MS1262 TFA
MS1262 TFA 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 TFA reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 TFA 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 TFA reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 TFA reduces the risk of thrombus rupture. MS1262 TFA can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer.
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- 화학식: C31H46F3N5O5
- 분자량:625.72
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보관:
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
MS1262 TFA 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) TFA 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) TFA 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) TFA 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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Appearance Solid
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분자량 625.72
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화학식 C31H46F3N5O5
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SMILES
COC1=CC2=C(C=C1OCCCN3CCCC3)N=C(N4CCOCC4)C=C2NC5CCN(C(C)C)CC5.O=C(O)C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (159.82 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
References
[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 | 1.5982 mL | 7.9908 mL | 15.9816 mL | 39.9540 mL |
| 5 mM | 0.3196 mL | 1.5982 mL | 3.1963 mL | 7.9908 mL | |
| 10 mM | 0.1598 mL | 0.7991 mL | 1.5982 mL | 3.9954 mL | |
| 15 mM | 0.1065 mL | 0.5327 mL | 1.0654 mL | 2.6636 mL | |
| 20 mM | 0.0799 mL | 0.3995 mL | 0.7991 mL | 1.9977 mL | |
| 25 mM | 0.0639 mL | 0.3196 mL | 0.6393 mL | 1.5982 mL | |
| 30 mM | 0.0533 mL | 0.2664 mL | 0.5327 mL | 1.3318 mL | |
| 40 mM | 0.0400 mL | 0.1998 mL | 0.3995 mL | 0.9988 mL | |
| 50 mM | 0.0320 mL | 0.1598 mL | 0.3196 mL | 0.7991 mL | |
| 60 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6659 mL | |
| 80 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4994 mL | |
| 100 mM | 0.0160 mL | 0.0799 mL | 0.1598 mL | 0.3995 mL |
MS1262 TFA Related Classifications
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