MI-2 (Menin-MLL Inhibitor)

Catalog No.S7618

MI-2 (Menin-MLL Inhibitor) Chemical Structure

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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Biological Activity

Description MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
Targets
Menin-MLL interaction [1]
(Cell-free assay)
446 nM
In vitro

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. [1]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: MLL-AF9 and E2A-HLF transduced murine BMC
  • Concentrations: ~20 μM
  • Incubation Time: 12 days
  • Method: The MLL-AF9 and E2A-HLF transduced murine BMC are plated in 12-well plates at the concentration of 5×103 cells/mL with 1 mL methylcellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds. 6 days later colonies are stained with 100 μL iodonitrotetrazolium chloride at final concentration of 1 mg/mL, incubated at 37°C for 30 min and counted. To replate for the 2nd round, colonies are counted at day 6 without staining and cells were washed out by 1×PBS buffer and resuspended in IMDM medium containing 15% FBS, 1% penicillin/streptomycin and IL-3. 5×103 cells are plated in 12-well plates with 1ml methycellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds. 6 days later colonies are stained and counted.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL warmed (199.7 mM)
Ethanol 75 mg/mL (199.7 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 375.55
Formula

C18H25N5S2

CAS No. 1271738-62-5
Storage powder
Synonyms N/A

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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 --

Tech Support

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.

Handling Instructions

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID