MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (K_d=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation^[1].

MI-2-2 is capable of inhibiting both the interaction of menin with MBM1 (IC₅₀= 46 nM) and with the bivalent fragment of MLL that comprises both MBM1 and MBM2 (IC₅₀=520 nM). MI-2-2 exhibits very pronounced activities at low micromolar concentrations in BMCs transformed with MLL-AF9 and in MV4;11, a human leukemia cell line harboring the MLL-AF4 translocation^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

415.50

C₁₇H₂₀F₃N₅S₂

1454920-20-7

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• [1]. Shi A, et al. Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood. 2012;120(23):4461-4469.