Biological Activity |
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected[1][2]. IC50 & Target: IC50: 3.7 uM (mTh1 cells), 9.2 uM (mTh2 cells)IC50: 26.9 uM (hTh1 cells), 31.6 uM (hTh2 cells)[1] In Vitro: CMP-5 (0-100 uM; 24-72 hours) is selectively toxic to lymphoma cells, but shows a limited toxicity to normal resting B lymphocytes even after prolonged incubation[1].CMP-5 (40 uM; 24 hours) decreases p-BTK and pY(416)SRC expression in 60A cells when it compares to the DMSO-treated group[1].CMP-5 (0-40 uM; 24 hours) preferentially suppresses the proliferation of human Th1 cells over Th2 cells (43 versus 9% inhibition, respectively). The sensitivity of Th1 cells over Th2 cells to PRMT5 inhibition is different, the IC50 values are 26.9 uM and 31.6 uM in human Th1 cells and Th2 cells, respectively[1].CMP-5 (25 uM; 24 hours) alone inhibits mouse Th1 cell proliferation by 91%, when added different doses IL-2, IL-2 enhances proliferation and reaches a peak at 5 ng/ml[1]. |