Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5/MLL 相互作用抑制剂,在 WDR5 结合检测中,IC50为 2.4 nM,Ki 小于 1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 389 | 现货 | ||
2 mg | ¥ 558 | 现货 | ||
5 mg | ¥ 1,170 | 现货 | ||
10 mg | ¥ 1,930 | 现货 | ||
25 mg | ¥ 3,460 | 现货 | ||
50 mg | ¥ 4,920 | 现货 | ||
100 mg | ¥ 7,150 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,780 | 现货 |
产品描述 | MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5) and results in the inhibition of MLL1 H3K4 histone methyltransferase (HMT) activity. Down-Regulation of H3K4me3 by MM-102 Facilitates Epigenetic Reprogramming of Porcine Somatic Cell Nuclear Transfer Embry |
靶点活性 | MLL1:0.4 μM |
体外活性 | MM-102, in bone marrow cells transduced with MLL1-AF9 fusion construct shows that the compound effectively decreases the expression of HoxA9 and Meis-1, two critical MLL1 target genes in MLL1 fusion protein mediated leukemogenesis.?MM-102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins. |
激酶实验 | In Vitro Histone Methyltransferase (HMT) Assay: The HMT assay is performed in 50 mM HEPES pH 7.8, 100 mM NaCl, 1.0 mM EDTA, and 5% glycerol at 22 °C. Each reaction contains 1.5 μCi of the co-factor, 3H-S-adenosylmethionine. H3 10-residue peptide is used as the substrate at 50 μM. Compounds are added at concentrations ranging from 0.125 to 128 μM and incubated with the pre-assembled WDR5/RbBP5/ASH2L complex at a final concentration of 0.5 μM for each protein for 2–5 min. Reactions are initiated by addition of the MLL1 protein at a final concentration of 0.5 μM and allowed to proceed for 30 min before preparing scintillation counting. To count samples, reactions are spotted on separate squares of P81 filter paper and precipitated by submerging in freshly prepared 50 mM sodium bicarbonate buffer with pH 9.0. After washing and drying, samples are vortexed in Ultima Gold scintillation fluid and counted. As a negative control, assays are performed using 0.5 μM MLL1/WDR5/RbBP5/ASH2L complex assembled with the non-interacting mutant, WDR5D107A. |
别名 | HMTase Inhibitor IX TFA |
分子量 | 783.83 |
分子式 | C37H50F5N7O6 |
CAS No. | 1883545-52-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 99 mg/mL(126.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.2758 mL | 6.3789 mL | 12.7579 mL | 31.8947 mL |
5 mM | 0.2552 mL | 1.2758 mL | 2.5516 mL | 6.3789 mL | |
10 mM | 0.1276 mL | 0.6379 mL | 1.2758 mL | 3.1895 mL | |
20 mM | 0.0638 mL | 0.3189 mL | 0.6379 mL | 1.5947 mL | |
50 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6379 mL | |
100 mM | 0.0128 mL | 0.0638 mL | 0.1276 mL | 0.3189 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MM-102 TFA 1883545-52-5 Chromatin/Epigenetic Histone Methyltransferase MM102 HMTase Inhibitor IX TFA HMTase Inhibitor IX MM-102 MM 102 TFA MM 102 inhibit MM102 TFA Inhibitor inhibitor