PRMT5-IN-50

PRMT5-IN-50 is an orally active selective inhibitor of PRMT5, demonstrating good metabolic stability and low clearance in human liver microsomes. It inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50 values for symmetric arginine methylation inhibition at 1.0 and 536 nM, respectively, and antiproliferative IC50 values at 19 and 1620 nM, respectively. Additionally, PRMT5-IN-50 suppresses tumor growth in mice.