | 0.5586 mL | 1.3964 mL | |
| 80 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0473 mL | |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3351 mL | 0.8379 mL |
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