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ML-7 hydrochloride

ML-7 hydrochloride

产品编号 T3050   CAS 110448-33-4
别名: ML-7 HCl, ML-7盐酸盐

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、PKAPKC

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ML-7 hydrochloride Chemical Structure
ML-7 hydrochloride, CAS 110448-33-4
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
其他形式的 ML-7 hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
产品目录号及名称: ML-7 hydrochloride (T3050)
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纯度: 99.61%
纯度: 99%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 22.6 mg/mL (50 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Cheng X, et al. Mol Med Rep. 2015, 12(3):4109-16. 2. Connell LE, et al. J Cell Sci. 2006, 119(Pt 11):2269-81. 3. Saitoh M, et al. J Biol Chem. 1987, 262(16):7796-801. 4. Fazal F, et al. Mol Cell Biol. 2005, 25(14):6259-66. 5. Zhang H, Lin F, Huang J, et al. Anisotropic stiffness gradient-regulated mechanical guidance drives directional migration of cancer cells[J]. Acta Biomaterialia. 2020.

TargetMol Library Books文献引用

1. Zhang H, Lin F, Huang J, et al. Anisotropic stiffness gradient-regulated mechanical guidance drives directional migration of cancer cells. Acta Biomaterialia. 2020 2. Sun L, Sun L, Li X, et al. A Novel Tigecycline Adjuvant ML-7 Reverses the Susceptibility of Tigecycline-Resistant Klebsiella pneumoniae. Frontiers in cellular and infection microbiology. 2022: 1341.
N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine kb NB 142-70 SGC-GAK-1 Chymotrypsin Pinostrobin FOY 251 SM1-71 Benzamidine hydrochloride

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 酪氨酸激酶分子库 TGF-β/Smad靶点化合物库 代谢化合物库 细胞凋亡化合物库 经典已知活性库 已知活性化合物库 干细胞分化化合物库 激酶抑制剂库 抗癌化合物库

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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。

Keywords

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

 

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