Menin-MLL-inhibitor-MI-2 - Epigenetic Reader Domain 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMenin-MLL inhibitor MI-2Cat. No.: HY-15222CAS No.: 1271738-62-5分式: CHNS分量: 375.55作靶點(diǎn): Epigenetic Reader Domain作通路: Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (133.1

2、4 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6628 mL 13.3138 mL 26.6276 mL5 mM 0.5326 mL 2.6628 mL 5.3255 mL10 mM 0.2663 mL 1.3314 mL 2.6628 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清

3、的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.66 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.66 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL

4、 (6.66 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Menin-MLL inhibitor MI-2 抑制 Menin-MLL 相互作，IC50 為 44628 nM。IC50 & Target IC50: 44628 nM (Menin-MLL) 1體外研究 Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced

5、BMC,with GI50 values of about 5 M. Assessment of diverse hydrophobic groups at R1 led to the development ofseveral compounds with IC50 values in the nanomolar range, including MI-2 (IC50= 44628 nM) and MI-3(IC50=64825 nM).The dissociation constants measured for the menin-MLL inhibitors are at the na

6、nomolarlevel, Kd=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLFtransduced BMC (GI5050 M), which may be due to inhibition of the menin interaction w

7、ith wild-type MLL.Treatment with MI-2 results in GI50 values below 10 M in MV4;11 (harboring MLL-AF4; GI50=9.5 M),KOPN-8 (MLL-ENL; GI50=7.2 M) and ML-2 (MLL-AF6; GI50=8.7 M), and in MonoMac6 (MLL-AF9;GI50=18 M) 1.PROTOCOLCell Assay 1 5105 HEK 293 cells/mL are plated in 12-well plates (1 mL/well) and

8、 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 at37C in a 5% CO2 incubator. After incubation, 1.5105 cells are harvested and resuspended in 100 L 1Annexin V binding buffer from the Annexin V-FITC Apoptosis kit, i

9、ncubated with 4 L of AnnexinV-FITC and6 L of Propidium iodide at room temperature in the dark for 10 minutes and analyzed by flow cytometry on aLSR II instrument. Data analysis is performed using WinList software. The experiments are performed threetimes in triplicates with calculation of mean and s

10、tandard deviation for each condition 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Syst. 2018 Apr 25;6(4):424-443.e7. Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology(2012), 8(3), 277-284.McePdfHeightCaution: Product has not been ful