产品描述
MI-2 (Menin-MLL Inhibitor) is an effective menin-MLL interaction inhibitor (IC50: 446 ± 28 nM).
体外活性
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].
体内活性
After 7 days of treatment with MI-2, MLL-AF9 transformed BMC showed great morphology changes and the expression of CD11b was greatly increased [1].
Cas No.
T22978
分子式
C18H25N5S2·2HCl
分子量
448.5
储存和溶解度
Ethanol:≤30mg/mL
DMSO:10mg/ml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years