SML3793
MS4322
≥95% (HPLC)
别名:
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
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
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.
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Yudao Shen et al.
Journal of medicinal chemistry, 63(17), 9977-9989 (2020-08-14)
The aberrant expression of protein arginine methyltransferase 5 (PRMT5) has been associated with multiple cancers. Using the proteolysis targeting chimera technology, we discovered a first-in-class PRMT5 degrader 15 (MS4322). Here, we report the design, synthesis, and characterization of compound 15
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