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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree 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|
References are publications that support the biological activity of the product.
Karatas et al (2013) High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J.Am.Chem.Soc. 135 669 PMID: 23210835
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Keywords: MM 102, MM 102 supplier, MM102, Mixed, lineage, leukemia, 1, MLL1, WD, repeat-containing, protein, 5, WDR5, interaction, inhibitors, inhibits, leukaemia, 14173292483, 1417329_24_83, Lysine, Methyltransferases, 5307, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.