Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ML-7 hydrochloride (ML-7 HCl) 是一种可渗透细胞的、可逆的、有效的、ATP 竞争性的肌球蛋白轻链激酶(MLCK) 特异性抑制剂,IC50为300 nM。它还抑制平滑肌肌球蛋白轻链激酶、PKA 和 PKC。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 241 | 现货 | ||
10 mg | ¥ 433 | 现货 | ||
25 mg | ¥ 868 | 现货 | ||
50 mg | ¥ 1,580 | 现货 | ||
100 mg | ¥ 2,980 | 现货 | ||
200 mg | ¥ 4,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 241 | 现货 |
产品描述 | ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC. |
靶点活性 | PKC:42 μM, PKA:21 μM, MLCK:0.3 μM(Ki) |
体外活性 | Inhibition of MLCK by ML-7 induces activation of caspase-3 in adherent MCF-10A and MCF-10A Ras-transformed cells[2]. Its treatment results in a dose-dependent decrease in MLC20 phosphorylation and a corresponding increase in cell death of SMC(smooth muscle cells). The inhibitory effect of ML-7 on MLCK is highly selective. The Ki of ML-7 for MLCK is 0.3 μM, while its Ki for protein kinase A is 21 μM and for protein kinase C is 42 μM. Overexpressing Bcl-2 can protect cells against apoptosis induced by ML-7[4]. |
体内活性 | ML7 is able to improve Vascular endothelial dysfunction(VED) and atherosclerosis(AS) by regulating the expression of the tight junction (TJ) proteins zona occludens (ZO)-1 and occludin via mechanisms involving MLCK and MLC phosphorylation in high-fat diet-fed rabbits. ML7 decreases the expression of MLCK and MLC phosphorylation in the arterial wall of rabbits fed a high-fat diet and reduces lipid deposition lesions in AS rabbits[1]. |
激酶实验 | IKK-2 Assay: Recombinant human IKK-2 (residues 1-756) is expressed in baculovirus as an N-terminal GST-tagged fusion protein, and its activity is assessed using a time-resolved fluorescence resonance energy transfer assay. In brief, IKK-2 (5 nM final) diluted in assay buffer (50 mM HEPES, 10 mM MgCl2, 1 mM CHAPS, pH 7.4, with 1 mM DTT and 0.01% w/v BSA) is added to wells containing various concentrations of compound or dimethyl sulfoxide (DMSO) vehicle (3% final). The reaction is initiated by the addition of GST-IκBα substrate (25 nM final)/ATP (1 μM final), in a total volume of 30 μL. The reaction is incubated for 30 min at room temperature, then terminated by the addition of 15 μL of 50 mM EDTA. Detection reagent (15 μL) in buffer (100 mM HEPES, pH 7.4, 150 mM NaCl, and 0.1% w/v BSA) containing antiphosphoserine- IκBα-32/36 monoclonal antibody 12C2, labeled with W-1024 europium chelate, and an allophycocyanin-labeled anti-GST antibody is added, and the reaction is further incubated for 60 min at room temperature. The degree of phosphorylation of GST- IκBαis measured as a ratio of specific 665-nm energy transfer signal to reference europium 620-nm signal, using a Packard Discovery plate reader. |
细胞实验 | Cells are treated with vehicle alone, Blebbistatin, ML-7, ML-9, latrunculin A or Y-27632 in media without serum at varying concentrations and time points before being fixed or prepared for FACS analysis. Untreated cells are also serum starved for the duration of the inhibitor treatment. Stock solutions of each agent are made in DMSO (50 μM Blebbistatin, 5 mM LA), 50% ethanol (10 mM ML-7), 70% ethanol (20 mM ML-9) or water (20 mM Y-27632) and are maintained at -20°C.(Only for Reference) |
别名 | ML-7 HCl, ML-7盐酸盐 |
分子量 | 452.74 |
分子式 | C15H18ClIN2O2S |
CAS No. | 110448-33-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.6 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2088 mL | 11.0439 mL | 22.0877 mL | 55.2193 mL |
5 mM | 0.4418 mL | 2.2088 mL | 4.4175 mL | 11.0439 mL | |
10 mM | 0.2209 mL | 1.1044 mL | 2.2088 mL | 5.5219 mL | |
20 mM | 0.1104 mL | 0.5522 mL | 1.1044 mL | 2.761 mL | |
50 mM | 0.0442 mL | 0.2209 mL | 0.4418 mL | 1.1044 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。
ML-7 hydrochloride 110448-33-4 Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Metabolism Stem Cells Tyrosine Kinase/Adaptors Serine/threonin kinase Myosin YAP PKA PKC ML-7 Hydrochloride Inhibitor Yes-associated protein ML-7 HCl inhibit ML-7 ML7 hydrochloride ML-7盐酸盐 ML7 ML7 Hydrochloride ML 7 ML 7 hydrochloride ML 7 Hydrochloride inhibitor