Chemical Structure : MS1262
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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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.
分子量 | 511.71 | |
分子式 | C29H45N5O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Xie L, et al. medRxiv. 2023 Oct 26:2023.10.25.23297491.
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