MM-102,WDR5-MLL1Antagonist

MM-102 is a highly potent and selective inhibitor of the MLL1/WDR5 interaction with an IC₅₀ ~2.9 nM binding affinity to WDR5. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. MM-102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.  MM-102 provides the first proof-of-concept small molecule inhibitor to target the WDR5/MLL1 protein-protein interaction as a novel therapeutic approach for acute leukemia harboring MLL1 fusion proteins.

How to Use:

• In vitro:  MM-102 was suggested to be used at 10-100 µM final concentration in vitro and in cellular assays. 
• In vivo:  n/a

Reference:

• 1. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. (2013)  J Am Chem Soc. 135(2):669-82.