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Description: Potent WDR5/MLL interaction inhibitor
Chemical Name: 1-[[(2S)-5-[(Aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]-cyclopentanecarboxamide trifluoroacetate
Purity: ≥95% (HPLC)
Biological Activity for MM 102
MM 102 is a 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.
Compound Libraries for MM 102
MM 102 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for MM 102
| M. Wt | 783.83 |
| Formula | C35H49F2N7O4.CF3CO2H |
| Storage | Store at -20°C |
| Purity | ≥95% (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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for MM 102
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 66.98 | 100 |
Preparing Stock Solutions for MM 102
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 |
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Product Datasheets for MM 102
References for MM 102
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
If you know of a relevant reference for MM 102, please let us know.
View Related Products by Target
Keywords: MM 102, MM 102 supplier, MM102, Mixed, lineage, leukemia, 1, MLL1, WD, repeat-containing, protein, 5, WDR5, interaction, inhibitors, inhibits, leukaemia, WD40, 14173292483, 1417329_24_83, Lysine, Methyltransferases, 5307, Tocris Bioscience
2 Citations for MM 102
Citations are publications that use Tocris products. Selected citations for MM 102 include:
Ilona et al (2019) Epigenetic stabilization of DC and DC precursor classical activation by TNFα contributes to protective T cell polarization. Sci Adv 5 eaaw9051 PMID: 31840058
Ayumu et al (2019) Inhibition of the H3K4 methyltransferase MLL1/WDR5 complex attenuates renal senescence in ischemia reperfusion mice by reduction of p16INK4a. Kidney Int 96 1162-1175 PMID: 31570196
Do you know of a great paper that uses MM 102 from Tocris? Please let us know.
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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* 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 in Cancer Poster
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.