MS33

Names

[ Name ]:
MS33

Biological Activity

[Description]:

MS33 is a potent WDR5 degrader, with Kds 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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Signaling Pathways >> PROTAC >> PROTAC

[Target]

VHL

WDR5:120 nM (Kd)

VCB:870 nM (Kd)

[In Vitro]

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 DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₆₄H₈₄F₃N₁₁O₇S

[ Molecular Weight ]:
1208.48

MS33

Names

Biological Activity

Chemical & Physical Properties

Related Compounds