prmt4-in-1

PRMT4-IN-1 is a selective inhibitor of PRMT4, demonstrating an IC50 value of 3.2 nM, and has been shown to reduce the relative viability of MCF7 cells [1].

DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM, occupying the SAM binding pocket to exert its inhibitory effect. It effectively blocks cell proliferation in breast cancer, liver cancer, and acute myeloid leukemia cell lines.

TP-064 is a potent and selective PRMT4 inhibitor, featuring an IC50 < 10nM for methylation of H3 (1-25) and over 100-fold selectivity compared to other histone methyltransferases and non-epigenetic targets. It inhibits the methylation of MED12 in cells with an IC50 of 43 nM.

MS049 dihydrochloride is a selective and cell-active dual inhibitor of PRMT4 and PRMT6 (IC50=34/43 nM), capable of reducing Med12me2a and H3R2me2a levels in HEK293 cells.

PRMT4-IN-3 (compound 56) is a potent class I protein arginine methyltransferase (PRMT) inhibitor, specifically targeting PRMT4 with an IC50 of 37 nM, while exhibiting weaker inhibition of PRMT6 with an IC50 of 253 nM [1].

PRMT4-IN-2 (compound 55) acts as a pan-inhibitor across various protein arginine methyltransferase (PRMT) isoforms, exhibiting inhibitory potencies with IC50 values of 92 nM for PRMT4, 436 nM for PRMT6, 460 nM for PRMT1, 823 nM for PRMT8, and 1.386 μM for PRMT3 [1].