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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-MS1262
MS1262

Chemical Structure : MS1262

CAS No.:

MS1262 (MS 1262)

货号: PC-21346Not For Human Use, Lab Use Only.

MS1262 is a highly potent, selective and brain-penetrant inhibitor of G9a/GLP methylase with IC50 of 19/6 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MS1262 is a highly potent, selective and brain-penetrant inhibitor of G9a/GLP methylase with IC50 of 19/6 nM, respectively.
MS1262 shows 23-fold and 37-fold higher potency than UNC0642.
MS1262 shows high binding affinities to G9a (Kd = 74 ± 10 nM) and GLP (Kd = 19 ± 5 nM) in isothermal titration calorimetry (ITC) assays.
MS1262 displays excellent selectivity for G9a and GLP over any of the 21 other methyltransferases tested.
MS1262 effectively reduces histone H3 lysine 9 dimethylation in cells in a concentrationdependent manner.
MS1262 restores both cognitive and noncognitive functions to healthy levels in multiple Alzheimer's disease (AD) mouse models.

物理化学性质&存储条件

分子量 511.71
分子式 C29H45N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(1-isopropylpiperidin-4-yl)-6-methoxy-2-morpholino-7-(3-(pyrrolidin-1-yl)propoxy)quinolin-4-amine

参考文献

1. Xie L, et al. medRxiv. 2023 Oct 26:2023.10.25.23297491.

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