MM-401 TFA (C007B-375106)

MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity ( IC 50 = 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 leukemiaIn VitroMM-401 maintains high binding affinity to WDR5 with a K i value of < 1 nM and disrupts WDR5-MLL1 interaction with an IC 50 value of 0.9 nM. MM-401 is able to specifically inhibit MLL1 activity (IC 50 value of 0.32µM) by blocking MLL1-WDR5 interaction and thus the complex assembly. MM-401 (20 μM; 48 h) specifically inhibits MLL1-dependent H3K4 methylation in cells. MM-401 induces similar changes in MLL-AF9 transcriptome as the MLL1 deletion. MM-401 (10, 20, 40 μM; 48 h) specifically inhibits growth of MLL leukemia cells by inducing cell cycle arrest, apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell 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 AnalysisCell 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-PCRCell 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.Form:SolidIC50& Target:Ki: < 1 nM (WDR5),IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 µM (MLL1).

Specifications and Purity: ≥99%

Molecular Formula: C31H47F3N8O7

Molecular Weight: 700.75