MS33 is a highly effective degrader of the WDR5 protein, exhibiting Kd values of 870 nM and 120 nM for VCB and WDR5, respectively. It induces degradation of WDR5 through an E3 ligase VHL-mediated and proteasome-dependent mechanism. MS33 holds promise for furthering research in the field of acute myeloid leukemia.

WDR5:120 nM (Kd), VCB:870 nM (Kd)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[1]. Western Blot Analysis[1]Cell Line: MV4;11 cells Concentration: 0.05, 0.1, 0.5, 1, 5 μM Incubation Time: 1, 2, 4, 8, 16, 24 hours Result: Concentration- and time-dependently induced WDR5 degradation. The DC 50 of MS33 was 260 nM, and the maximum degradation of 71%.