EPZ015666 is a potent, selective, competitive PRMT5 inhibitor (IC50 = 22 nM). EPZ015666 exhibits >10,000-fold specificity for PRMT5 vs. other methyltransferases. EPZ015666 blocks the association of PRMT5 with methylosome protein 50 (WDR77), which is necessary to form an active methyltransferase complex. Treatment of MCL cell lines with nM concentrations of EPZ015666 leads to inhibition of SmD3 methylation and cell death."

PRMT5, HRMT1L5, IBP72, JBP1, SKB1, PRMT Protein

Stable at -20°C for up to two years. The solubility of this compound in DMSO is > 19.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.

1. Chan-Penebre E, Kuplast KG, Majer CR, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat Chem Biol, 2015, 11(6): 432-437.

Methyltransferase

Inhibitor