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MM-401 TFA

目录号 : GC67758

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 Chemical Structure

Cas No.:1442106-11-7

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5mg
¥10,080.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

Cas No. 1442106-11-7 SDF Download SDF
分子式 C31H47F3N8O7 分子量 700.75
溶解度 Methanol : 125 mg/mL (178.38 mM; Need ultrasonic) 储存条件 4°C, protect from light
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1 mM 1.427 mL 7.1352 mL 14.2704 mL
5 mM 0.2854 mL 1.427 mL 2.8541 mL
10 mM 0.1427 mL 0.7135 mL 1.427 mL
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