MS-444 (BE-34776)
(Synonyms: BE-34776) 目录号 : GC33214
MS-444 (BE-34776) 抑制纯化的平滑肌肌球蛋白轻链激酶 (MLCK) 的活性，IC50 值为 10 μM.
Cas No.:150045-18-4
Sample solution is provided at 25 µL, 10mM.
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MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.
MS-444 is a small molecule RNA-binding protein HuR (ELAVL1) inhibitor. Colorectal cancer (CRC) cells that display HuR overexpression are treated with MS-444 (1-100 μM) for 48 hr with IC50s of 10.98±1.76 μM, 12.84±2.10 μM, 5.60±0.90 μM, 14.21±2.11 μM, and 10.98±1.24 μM for HCT116, HCA-7, RKO, HT-29, and SW480 cells, respectively. Growth inhibition is observed in all CRC lines with IC50 values ranging from 5.60 μM to 14.21 μM with observable effects seen at 10 μM MS-444. Contrasting effects are observed using non-transformed small intestinal (RIE-1 (IC50=40.70±3.53 μM)) and colonic (YAMC (IC50=28.16±3.23 μM)) epithelial cells. Both cell types display properties of normal intestinal epithelial cells and are proficient in 3′UTR AU-rich elements (ARE)-mRNA decay. Both non-transformed cell lines are ~3- to 4-fold less responsive to MS-444-mediated growth inhibition, with IC50 values of 40.70 μM and 28.16 μM (P<0.05)[2].
To test the effects of MS-444 on CRC cell growth in vivo, mice bearing HCT116 cell xenografts receive IP injections of MS-444 (25 mg/kg bw) or vehicle every 48 hr. Over the experiment course, mice do not display any adverse effects and maintained similar weights. Anti-tumor effects of MS-444 are observed with approximately 1.7-fold reduction in tumor size. Mice treated with MS-444 show a marked 2- to 3-fold decrease in microvessel density (MVD), indicating the anti-angiogenic potential of MS-444[2].
[1]. Satoshi Nakanishi. et al. MS-444, a new inhibitor of myosin light chain kinase from Micromonosporasp.KY7123. The Journal Of Antibiotics. 1995,48(9):948-951. [2]. Fernando F. Blanco.et al, Impact of HuR inhibition by the small molecule MS-444 on colorectal cancer cell tumorigenesis. Oncotarget. 2016 Nov 8; 7(45): 74043-74058.
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Cell experiment: |
Human colorectal cancer cell lines RKO, HCA-7, HCT116, HT-29, SW480 and the non-transformed intestinal epithelial cell lines RIE-1, YAMC are treated with varying concentrations of MS-444 (1-100 μM) for 48 hr. Cell survival is measured by MTT assay after incubation of cells for 48 hr with MS-444. Relative cell survival is calculated as percentage normalized to DMSO vehicle-treated cells and plotted to determine IC50[2]. |
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Animal experiment: |
Mice[2]Athymic nude (Nu/Nu) mice are used. HCT116 (2×106 cells) and HCA-7 (2.5×106) cells resuspended in PBS are injected into the dorsal subcutaneous tissue. Mice (n=5 per group) receive intraperitoneal (IP) injections of MS-444 (25 mg/kg) dissolved in PBS/5% N-Methyl Pyrrolidine (NMP) or vehicle control every 48 hr. Tumor growth is assayed[2]. |
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References: [1]. Satoshi Nakanishi. et al. MS-444, a new inhibitor of myosin light chain kinase from Micromonosporasp.KY7123. The Journal Of Antibiotics. 1995,48(9):948-951. |
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| Cas No. | 150045-18-4 | SDF | |
| 别名 | BE-34776 | ||
| Canonical SMILES | O=C(C1=C(C)OC=C1C2)C3=C2C(O)=CC=C3O | ||
| 分子式 | C13H10O4 | 分子量 | 230.22 |
| 溶解度 | DMSO: 12.5 mg/mL (54.30 mM) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3437 mL | 21.7184 mL | 43.4367 mL |
| 5 mM | 0.8687 mL | 4.3437 mL | 8.6873 mL |
| 10 mM | 0.4344 mL | 2.1718 mL | 4.3437 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
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