Chemical Structure : MS2133
CAS No.:
MS2133
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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1291.82
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Formula
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C58H66ClF3N14O11S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Yim H, et al. Eur J Med Chem. 2025 Apr 2;291:117595.
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