PRMT5-MTA-IN-1 is a selective inhibitor of protein arginine methyltransferase PRMT5, targeting its enzymatic activity. This compound effectively inhibits the proliferation of colorectal cancer cells, including HCT116 wildtype and MTAP del mutant strains, with an IC50 of 16 nM and 2.47 μM, respectively. Additionally, PRMT5-MTA-IN-1 shows favorable liver microsomal stability and membrane permeability, indicating potential for in vivo applications. Its promising pharmacokinetic profile was observed in CD-1 mice, supporting further research into its therapeutic efficacy.
PRMT5-MTA-IN-1 is a selective inhibitor of protein arginine methyltransferase PRMT5, targeting its enzymatic activity. This compound effectively inhibits the proliferation of colorectal cancer cells, including HCT116 wildtype and MTAP del mutant strains, with an IC50 of 16 nM and 2.47 μM, respectively. Additionally, PRMT5-MTA-IN-1 shows favorable liver microsomal stability and membrane permeability, indicating potential for in vivo applications. Its promising pharmacokinetic profile was observed in CD-1 mice, supporting further research into its therapeutic efficacy.
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