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

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

Cat.No.S7619

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

Chemical Structure

Molecular Weight: 375.55

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 375.55 Formula

C18H25N5S2

 Storage (From the date of receipt)
CAS No. 1271738-59-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)C1=CC2=C(N=CN=C2S1)N3CCN(CC3)C4=NCC(C)(C)S4

Solubility

In vitro
Batch:

DMSO : 19 mg/mL (50.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Menin-MLL interaction [1]
648 nM
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 screened as follows: 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, 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 this compound 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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