SML3793

MS4322

≥95% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₅₅H₇₆N₁₀O₁₂S
• CAS Number: 2375432-47-4
• Molecular Weight: 1101.32
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Description

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable