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Menin-MLL inhibitor MI-2

CAS No. : 1271738-62-5

MCE 站：Menin-MLL inhibitor MI-2

产品活性：Menin-MLL inhibitor MI-2 抑制 Menin-MLL 相互作用，IC₅₀ 为 446±28 nM。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Epigenetic Reader Domain  |  Apoptosis

In Vitro: Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI₅₀ values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC₅₀ values in the nanomolar range, including MI-2 (IC₅₀= 446±28 nM) and MI-3 (IC₅₀=648±25 nM).The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, K_d=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI₅₀>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI₅₀ values below 10 μM in MV4;11 (harboring MLL-AF4; GI₅₀=9.5 μM), KOPN-8 (MLL-ENL; GI₅₀=7.2 μM) and ML-2 (MLL-AF6; GI₅₀=8.7 μM), and in MonoMac6 (MLL-AF9; GI₅₀=18 μM).

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