| References: |
EPZ020411 is a potent inhibitor of PRMT6 in biochemical (IC50 = 10 nM) and cellular (IC50 = 600 nM) assays. EPZ020411 is selective against the related enzymes PRMT3, PRMT4, PRMT5, and PRMT7 in a biochemical assay, and relatively selective against PRMT1 and PRMT8. In biochemical (IC50s = 100 and 200 nM, respectively) and cellular assays (for PRMT1). Even though EPZ020411 is selective within the PRMT family, there is no information on other relevant human methyltransferases.EPZ020411 is not greatly selective for PRMT6 over PRMT1 or PRMT8 in vitro. PRMT6 is the only PRMT known to methylate the H3R2 position, and EPZ020411 can be used as a probe to assess the functionality of this post-translational modification. While this compound shows poor bioavailability following oral dosing (<5%), subcutaneous (SC) dosing results in significant plasma levels, making this compound suitable for in vivo studies of the H3R2 mark using SC dosing. |
