Biological Activity
Potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM). Inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins.
Technical Data
M. Wt | 783.83 |
Formula | C35H49F2N7O4.CF3CO2H |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1883545-52-5 |
PubChem ID | 71520620 |
InChI Key | ZRKTWBXVGMHWHM-YCBFMBTMSA-N |
Smiles | O=C(NC(C2=CC=C(F)C=C2)C1=CC=C(F)C=C1)C3(CCCC3)NC([C@@H](NC(C(CC)(CC)NC(C(C)C)=O)=O)CCCNC(N)=N)=O.OC(C(F)(F)F)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 66.98 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 783.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.28 mL | 6.38 mL | 12.76 mL |
5 mM | 0.26 mL | 1.28 mL | 2.55 mL |
10 mM | 0.13 mL | 0.64 mL | 1.28 mL |
50 mM | 0.03 mL | 0.13 mL | 0.26 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Karatas et al (2013) High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J.Am.Chem.Soc. 135 669 PMID: 23210835
Keywords: MM 102, supplier, MM102, Mixed, lineage, leukemia, 1, MLL1, WD, repeat-containing, protein, 5, WDR5, interaction, inhibitors, inhibits, leukemia, leukaemia, 14173292483, 1417329_24_83, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience