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WDR5-C47 is a highly potent and selective antagonist of WDR5-MLL interaction with an IC₅₀ ~0.3 µM. It was designed based on the structure of the WDR5-MLL complex. The WD40-repeat protein WDR5 plays a critical role in maintaining the integrity of the MLL complex and fully activating its methyltransferase function. The MLL complex, the trithorax-like family of SET1 methyltransferase, catalyzes trimethylation of lysine 4 on histone 3, and they have been widely implicated in various cancers. WDR5-C47 could serve as a tool compound to study functions of SET1-family of human histone methyltransferases and further develop therapeutic drug molecules targeting the WDR5−MLL interaction. 

How to Use:

• In vitro:  WDR5-C47 was suggested to be used at 10 µM final concentration in vitro and in cellular assays.
• In vivo:  n/a

Reference: 

• 1. Bolshan Y, et al. Synthesis, Optimization, and evalsuation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction.  (2013) ACS Med. Chem. Lett., 4 (3), 353–357.

Products are for research use only. Not for human use.