MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 µM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, Apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia[1].
MM-401 maintains high binding affinity to WDR5 with a Ki value of < 1 nM and disrupts WDR5-MLL1 interaction with an IC50 value of 0.9 nM[1].
MM-401 is able to specifically inhibit MLL1 activity (IC50 value of 0.32µM) by blocking MLL1-WDR5 interaction and thus the complex assembly[1].
MM-401 (20 μM; 48 h) specifically inhibits MLL1-dependent H3K4 methylation in cells[1].
MM-401 induces similar changes in MLL-AF9 transcriptome as the MLL1 deletion[1].
MM-401 (10, 20, 40 μM; 48 h) specifically inhibits growth of MLL leukemia cells by inducing cell cycle arrest, apoptosis[1].
Apoptosis Analysis[1]
| Cell Line: | Murine MLL-AF9 and Hoxa9/Meis1 cells |
| Concentration: | 10, 20, 40 μM |
| Incubation Time: | 48 h |
| Result: | Specifically induced apoptosis of MLL-AF9 cells. |
Cell Cycle Analysis[1]
| Cell Line: | Murine MLL-AF9 and Hoxa9/Meis1 cells |
| Concentration: | 10, 20, 40 μM |
| Incubation Time: | 48 h |
| Result: | Induced prominent G1/S arrest in MLL-AF9 cells in a concentration dependent manner. |
RT-PCR[1]
| Cell Line: | MLL-AF9 cells |
| Concentration: | 20 μM |
| Incubation Time: | 48 h |
| Result: | Significantly decreased H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10. |
[1]. Fang Cao, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell. 2014 Jan 23;53(2):247-61.