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) ).
Product Specifications
UNSPSC
12352005
Target
Histone Methyltransferase; PROTACs
Related Pathways
Epigenetics; PROTAC
Field of Research
Cancer
Smiles
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
Molecular Formula
C58H66ClF3N14O11S2
Molecular Weight
1291.81
References & Citations
[1]Yim H, et al. Discovery of the first-in-class DOT1L PROTAC degrader. Eur J Med Chem. 2025 Jul 5;291:117595.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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