3070323-06-4
Chemical Structure
MS1262
- CAS No.: 3070323-06-4
- Formula:C29H45N5O3
- Molecular Weight:511.70
InChIKey: IGXWMDSNAGPQFL-UHFFFAOYSA-N
SMILES: COC1=CC2=C(C=C1OCCCN3CCCC3)N=C(N4CCOCC4)C=C2NC5CCN(C(C)C)CC5
Biological Activity: 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[1][2][3].
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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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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]
