MI-2 (Menin-MLL Inhibitor)
Molecular Weight(MW): 375.55
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
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Choose Selective Histone Methyltransferase Inhibitors
|Description||MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.|
In HEK293 cells, MI-2 accessed the protein target and effectively inhibits the menin-MLL-AF9 interaction. MI-2 effectively blocks MLL fusion protein-mediated leukemic transformation by downregulating the expression of target genes required for MLL fusion protein oncogenic activity. MI-2 also effectively blocks cell proliferation, and induces cell apoptosis in human MLL leukemia cell lines harboring different MLL translocations. 
High Throughput Screening:FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program.
|In vitro||DMSO||75 mg/mL warmed (199.7 mM)|
|Ethanol||75 mg/mL (199.7 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01267110||Completed||Breast Cancer Screening||University of Kansas|University of Kansas Medical Center||September 2010||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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