LLY-283 is a potent and selective SAM-competitive PRMT5 inhibitor (IC50 = 20 nM against PRMT5-catalyzed methylation of an H4R3-derived peptide substrate) with greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. LLY-283 inhibits Smith (Sm) antigen SmBB′ methylation in MCF7 cells (IC50 = 25 nM; 3 days) and affects MDM4 splicing in A375 cells (IC50 = 40 nM; 3 days). The diastereomer LLY-284 is less potent in the biochemical assay and is an ideal control compound for cellular studies. For characterization details of LLY-283, please visit the LLY-283 probe summary
on the Structural Genomics Consortium (SGC) website.
LLY-284 is the negative control for the active probe, LLY-283. LLY-284 is available from Sigma. To learn more about and purchase LLY-284, click here
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc