PRMT5-IN-58

PRMT5-IN-58 (compound 9u) (10 days) exhibits potent antiproliferative activity against HCT116 MTAP-deleted cells with an IC₅₀ of 13 nM and 70-fold selectivity over HCT116 MTAP wild-type cells^[1].
PRMT5-IN-58 exhibits potent and selective antiproliferative activity in multiple MTAP-deleted cancer cell lines (H1650, LU99, LN18, MIA PaCa-2), with IC₅₀ values ranging from < 1.5 to 51 nM, while showing minimal effect on MTAP wild-type H358 cells^[1].
PRMT5-IN-58 (4 days) selectively inhibits SDMA production in HCT116 MTAP-deleted cells with an IC₅₀ of 6.9 nM and exhibits 8-fold selectivity over HCT116 MTAP wild-type cells (IC₅₀ = 55.5 nM)^[1].
PRMT5-IN-58 significantly inhibits the PRMT5⋅MTA complex with an IC₅₀ of 11.7 nM^[1].
PRMT5-IN-58 binds to the PRMT5-MTA complex and forms key interactions with residues such as Phe327, Trp579, Glu444, Glu435, Phe580, and Thr323^[1].
PRMT5-IN-58 (10-100 nM; 7 days) selectively triggers apoptosis in MTAP-deleted Miapaca-2 and PSN-1 cells in a concentration-dependent manner, without affecting the cell cycle of MTAP wild-type HCT116 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.