Chemical Structure : MS152
CAS No.:
MS152
(MS 152, MS-152)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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385.51
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Formula
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C22H31N3O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)-4-(tetrahydro-2H-pyran-4-yl)quinolin-2-amine
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References
1. Wang SE, et al. Mol Ther. 2024 May 24:S1525-0016(24)00336-8.
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