Menin-MLL inhibitor MI-2

Name: Menin-MLL inhibitor MI-2
Brand: MedChemExpress
SKU: HY-15222
Rating: 5.0 (4 reviews)

製品番号: HY-15222 純度: 99.41%: Data Sheet SDS COA 取扱説明書
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Menin-MLL inhibitor MI-2 is a competitive and selective Menin-MLL interaction inhibitor with an IC₅₀ value of 446 nM and a K_i value of 158 nM. Menin-MLL inhibitor MI-2 downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).

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Menin-MLL inhibitor MI-2 構造式

CAS 番号 : 1271738-62-5

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$70	在庫あり	Estimated Time of Arrival: December 31
10 mg	$100	在庫あり	Estimated Time of Arrival: December 31
25 mg	$210	在庫あり	Estimated Time of Arrival: December 31
50 mg	$310	在庫あり	Estimated Time of Arrival: December 31
100 mg	$480	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Menin-MLL inhibitor MI-2:

Menin-MLL inhibitor MI-2 dihydrochloride お問い合わせ

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製品説明

IC₅₀ & Target

IC50: 446±28 nM (Menin-MLL)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	>10 μM Compound: 1; MI-2	Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay	[PMID: 36173787]
HL-60	IC₅₀	>10 μM Compound: 7; MI-2	Antiproliferative activity against human HL-60 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
MV4-11	GI₅₀	9.5 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 34726905]
MV4-11	IC₅₀	7.62 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay	[PMID: 36173787]
MV4-11	IC₅₀	8.52 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay	[PMID: 36173787]
MV4-11	IC₅₀	9.2 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay	[PMID: 36173787]
MV4-11	IC₅₀	9.2 μM Compound: 7; MI-2	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]

体外実験

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, K_d=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].

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

分子量

375.55

分子式

C₁₈H₂₅N₅S₂

CAS 番号

1271738-62-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (133.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.41%

Select Batch:

データシート (276 KB) SDS (396 KB)

COA (249 KB) HNMR (118 KB) LCMS (105 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284. [Content Brief]

細胞実験
^[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6628 mL	13.3138 mL	26.6276 mL	66.5690 mL
	5 mM	0.5326 mL	2.6628 mL	5.3255 mL	13.3138 mL
	10 mM	0.2663 mL	1.3314 mL	2.6628 mL	6.6569 mL
	15 mM	0.1775 mL	0.8876 mL	1.7752 mL	4.4379 mL
	20 mM	0.1331 mL	0.6657 mL	1.3314 mL	3.3285 mL
	25 mM	0.1065 mL	0.5326 mL	1.0651 mL	2.6628 mL
	30 mM	0.0888 mL	0.4438 mL	0.8876 mL	2.2190 mL
	40 mM	0.0666 mL	0.3328 mL	0.6657 mL	1.6642 mL
	50 mM	0.0533 mL	0.2663 mL	0.5326 mL	1.3314 mL
	60 mM	0.0444 mL	0.2219 mL	0.4438 mL	1.1095 mL
	80 mM	0.0333 mL	0.1664 mL	0.3328 mL	0.8321 mL
	100 mM	0.0266 mL	0.1331 mL	0.2663 mL	0.6657 mL