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MI-3

Catalog No. T2643Cas No. 1271738-59-0
Alias MI 3, Menin-MLL inhibitor 3, Menin-MLL Inhibitor

MI-3 (Menin-MLL Inhibitor) (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).

MI-3

MI-3

Purity: 98.97%
Catalog No. T2643Alias MI 3, Menin-MLL inhibitor 3, Menin-MLL InhibitorCas No. 1271738-59-0
MI-3 (Menin-MLL Inhibitor) (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
Pack SizePriceAvailabilityQuantity
1 mg$47In Stock
5 mg$108In Stock
10 mg$166In Stock
25 mg$285In Stock
50 mg$415In Stock
1 mL x 10 mM (in DMSO)$119In Stock
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Purity:98.97%
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Product Introduction

Bioactivity
Description
MI-3 (Menin-MLL Inhibitor) (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
Targets&IC50
Menin-MLL:648 nM
In vivo
In HEK293 cells, MI-3 was in close proximity to the protein target, which in turn produced a significant inhibitory effect on the menin-MLL-AF9 interaction. In human MLL leukemia cell lines carrying different MLL translocations, MI-3 effectively blocked cell differentiation and promoted cell apoptosis. Intracellularly, Amlodipine caused neuronal Ca2+ elevation by attenuating KCl depolarization.
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
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 methylcellulose 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. (Only for Reference)
AliasMI 3, Menin-MLL inhibitor 3, Menin-MLL Inhibitor
Chemical Properties
Molecular Weight375.55
FormulaC18H25N5S2
Cas No.1271738-59-0
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 16 mg/mL (42.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16 mg/mL (42.6 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.6628 mL13.3138 mL26.6276 mL133.1381 mL
5 mM0.5326 mL2.6628 mL5.3255 mL26.6276 mL
10 mM0.2663 mL1.3314 mL2.6628 mL13.3138 mL
20 mM0.1331 mL0.6657 mL1.3314 mL6.6569 mL

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