PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies[1].
PR5-LL-CM01 has a range of IC50 at 2-4 μM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC50 at 10-11 μM in CRC cells (HT29, HCT116 and DLD1). PR5-LL-CM01 has higher efficacy to specifically inhibit cancer cells and demonstrated low toxicity in normal cells. PR5-LL-CM01 strongly inhibited colony forming ability in both PANC1 and HT29 cells[1].PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells[1].PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 cells[1].
PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[1].
[1]. Prabhu L, et al. Adapting AlphaLISA high throughput screen to discover a novel small-molecule inhibitor targeting protein arginine methyltransferase 5 in pancreatic and colorectal cancers. Oncotarget. 2017;8(25):39963-39977.