PR5-LL-CM01 is a novel selective, small-molecule inhibitor of PRMT5 methyltransferase with IC50 of 7.5 uM.
PR5-LL-CM01 displays >10-fold selectivity over PRMT3, and no inhibitory activity over PRMT1/4/6/8.
PR5-LL-CM01 exhibits cell viability inhibition with IC50 of 2-4 uM in PDAC cells, IC50 of 10-11 uM in CRC cells, more potent than EPZ015666.
PR5-LL-CM01 significantly inhibits NF-κB activation in PDAC and CRC cells, and shows dramatic anti-tumor efficacy in vivo.
