Home Epigenetics Histone Methyltransferase inhibitor - MLL inhibitor MI-2 (Menin-MLL Inhibitor) For research use only.

MI-2 (Menin-MLL Inhibitor)

MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

MI-2 (Menin-MLL Inhibitor) Chemical Structure

MI-2 (Menin-MLL Inhibitor) Chemical Structure

CAS No. 1271738-62-5

Purity & Quality Control

MI-2 (Menin-MLL Inhibitor) Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

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 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]
Kinase Assay 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 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05318482 Recruiting
Cardiorespiratory Failure
Istituti Clinici Scientifici Maugeri SpA
 March 23 2022 Not Applicable
NCT00624000 Completed
Ischemic Stroke
University of North Carolina Chapel Hill|Genentech Inc.
 March 2004 Not Applicable

Chemical Information & Solubility

Molecular Weight 375.55 Formula

C18H25N5S2
CAS No. 1271738-62-5 SDF Download MI-2 (Menin-MLL Inhibitor) SDF
Smiles CCCC1=CC2=C(N=CN=C2S1)N3CCN(CC3)C4=NCC(S4)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (199.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 75 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy MI-2 (Menin-MLL Inhibitor) | MI-2 (Menin-MLL Inhibitor) supplier | purchase MI-2 (Menin-MLL Inhibitor) | MI-2 (Menin-MLL Inhibitor) cost | MI-2 (Menin-MLL Inhibitor) manufacturer | order MI-2 (Menin-MLL Inhibitor) | MI-2 (Menin-MLL Inhibitor) distributor