PRMT5-IN-57

PRMT5-IN-57 (Compound 27; up to 20 μM; 10 days) exhibits potent antiproliferative activity against MTAP-null cancer cells, with IC₅₀ values of 6.4 nM (HCT116 MTAP-del), 5.0 nM (NCI-H1650), and 3.0 nM (SK-HEP-1), showing 102-, 392-, and 168-fold selectivity over their respective MTAP-WT counterparts ^[1].
PRMT5-IN-57 (10 min preincubation + 180 min reaction) shows potent PRMT5/MTA enzyme inhibition with an IC₅₀ of 8.39 nM in the MTase-Glo assay^[1].
PRMT5-IN-57 (3-6 nM; 4 days) reduces SDMA levels in MTAP-null cells (HCT116 MTAP-/-, NCI-H1650, and SK-HEP-1) while showing minimal effect on MTAP-WT cells (HCT116 WT, Calu-1, and HepG2) at the same concentrations, as determined by Western blot analysis^[1].
PRMT5-IN-57 (10 μM) shows no inhibitory effect on CYP3A4-midazolam and CYP3A4-testosterone in human liver microsomes^[1].
PRMT5-IN-57 (IC₅₀10 μM) exhibits minimal inhibition of the hERG potassium channel in the Predictor^TM hERG Fluorescence Polarization Assay^[1].
PRMT5-IN-57 demonstrates high metabolic stability in mouse, rat, and human liver microsomes, with half-lives (T_1/2) of 38.5 min, 39.1 min, and 49.6 min, respectively^[1].

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