| CAS |
No.150045-18-4 |
| 英文名称 |
MS-444 |
| 别名 |
BE-34776 |
| 分子式 |
C13H10O4 |
| 分子量 |
230.22 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
Light yellow to brown Solid |
| 储存条件 |
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00923100 |
| SMILES |
O=C(C1=C(C)OC=C1C2)C3=C2C(O)=CC=C3O |
| InChIKey |
TZUYDLKHNQUNKS-UHFFFAOYSA-N |
| InChI |
InChI=1S/C13H10O4/c1-6-11-7(5-17-6)4-8-9(14)2-3-10(15)12(8)13(11)16/h2-3,5,14-15H,4H2,1H3 |
| PubChem CID |
132904 |
| 靶点 |
MLCK（myosin light chain kinase） |
| 通路 |
Cytoskeleton |
| 背景说明 |
MS-444是mLCK的抑制剂。 |
| 生物活性 |
MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.[1-2] |
| IC50 |
IC50: 10 μM (myosin)[1]. |
| In Vitro |
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[2]. |
| In Vivo |
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]. |
| 细胞实验 |
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]. |
| 动物实验 |
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]. |
| 数据来源文献 |
[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. |
| 规格 |
1mg |
| 单位 |
瓶 |
中文
英语
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