Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MM-102 (HMTase Inhibitor IX) 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 | ¥ 428 | 现货 | ||
2 mg | ¥ 622 | 现货 | ||
5 mg | ¥ 1,280 | 现货 | ||
10 mg | ¥ 1,980 | 现货 | ||
25 mg | ¥ 4,230 | 现货 | ||
50 mg | ¥ 7,360 | 现货 | ||
100 mg | ¥ 9,930 | 现货 | ||
500 mg | ¥ 19,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,790 | 现货 |
产品描述 | MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM. |
靶点活性 | MLL1:0.4 μM |
体外活性 | MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and Ki of < 1 nM. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins. [1] |
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. |
细胞实验 | MV4;11, KOPN8, and K562 cells are cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillin-streptomycin and incubated at 37 °C under 5% CO2. Cells are seeded into 12-well plates for suspension at a density of 5 × 105 per well (1 mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 for 7 days. The medium is changed every 2 days, and compounds are resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit is used following the manufacturer’s instruction. First, 100 μL of the assay reagent is added into each well, and the content is mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence is read on a microplate reader. (Only for Reference) |
别名 | MM102, HMTase Inhibitor IX |
分子量 | 669.8 |
分子式 | C35H49F2N7O4 |
CAS No. | 1417329-24-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (138.8 mM)
H2O: 92 mg/mL (137.4 mM)
Ethanol: 93 mg/mL (138.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O / Ethanol | 1 mM | 1.493 mL | 7.4649 mL | 14.9298 mL | 37.3246 mL |
5 mM | 0.2986 mL | 1.493 mL | 2.986 mL | 7.4649 mL | |
10 mM | 0.1493 mL | 0.7465 mL | 1.493 mL | 3.7325 mL | |
20 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
50 mM | 0.0299 mL | 0.1493 mL | 0.2986 mL | 0.7465 mL | |
100 mM | 0.0149 mL | 0.0746 mL | 0.1493 mL | 0.3732 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 1417329-24-8 Chromatin/Epigenetic Histone Methyltransferase MM102 HMTase Inhibitor IX MM 102 Inhibitor inhibit inhibitor