MM-401 (TFA) 是一种 MLL1 H3K4 甲基转移酶抑制剂。MM-401 通过阻断 MLL1-WDR5 相互作用来抑制 MLL1 活性（IC₅₀ 值为 0.32 µM）。MM-401 可诱导细胞周期停滞、凋亡和分化。MM-401 可用于 MLL 白血病的研究。

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 leukemia.

Solid

Ki: < 1 nM (WDR5); IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 μM (MLL1).

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.
MM-401 is able to specifically inhibit MLL1 activity (IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Fang Cao, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell. 2014 Jan 23;53(2):247-61.

In Vitro: DMSO : 100 mg/mL (142.70 mM; ultrasonic and warming and heat to 60°C)配制储备液