5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone
MS-444
CAS: 150045-18-4
Molecular Formula: C13H10O4
5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone - Names and Identifiers
| Name | MS-444 |
| Synonyms | MS-444 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- |
| CAS | 150045-18-4 |
5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone - Physico-chemical Properties
| Molecular Formula | C13H10O4 |
| Molar Mass | 230.22 |
| Density | 1.452±0.06 g/cm3(Predicted) |
| Boling Point | 448.7±45.0 °C(Predicted) |
| pKa | 8.14±0.20(Predicted) |
| Storage Condition | 2-8°C，密封，干燥 |
| In vitro study | 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). |
| In vivo study | 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. |
5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone - Reference Information
| biological activity | MS-444 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μm. |
| Target | IC50: 10 μm (myosin). |
Last Update：2024-04-10 22:29:15
