MI-2 is a potent and specific Menin-MLL inhibitor with an IC₅₀ ~446 nM. It specifically binds to Menin and inhibits Menin’s interaction with MLL fusion proteins in cells. It can effectively reverse MLL fusion protein–mediated leukemic transformation by downregulating the expression of target genes downstream of MLL fusion protein oncogenic activity. MI-2 is a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of Menin as an oncogenic cofactor of MLL fusion proteins.

How to Use:

• In vitro: MI-2 was used at 10-25 µM concentration in vitro and in the cellular assays. 
• In vivo: n/a 

Reference:

• 1. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. (2012) Nat Chem Biol. 8(3):277-84.