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    MI-2 (Menin-MLL Inhibitor)
    MI-2 (Menin-MLL Inhibitor)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0396
    CAS #: 1271738-62-5Purity ≥98%

    Description: MI-2 (MI2, Menin-MLL Inhibitor) is a novel, potent and selective inhibitor of menin-MLL interaction with antineoplastic activity. It inhibits menin-MLL interaction with an IC50 of 446 nM. MI-2 acts by binding to the wild-type menin but doesn't bind M278K and Y323K menin mutants. In HEK293 cells transfected with Flag-MLL-AF9, MI-2 effectively inhibited the menin-MLL-AF9 interaction without affecting the expression level of menin and MLL-AF9. 

    References: Nat Chem Biol. 2012 Jan 29;8(3):277-84.

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    Molecular Weight (MW)375.55
    FormulaC18H25N5S2
    CAS No.1271738-62-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 75 mg/mL (199.7 mM)
    Water:<1 mg/mL 
    Ethanol: NA
    Other info

    Chemical Name: 4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-propylthieno[2,3-d]pyrimidine

    InChi Key: SRQYLNYQAPCPIR-UHFFFAOYSA-N

    InChi Code: InChI=1S/C18H25N5S2/c1-4-5-13-10-14-15(20-12-21-16(14)24-13)22-6-8-23(9-7-22)17-19-11-18(2,3)25-17/h10,12H,4-9,11H2,1-3H3

    SMILES Code: CCCC1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1

    SynonymsMI2 ; Menin-MLL inhibitor 2; MI 2 ; Menin MLL inhibitor 2; MI-2 ; Menin-MLL inhibitor-2;


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: 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 Assay: 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.

    In VivoMLL-AF9 transformed BMC that remained viable after 7 days of treatment with MI-2 and MI-3 showed substantial changes in morphology, indicative of monocytic differentiation, as evidenced by increased cell size, lower nuclear to cytoplasmic ratio and highly vacuolated cytoplasm. Consistent with the change in cell morphology, the expression of CD11b was substantially increased on MLL-AF9 transformed BMC after 7 days of treatment with MI-2 and MI-3. 
    Animal modelNA
    Formulation & DosageNA
    References

    Nat Chem Biol. 2012 Jan 29;8(3):277-84.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    MI-2 (Menin-MLL Inhibitor)

    Effect of MI-2 and MI-3 in human MLL leukemia cells. Nat Chem Biol. 2012 Jan 29; 8(3): 277–284.
    MI-2 (Menin-MLL Inhibitor)MI-2 (Menin-MLL Inhibitor)


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