| CAS NO: | 1417329-24-8 |
| 规格: | 98% |
| 分子量: | 669.8 |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 20mg | 电议 |
Background:
MM-102 is an antagonist of MLL1 with IC50 value of 2.4nM [1].
Mixed lineage leukemia 1 (MLL1) is a histone H3 lysine 4 (H3K4) methyltransferase. The interaction of MLL1 and WDR5 is essential for MLL1 enzymatic activity and is a target for the treatment of acute leukemia. MM-102 is a peptidomimetic of MLL1. It has a high binding affinity to WDR5 with IC50 value of 2.4nM [1].
MM-102 is reported to reduce the expression of MLL1 targeted genes HoxA9 and Meis-1 in MLL1-AF9 transduced murine cells. Since these two genes are required for MLL1 mediated leukemogenesis, MM-102 is found to inhibit cell growth of leukemia cells harboring MLL1 fusion proteins. It dose-dependently inhibits the cell growth in the MV4;11 and KOPN8 cell lines with IC50 values both of 25μM[1].
参考文献:
[1] Karatas H, Townsend EC, Cao F, Chen Y, Bernard D, Liu L, Lei M, Dou Y, Wang S. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013 Jan 16;135(2):669-82.
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