Catalog No.: PC-24610Not For Human Use, Lab Use Only.
AM-9934 is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of12 nM for PRMT5 methyltransferase activity and 40 nM for PRMT5:MEP50 enzymatic affinity, selectively inhibits PRMT5 in MTAP-deleted cells.
AM-9934 is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of12 nM for PRMT5 methyltransferase activity and 40 nM for PRMT5:MEP50 enzymatic affinity, selectively inhibits PRMT5 in MTAP-deleted cells.
AM-9934 has Kd of 55 nM in the presence of MTA using microscale thermophoresis (MST), with much weaker to either the apo enzyme or the SIN-bound enzyme (>10 uM).
AM-9934 is highly selective for MTA-bound PRMT5.
AM-9934 is selective against a broad panel of arginine-, lysine-, and DNA-methyltransferases.
AM-9934 shows enhanced potency in the MTAP-deleted line (IC50 of 9.2 nM) and only weakly reduced SDMA in parental HCT116 cells (IC50 of 143 nM).
AM-9934 inhibits cell viability more potently against MTAP-deleted cells (IC50 of 0.16 µM vs. 4.1 µM in parental cells.
AM-9934 suppresses SDMA levels in MTAP-deleted tumors.
