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 (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424))^[1].

1291.81

C₅₈H₆₆ClF₃N₁₄O₁₁S₂

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yim H, et al. Discovery of the first-in-class DOT1L PROTAC degrader. Eur J Med Chem. 2025 Jul 5;291:117595.  [Content Brief]