2601727-80-2

MS4322 is a potent PRMT5 degrader.

MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 ))[1].

VHL; Cereblon; MDM2; SMYD2; SMYD3; EHMTI PEP; SETD7/KMT7; PRMT4; PRMT8; EZH1; SETDB1/KMT2G; SETD8/KMT5A; PRMT5; EZH2; SUV39H2/KMT1B; SETD2/KMT3A; PRMT1; PRMT6; DOT1L; EHMT2/G9a/KMT1C; NSD2; PRMT3; PRMT7

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[1] Shen Y, et al. Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. J Med Chem. 2020 Sep 10;63(17):9977-9989. DOI:10.1021/acs.jmedchem.0c01111