Biologically Active Small Molecules

A potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.

A potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6 IC₅₀ = 10 nM) that less potently targets PRMT1 and PRMT8 (IC₅₀s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6 IC₅₀ = 10 nM) that less potently targets PRMT1 and PRMT8 (IC₅₀s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6 IC₅₀ = 10 nM) that less potently targets PRMT1 and PRMT8 (IC₅₀s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6 IC₅₀ = 10 nM) that less potently targets PRMT1 and PRMT8 (IC₅₀s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6

A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) inhibits the H3K79 methylation in various human leukemia cell lines (IC₅₀s = 3-5 nM), decreasing MLL-fusion target gene expression and

A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) inhibits the H3K79 methylation in various human leukemia cell lines (IC₅₀s = 3-5 nM), decreasing MLL-fusion target gene expression and

A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) inhibits the H3K79 methylation in various human leukemia cell lines (IC₅₀s = 3-5 nM), decreasing MLL-fusion target gene expression and

A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) inhibits the H3K79 methylation in various human leukemia cell lines (IC₅₀s = 3-5 nM), decreasing MLL-fusion target gene expression and

An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM) blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC₅₀s range from 2-90 nM) induces apoptosis and differentiation specifically in SMARCB1-deleted

An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM) blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC₅₀s range from 2-90 nM) induces apoptosis and differentiation specifically in SMARCB1-deleted