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MS152

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

M.Wt 385.51
Formula C22H31N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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