MM-102 TFA  ≥98%

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包装规格:2mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(≥100mg/mL)
产品描述:基本信息 产品编号:M10871  产品名称:MM-102 TFA CAS: 1883545-52-5   储存条件 粉末 -20℃ 四年     分子式: C37H50F5N7O6 溶于液体 -80℃ 六个月 分子量: 783.83 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.2758mL 6.3789mL 12.7579mL 5mM 0.2552mL 1.2758mL 2.5516mL 10mM 0.1276mL 0.6379mL 1.2758mL   生物活性 产品描述 一种有效的 WDR5/MLL 相互作用抑制剂, WDR5 结合检测中, IC50 =2.4nM, Ki< 1nM。 靶点/IC50 2.4nM (MLL).   体外研究 MM-102 (HMTase Inhibitor IX) inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins.MM-102 (TFA), with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay withIC50=0.4-0.9μM.MM-102 (HMTase Inhibitor IX) dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively.MM-102 (HMTase Inhibitor IX) has IC50=25μM in both cell lines and completely inhibits cell growth in these cell lines at 75μM.MM-102 (HMTase Inhibitor IX) effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein.   推荐实验方法(仅供参考) 细胞实验: MV4;11, KOPN8, and K562 cells were cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillinstreptomycin and incubated at 37℃under 5% CO2.Cells were seeded into 12-well plates for suspension at a density of 5×105 per well (1mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 (HMTase Inhibitor IX) for 7 days.The medium was changed every 2 days, and compounds were resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit was used. First, 100μL of the assay reagent was added into each well, and the content was mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence was read on a microplate reader.
保存条件:-20℃