MS8511
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
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- No. CAS: 2866408-21-9
- Fòrmula: C28H41N5O3
- Peso molecular:495.66
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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
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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G9a 100 nM (IC50) |
G9a 44 nM (Kd) |
GLP 140 nM (IC50) |
GLP 46 nM (Kd) |
MS8511 (Compound 8, 0-100 μΜ, 10 min) selectively inhibits G9a and GLP against other PKMTs and PRMTs, with IC50 values of 100 nM (G9a) and 140 nM (GLP)[1].
MS8511 (50 min) prefers covalent modification for G9a over GLP, with Kd values of 44 nM (G9a) and 46 nM (GLP)[1].
MS8511 (0-5 μM, 24-72 h) effectively reduces the H3K9me2 mark in MDA-MB-231 and K562 cellssup>[1].
MS8511 (0.8-25 μM, 3 days) inhibits the growth of MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, K562 cells.
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Concentration:0.2, 1, 5 μM.
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Incubation Time:24, 48, 72 h.
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Result:Reduced the H3K9me2 mark in a concentration- and time-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:0.8, 1.6, 3.1 6.3, 12.5, 25 μM.
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Incubation Time:3 days
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Result:Inhibited the growth of MDA-MB-231 cells.
Chemical Information
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No. CAS 2866408-21-9
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Appearance Solid
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Peso molecular 495.66
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Fòrmula C28H41N5O3
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Color White to off-white
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SMILES
COC1=CC(C(C=C1OCCCN2CCCC2)=NC(NC(C=C)=O)=C3)=C3NC4CCN(CC4)C(C)C
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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
Solvente y solubilidad
DMSO : 100 mg/mL (201.75 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 (5.04 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (5.04 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (273 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 |
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| DMSO | 1 mM | 2.0175 mL | 10.0876 mL | 20.1751 mL | 50.4378 mL |
| 5 mM | 0.4035 mL | 2.0175 mL | 4.0350 mL | 10.0876 mL | |
| 10 mM | 0.2018 mL | 1.0088 mL | 2.0175 mL | 5.0438 mL | |
| 15 mM | 0.1345 mL | 0.6725 mL | 1.3450 mL | 3.3625 mL | |
| 20 mM | 0.1009 mL | 0.5044 mL | 1.0088 mL | 2.5219 mL | |
| 25 mM | 0.0807 mL | 0.4035 mL | 0.8070 mL | 2.0175 mL | |
| 30 mM | 0.0673 mL | 0.3363 mL | 0.6725 mL | 1.6813 mL | |
| 40 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2609 mL | |
| 50 mM | 0.0404 mL | 0.2018 mL | 0.4035 mL | 1.0088 mL | |
| 60 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8406 mL | |
| 80 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
| 100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL |
MS8511 Related Classifications
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