产品详情
简单介绍：
MM-102,WDR5-MLL1Antagonist
详情介绍：
Product Information
| Molecular Weight: | 669.80 |
| Formula: | C35H49F2N7O4 |
| Purity: | ≥98% |
| CAS#: | 1417329-24-8 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | (S)-N-(bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
MM-102 is a highly potent and selective inhibitor of the MLL1/WDR5 interaction with an IC50 ~2.9 nM binding affinity to WDR5. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. MM-102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins. MM-102 provides the first proof-of-concept small molecule inhibitor to target the WDR5/MLL1 protein-protein interaction as a novel therapeutic approach for acute leukemia harboring MLL1 fusion proteins.
How to Use:
- In vitro: MM-102 was suggested to be used at 10-100 µM final concentration in vitro and in cellular assays.
- In vivo: n/a
Reference:
- 1. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. (2013) J Am Chem Soc. 135(2):669-82.
Products are for research use only. Not for human use.
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