CARM1-IN-1

Uses

CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity[1].

Biological Activity

Cell permeable: yes', 'Primary Target
PRMT4', 'Reversible: yes', 'Secondary Target
SET7', 'Target IC50: CARM1-mediated methylation over PRMT1 and SET7 (IC60 = 7.1, 63 and 943 μM,

IC 50

PRMT4

References

[1] Cheng D, et al. Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity. J Med Chem. 2011 Jul 14;54(13):4928-32. DOI:10.1021/jm200453n