生物活性 | |||
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描述 | MI-2-2 is a potent inhibitor of menin-MLL. MI-2-2 binds to menin with a Kd value of 22 nM and is very effective in disrupting the bivalent protein-protein interactions between menin and MLL. MI-2-2 exhibits a very pronounced specific activity against MLL leukaemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression and differentiation[1].MI-2-2 inhibits both the interaction of menin with MBM1 (IC50=46 nM) and with the bivalent fragment of MLL consisting of MBM1 and MBM2 (IC50=520 nM). In BMC transformed with MLL-AF9 and in the human leukaemia cell line MV4;11 carrying the MLL-AF4 translocation, MI-2-2 showed very pronounced activity at low micromolar concentrations[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.03mL 2.41mL 1.20mL |
24.07mL 4.81mL 2.41mL |
参考文献 |
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