Home Epigenetics Histone Methyltransferase inhibitor - MLL inhibitor MI-3 (Menin-MLL Inhibitor)

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MI-3 (Menin-MLL Inhibitor) Histone Methyltransferase inhibitor

MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.

MI-3 (Menin-MLL Inhibitor) Histone Methyltransferase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 375.55

Purity & Quality Control

Batch: S761901 DMSO]19 mg/mL]false]Ethanol]19 mg/mL]false]Water]Insoluble]false Purity: 99.86%
99.86

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Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Mechanism of Action

Targets
Menin-MLL interaction [1]
648 nM

In vitro
In vitro In HEK293 cells, MI-3 (Menin-MLL Inhibitor) accesses the protein target and effectively inhibits the menin-MLL-AF9 interaction. It effectively blocks MLL fusion protein-mediated leukemic transformation by downregulating the expression of target genes required for MLL fusion protein oncogenic activity. In human MLL leukemia cell lines harboring different MLL translocations, this compound effectively blocks cell proliferation, and induces apoptosis. [1]
Kinase Assay High Throughput Screening
MI-3 (Menin-MLL Inhibitor) is used at a final concentration of 20 μM (1% DMSO) in point screening, where 0.2 μL of this compound is added to 20 μL of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. The protein-peptide mixture is prepared by mixing FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer, followed by incubation for 1h in the dark at room temperature. In confirmation screening, 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 Cell lines MLL-AF9 and E2A-HLF transduced murine BMC
Concentrations ~20 μM
Incubation Time 12 days
Method

MI-3 (Menin-MLL Inhibitor) is used in the following procedure: 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 this compound. 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 methylcellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or it. 6 days later colonies are stained and counted.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05322395 Recruiting
Acute Coronary Syndrome|Troponin|Chest Pain|Point-of-care Systems
Liverpool University Hospitals NHS Foundation Trust|northwest coast academic science network|Quidel Corporation|Siemens Corporation Corporate Technology|Abbott Diagnostics Division
 December 10 2021 Not Applicable

References
  • https://pubmed.ncbi.nlm.nih.gov/22286128/

Chemical Information

Molecular Weight 375.55 Formula

C18H25N5S2
CAS No. 1271738-59-0 SDF Download SDF
Synonyms N/A
Smiles CC(C)C1=CC2=C(N=CN=C2S1)N3CCN(CC3)C4=NCC(C)(C)S4

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 19 mg/mL ( (50.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble


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In vivo
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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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