MS4322，25MG，SML3793-25MG，Sigma

Biochem/physiol Actions

Potent, cell-permeable, highly selective and yet a slow PRMT5 degrader.

MS4322 is a potent, cell-permeable, highly selective and yet a slow PRMT5 (protein arginine methyltransferase 5) degrader. It comprises of PRMT5 inhibitor EPZ015666 linked to a von Hippel-Lindau (VHL) E3 ligase ligand (S,R,S)-AHPC-Me (VHL-2). MS4322 reduces PRMT5 protein levels in a concentration-, time-, VHL- and proteasome-dependent manner. Inhibits PRMT5 activity (IC50 = 18 nM) and reduces arginine symmetric dimethylation (SDMA) levels. MS4322 displays good plasma exposure in a mouse PK study and in vivo availability.