MS33 is a potent WDR5 degrader, with K d s of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia [1] [2] [3]. (Pink: WDR5 ligand; Blue: VHL ligand; Black: linker).
In Vitro, MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[1].
References:
[1]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.
In Vitro, MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[1].
References:
[1]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.