CM112

Chemical Structure : CM112

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货号: PC-24375Not For Human Use, Lab Use Only.

CM112 is a potent, selective PRMT1 degrader designed by tethering adamantane to MS023 via a 5-PEG linker, has DC50 of 0.83 uM in MCF-7 cells.

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生物&药学活性

CM112 is a potent, selective PRMT1 degrader designed by tethering adamantane to MS023 via a 5-PEG linker, has DC50 of 0.83 uM in MCF-7 cells.
CM112 reduces PRMT1 level in a time-dependent manner.
Cotreatment with the proteasome inhibitor MG132 (0.1 μM or 1 μM) and CM112 (10 μM) effectively prevent the degradation of PRMT1 in MCF-7 cells, aligning with the proteasome-dependent mechanism of HyTDs.
CM112 induces the degradation of post-translational PRMT1 without impairing the processes of genetic transcription and translation.
CM112 is still a potent type I PRMTs (PRMT1/3/4/6) pan inhibitor with IC50 values ranging from 9 nM to 224 nM.
CM112 does not affect protein level of PRMT3/4/6.
CM112 suppressed the proliferation of MCF-7 and MDA-MB-231 cells.
CM112 reduces the stability of orphan receptor TR3, which is a binding partner of PRMT1.

物理化学性质&存储条件

分子量	711.95
分子式	C39H61N5O7
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	1-(2-((3r,5r, 7r)-adamantan-1-yl)acetamido)-N-(4-(4-(((2-aminoethyl) (methyl)amino)methyl)-1H-pyrrol-3-yl)phenyl)-3,6,9,12,15-pentaoxaoctadecan-18-amide

参考文献

1. Ma C, et al. Eur J Med Chem. 2025 Apr 14;291:117625.

CM112

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CM112

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