MI-2 (hydrochloride)

An inhibitor of menin-MLL interactions

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1mg

￥300.00

240.00

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5mg

￥1212.00

970.00

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10mg

￥1837.00

1470.00

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25mg

￥3600.00

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货号: ajcx11018
CAS: N/A
别名:
分子式: C18H25N5S2 ? 2HCl
分子量: 448.5
纯度: >98%
溶解度: ≤30mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with an IC50 value of 446 ± 28 nM.

Menin is an oncogenic cofactor in leukemic transformations which could bind to the N-terminal fragment of MLL existed in all MLL fusion proteins. Menin is a highly specific and direct binding partner of MLL and MLL fusion proteins which is essential for regulation of their target genes. Disruption of the menin-MLL protein interaction abrogates oncogenic properties of MLL fusion proteins and blocks the development of acute leukemia [2].

In vitro: In HEK293 cells, MI-2 accessed the protein target menin-MLL and effectively inhibited the menin-MLL-AF9 interaction. MI-2 effectively blocked cell proliferation, and induced cell apoptosis in human MLL leukemia cell lines harboring different MLL translocations MLL-AF9 and MLL-ENL, with the GI50 value of about 5 μM for MI-2. MI-2 showed little effect on the cell growth of E2A-HLF transduced BMC with the GI50 of > 50 μM. MI-2 specifically reduced the immortalization potential of cells transformed with MLL fusion oncoproteins by downregulating the expression of target genes required for MLL fusion protein oncogenic activity [1].

In vivo: After 7 days treatment with MI-2, MLL-AF9 transformed BMC showed great morphology changes and the expression of CD11b was greatly increased [1].

参考文献:
[1].? Grembecka J, He S, Shi A, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia[J]. Nature chemical biology, 2012, 8(3): 277-284.
[2].? Borkin D, He S, Miao H, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo[J]. Cancer Cell, 2015, 27(4): 589-602.