MS2133

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 ; Blue: E3 ligase VHL ligand (HY-47070) ; Black: Linker (HY-79577) ; E3 ligase VHL ligand-linker conjugate (HY-173424) ).

C58H66ClF3N14O11S2

1291.81

O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3)CC(NCCCCCCNC(COC5=NC(N)=NC(NC6=CC(S(=O)(N)=O)=CC=C6N[C@H](C7=NC=CC=C7Cl)C8=C9OC(F)(F)OC9=CC=C8)=N5)=O)=O

Histone Methyltransferase; PROTACs

Room temperature