| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M651052-5mg |
5mg |
期货  |
| |
| M651052-10mg |
10mg |
期货 |
|
| 英文别名 | 5,8-Dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone | BDBM50326009 | DTXSID40164458 | MS 444 | 5,8-Dihydroxy-3-methyl-9H-naphtho[2,3-c]furan-4-one | Naphtho[2,3-c]furan-4(9H)-one, 5,8-dihydroxy-3-methyl- | BE-34776 | 5,8-Dihydroxy-3-methyl-naphtho[2,3-c] |
|---|---|
| 规格或纯度 | ≥98% |
| 英文名称 | MS-444 |
| 生化机理 | MS-444 可抑制纯化的平滑肌肌球蛋白轻链激酶（MLCK）的活性，IC 50 值为 10 μM。 |
| 储存温度 | 避光,-20°C储存,充氩 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase ( MLCK ) with an IC 50 value of 10 μM. 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 IC 50 s 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 IC 50 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 (IC 50 =40.70±3.53 μM)) and colonic (YAMC (IC 50 =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 IC 50 values of 40.70 μM and 28.16 μM ( P <0.05). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Assay 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 IC 50. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal administration Mice Athymic nude (Nu/Nu) mice are used. HCT116 (2×10 6 cells) and HCA-7 (2.5×10 6 ) 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 . aladdin has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 10 μM (myosin) |
| 纯度 | ≥98% |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 5,8-dihydroxy-3-methyl-9H-benzo[f][2]benzofuran-4-one |
| 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 |
| InChi Key | TZUYDLKHNQUNKS-UHFFFAOYSA-N |
| Smiles | CC1=C2C(=CO1)CC3=C(C=CC(=C3C2=O)O)O |
| Isomeric SMILES | CC1=C2C(=CO1)CC3=C(C=CC(=C3C2=O)O)O |
| 关联CAS | 150045-18-4 |
| PubChem CID | 132904 |
| MeSH Entry Terms | 5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone;MS 444;MS-444 |
| 分子量 | 230.22 |
| 溶解性 | DMSO : 50 mg/mL (217.18 mM; Need ultrasonic) 1-Methyl-2-pyrrolidinone : 20 mg/mL (86.87 mM; Need ultrasonic) |
|---|---|
| 分子量 | 230.220 g/mol |
| XLogP3 | 2.700 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 4 |
| 可旋转键计数Rotatable Bond Count | 0 |
| 精确质量Exact Mass | 230.058 Da |
| 单同位素质量Monoisotopic Mass | 230.058 Da |
| 拓扑极表面积Topological Polar Surface Area | 70.700 Ų |
| 重原子数Heavy Atom Count | 17 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 329.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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