Name: MI-2 (Menin-MLL Inhibitor)
Brand: Selleck Chemicals
SKU: S7618
Availability: InStock
Rating: 5 (11 reviews)

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 Trihydrochloride UNC1999 EPZ015666 (GSK3235025) EPZ004777 MM-102 (HMTase Inhibitor IX) Chaetocin SGC 0946 EPZ005687

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (199.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 75 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (7.99mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	375.55	Formula	C₁₈H₂₅N₅S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1271738-62-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCC1=CC2=C(N=CN=C2S1)N3CCN(CC3)C4=NCC(S4)(C)C

Mechanism of Action

Targets/IC₅₀/Ki	Menin-MLL interaction (Cell-free assay) 446 nM
In vitro	In HEK293 cells, MI-2 (Menin-MLL Inhibitor) accessed 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. This compound also effectively blocks cell proliferation, and induces cell apoptosis in human MLL leukemia cell lines harboring different MLL translocations.
Kinase Assay	High Throughput Screening
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, 0.2 μL of MI-2 (Menin-MLL Inhibitor) (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	[1] https://pubmed.ncbi.nlm.nih.gov/22286128/

Clinical Trial Information

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

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

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MI-2 (Menin-MLL Inhibitor) Histone Methyltransferase inhibitor

Chemical Structure

Molecular Weight: 375.55