MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423), Blue: E3 ligase VHL ligand (HY-47070), Black: Linker (HY-79577), E3 ligase VHL ligand-linker conjugate (HY-173424))[1].
Molecular Weight:
1291.81
Formula:
C58H66ClF3N14O11S2
Target:
Histone Methyltransferase,PROTACs
Application Notes:
MCE Product type: Reference compound
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