150045-18-4
基本信息
化合物 T16145
BE-34776
5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone
Naphtho[2,3-c]furan-4(9H)-one, 5,8-dihydroxy-3-methyl-
物理化学性质
| 沸点 | 448.7±45.0 °C(Predicted) |
| 密度 | 1.452±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 8.14±0.20(Predicted) |
| 形态 | Solid |
| 颜色 | Light yellow to brown |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
常见问题列表
IC50: 10 μM (myosin).
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).
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.