MS2133

Chemical Structure : MS2133

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货号: PC-24355Not For Human Use, Lab Use Only.

MS2133 is a first-in-class, potent and selective DOT1L PROTAC degrader with a DC50 of 56 nM and Dmax of 69 in THP-1 cells and a DC50 of 25 nM and Dmax of 93 in MV4-11 cells.

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生物&药学活性

MS2133 is a first-in-class, potent and selective DOT1L PROTAC degrader with a DC50 of 56 nM and Dmax of 69 in THP-1 cells and a DC50 of 25 nM and Dmax of 93 in MV4-11 cells.
MS2133 potently induces DOT1L degradation in a concentration- and time-dependent manner, without affecting DOT1L mRNA expression.
The DOT1L degradation induced by MS2133 requires binding to the E3 ligase von Hippel-Lindau (VHL) and DOT1L and occurs through the ubiquitin-proteasome system.
MS2133 is selective for DOT1L over other methyltransferases.
MS2133 effectively inhibits the growth of mixed lineage leukemia-rearranged (MLL-r) leukemia cells (MV4-11 cells, GI50=212 nM) while having no toxicity on normal cells.

物理化学性质&存储条件

分子量	1291.82
分子式	C58H66ClF3N14O11S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2S,4R)-N-((S)-3-((6-(2-((4-amino-6-((2-(((S)-(3-chloropyridin-2-yl)(2,2-difluorobenzo[d] [1,3]dioxol-4-yl)methyl)amino)-5-sulfamoylphenyl)amino)-1,3,5-triazin-2-yl)oxy)acetamido)hexyl)amino)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide

参考文献

1. Yim H, et al. Eur J Med Chem. 2025 Apr 2;291:117595.

MS2133

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MS2133

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