MS152 | EHMT2/G9a inhibitor | Probechem Biochemicals

Chemical Structure : MS152

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MS152 (MS 152, MS-152)

货号: PC-22432Not For Human Use, Lab Use Only.

MS152 is a potent, selective and brain penetrant EHMT2/G9a inhibitor with biochemical IC50 of 126 nM/76 nM, respectively.

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生物&药学活性

MS152 is a potent, selective and brain penetrant EHMT2/G9a inhibitor with biochemical IC50 of 126 nM/76 nM, respectively.
MS152 dose-dependently reduced H3K9me2 levels at 48 hours in K562 cell line with EC50 of 60 nM, 5-fold more potent than UNC0642 (EC50=294 nM).
MS152 displayed excellent selectivity against 21 PKMTs and protein arginine methyltransferases (PRMTs), with no significant inhibition at 1 uM.
MS152 can efficiently reactivate the expression of paternally expressed genes from the maternal chromosome in PWS patient-derived fibroblasts.
MS152 is capable of reactivating the expression of maternal Snrpn-EGFP in mice.
MS152 treatment ameliorated the growth retardation and perinatal lethality in the PWS mouse model.

物理化学性质&存储条件

分子量	385.51
分子式	C22H31N3O3
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	6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)-4-(tetrahydro-2H-pyran-4-yl)quinolin-2-amine

参考文献

1. Wang SE, et al. Mol Ther. 2024 May 24:S1525-0016(24)00336-8.

MS152 (MS 152, MS-152)

生物&药学活性

物理化学性质&存储条件

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MS152 (MS 152, MS-152)

生物&药学活性

物理化学性质&存储条件

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