MS1262
MS1262 is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC50 of 19 nM and a Kd of 74 nM against G9a, and an IC50 of 6 nM and a Kd of 19 nM against GLP. MS1262 reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 reduces the risk of thrombus rupture. MS1262 can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer.
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- CAS. Nr.: 3070323-06-4
- Formel: C29H45N5O3
- Molecular Weight:511.70
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
MS1262 is a highly potent inhibitor of purified G9a and GLP proteins, with IC50 values of 19 nM and 6 nM, respectively, and Kd values of 74 nM and 19 nM, respectively[1].
MS1262 (1 µM) exhibits excellent selectivity for G9a and GLP, with no significant inhibition of 21 other methyltransferases at 1 µM[1].
MS1262 (5-5000 nM; 48 h) reduces H3K9me2 levels in K562 cells in a concentration-dependent manner following 48 hours of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:5-5000 nM
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Incubation Time:48 h
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Result:Reduced H3K9me2 levels in a concentration-dependent manner.
Showed visible decreases at all tested concentrations compared to DMSO vehicle control.
MS1262 (1 mg/kg; i.p.; once every 3.5 days; 6 weeks) treatment fully restores cognitive and noncognitive functions to wild-type levels and reverses AD-associated proteomic and phosphoproteomic dysregulation in APPNLGF knock-in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5xFAD (C57BL/6J) (16-24 weeks old, both male and female, sex-matched; Alzheimer's disease transgenic model)[3]
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Dosage:1 mg/kg
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Administration:i.p.; once every 3.5 days; 6 weeks
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Result:Rescued spatial memory deficits, with discrimination ratio restored to wild-type levels (p < 0.0001).
Increased time spent in the open arms of the elevated zero maze, indicating reduced anxiety-like behavior.
Reduced time spent immobile in the forced swim test, indicating reduced depression-like behavior.
Left locomotion unaffected.
Increased frequency of spontaneous excitatory postsynaptic currents (sEPSCs) in dentate granule cells, with no change in sEPSC amplitude or intrinsic cellular properties.
Reversed AD-characteristic dysregulation of 9764 entities (1346 proteins, 8418 phosphosites; log2FC ±0.2, P < 0.05), including m6A RNA regulators, synaptic proteins, tau isoforms, and proteins involved in calcium signaling, CREB signaling, synaptogenesis, and CDK5 pathways.
Reversed AD-dysregulated expression of early-stage AD CSF biomarkers and proteins associated with blood coagulation pathways.
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Animal Model:APP NLGF (C57BL/6J-A^w-J/J) (16-24 weeks old, both male and female, sex-matched; Alzheimer's disease knock-in model)[3]
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Dosage:1 mg/kg
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Administration:i.p.; once every 3.5 days; 6 weeks
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Result:Rescued spatial memory deficits, with discrimination ratio restored to wild-type levels (p < 0.001).
Increased time spent in the center of the open field and time spent in the open arms of the elevated zero maze, indicating reduced anxiety-like behavior.
Reduced time spent immobile in the forced swim test, indicating reduced depression-like behavior.
Left locomotion unaffected.
Reversed AD-characteristic dysregulation of 6576 proteins and 13668 phosphosites, including m6A RNA regulators, synaptic proteins, and proteins involved in calcium signaling, CREB signaling, and opioid pathways.
Reversed AD-dysregulated expression of early-stage AD CSF biomarkers and proteins associated with blood coagulation pathways.
Chemical Information
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CAS. Nr. 3070323-06-4
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Appearance Solid
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Molecular Weight 511.70
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Formel C29H45N5O3
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Color White to off-white
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SMILES
COC1=CC2=C(C=C1OCCCN3CCCC3)N=C(N4CCOCC4)C=C2NC5CCN(C(C)C)CC5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (195.43 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (4.89 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 (4.89 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (279 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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Handling Instructions (2659 KB)
Verweise
[1]. Xie L, et al. Development of a brain-penetrant G9a methylase inhibitor to target Alzheimer's disease-associated proteopathology. Nature communications. 2025 May 07;16(1):4222. [Content Brief]
[2]. Deng Z, et al. Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation. Journal of medicinal chemistry. 2025 Apr 24;68(8):8634-8647. [Content Brief]
[3]. Chen X, et al. Novel brain-penetrant inhibitor of G9a methylase blocks Alzheimer's disease proteopathology for precision medication. Res Sq [Preprint]. 2023 Nov 21:rs.3.rs-2743792. doi: 10.21203/rs.3.rs-2743792/v1. Update in: Nat Commun. 2025 May 7;16(1):4222. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.9543 mL | 9.7714 mL | 19.5427 mL | 48.8568 mL |
| 5 mM | 0.3909 mL | 1.9543 mL | 3.9085 mL | 9.7714 mL | |
| 10 mM | 0.1954 mL | 0.9771 mL | 1.9543 mL | 4.8857 mL | |
| 15 mM | 0.1303 mL | 0.6514 mL | 1.3028 mL | 3.2571 mL | |
| 20 mM | 0.0977 mL | 0.4886 mL | 0.9771 mL | 2.4428 mL | |
| 25 mM | 0.0782 mL | 0.3909 mL | 0.7817 mL | 1.9543 mL | |
| 30 mM | 0.0651 mL | 0.3257 mL | 0.6514 mL | 1.6286 mL | |
| 40 mM | 0.0489 mL | 0.2443 mL | 0.4886 mL | 1.2214 mL | |
| 50 mM | 0.0391 mL | 0.1954 mL | 0.3909 mL | 0.9771 mL | |
| 60 mM | 0.0326 mL | 0.1629 mL | 0.3257 mL | 0.8143 mL | |
| 80 mM | 0.0244 mL | 0.1221 mL | 0.2443 mL | 0.6107 mL | |
| 100 mM | 0.0195 mL | 0.0977 mL | 0.1954 mL | 0.4886 mL |
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