MI-2-2

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MI-2-2 

MI-2-2 是一种有效的 menin-MLL 抑制剂。MI-2-2 以低纳摩尔亲和力 (Kd=22 nM) 与 menin 结合,并非常有效地破坏 menin 和 MLL 之间的二价蛋白质-蛋白质相互作用。MI-2-2 在 MLL 白血病细胞中具有特异且非常显著的活性,包括抑制细胞增殖、下调 Hoxa9 表达和分化。

MI-2-2

MI-2-2 Chemical Structure

CAS No. : 1454920-20-7

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生物活性

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=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].

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

415.50

Formula

C17H20F3N5S2

CAS 号

1454920-20-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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