MI-2 (hydrochloride)

Short Summary : menin-MLL interaction inhibitor

Category : Others|Menin-MLL

Purity : 0.98

CAS Number :

Formula : C18H25N5S2 • 2HCl

Molecular Weight :

Molecular Weight : 448.5

SMILE : CCCC(S1)=CC(C1=NC=N2)=C2N3CCN(C4=NCC(C)(C)S4)CC3.Cl.Cl

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : 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 M for MI-2. MI-2 showed little effect on the cell growth of E2A-HLF transduced BMC with the GI50 of > 50 M. 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].References:[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.

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