CARM1-IN-1 is a potent and selective inhibitor of the histone methyltransferase CARM1, with an IC50 value of 8.6 μM and minimal activity against PRMT1 and SET7 (IC50 >667 μM). This compound effectively reduces the methylation activity of CARM1 on various substrates, including PABP1, CA150, SmB, and histone H3. Additionally, CARM1-IN-1 has been shown to suppress the promoter activity of prostate-specific antigen (PSA) while displaying low cytotoxicity, making it a valuable tool for studying epigenetic regulation and prostate cancer biology.
CARM1-IN-1 is a potent and selective inhibitor of the histone methyltransferase CARM1, with an IC50 value of 8.6 μM and minimal activity against PRMT1 and SET7 (IC50 >667 μM). This compound effectively reduces the methylation activity of CARM1 on various substrates, including PABP1, CA150, SmB, and histone H3. Additionally, CARM1-IN-1 has been shown to suppress the promoter activity of prostate-specific antigen (PSA) while displaying low cytotoxicity, making it a valuable tool for studying epigenetic regulation and prostate cancer biology.
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