1. Epigenetics
  2. Histone Methyltransferase
  3. Menin-MLL inhibitor MI-2

Menin-MLL inhibitor MI-2 

Cat. No.: HY-15222 Purity: 99.81%
Handling Instructions

Menin-MLL inhibitor MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.

For research use only. We do not sell to patients.

Menin-MLL inhibitor MI-2 Chemical Structure

Menin-MLL inhibitor MI-2 Chemical Structure

CAS No. : 1271738-62-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 172 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 960 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

Menin-MLL inhibitor MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.

IC50 & Target

IC50: 446±28 nM (Menin-MLL)[1]

In Vitro

Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC50 values in the nanomolar range, including MI-2 (IC50= 446±28 nM) and MI-3 (IC50=648±25 nM).The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, Kd=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI50>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI50 values below 10 μM in MV4;11 (harboring MLL-AF4; GI50=9.5 μM), KOPN-8 (MLL-ENL; GI50=7.2 μM) and ML-2 (MLL-AF6; GI50=8.7 μM), and in MonoMac6 (MLL-AF9; GI50=18 μM)[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (133.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6628 mL 13.3138 mL 26.6276 mL
5 mM 0.5326 mL 2.6628 mL 5.3255 mL
10 mM 0.2663 mL 1.3314 mL 2.6628 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

5×105 HEK 293 cells/mL are plated in 12-well plates (1 mL/well) and treated with compounds (e.g., MI-2) (0.25% final concentration of DMSO for each condition) or 0.25% DMSO control and incubated for 48h at 37°C in a 5% CO2 incubator. After incubation, 1.5×105 cells are harvested and resuspended in 100 μL 1× Annexin V binding buffer from the Annexin V-FITC Apoptosis kit, incubated with 4 μL of AnnexinV-FITC and 6 μL of Propidium iodide at room temperature in the dark for 10 minutes and analyzed by flow cytometry on a LSR II instrument. Data analysis is performed using WinList software. The experiments are performed three times in triplicates with calculation of mean and standard deviation for each condition[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

375.55

Formula

C₁₈H₂₅N₅S₂

CAS No.

1271738-62-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Menin-MLL inhibitor MI-2
Cat. No.:
HY-15222
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Menin-MLL inhibitor MI-2

Cat. No.: HY-15222