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Chemical Structure : MS4322
CAS No.: 2375432-47-4
Catalog No.: PC-72471Not For Human Use, Lab Use Only.
MS4322 (MS-4322) is a potent, highly selective PRMT5 degrader (PROTAC) by linking the PRMT5 inhibitor EPZ015666 to a von Hippel-Lindau (VHL) E3 ligase ligand, with PRMT5 protein DC50 of 1.1 uM in MCF-7 cells.
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MS4322 (MS-4322) is a potent, highly selective PRMT5 degrader (PROTAC) by linking the PRMT5 inhibitor EPZ015666 to a von Hippel-Lindau (VHL) E3 ligase ligand, with PRMT5 protein DC50 of 1.1 uM in MCF-7 cells.
MS4322 effectively reduced PRMT5 protein levels in multiple cell lines, reduced the PRMT5 protein level in MCF7 cells in a concentration-, time-, VHL- and proteasome-dependent manner.
MS4322 inhibited cell growth at least as effectively as EPZ015666 in multiple cancer cell lines and exhibited good plasma exposure in a mouse pharmacokinetic (PK) study.
| M.Wt | 1101.32 | |
| Formula | C55H76N10O12S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-((S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-((1-((S)-19-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidine-1-carbonyl)-20,20-dimethyl-17-oxo-3,6,9,12,15-pentaoxa-18-azahenicosanoyl)azetidin-3-yl)amino)pyrimidine-4-carboxamide |
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1. Yudao Shen, et al. J Med Chem. 2020 Sep 10;63(17):9977-9989.
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