150045-18-4
150045-18-4 structure
- Name: MS-444
- Chemical Name: 5,8-dihydroxy-3-methyl-9H-benzo[f][2]benzofuran-4-one
- CAS Number: 150045-18-4
- Molecular Formula: C13H10O4
- Molecular Weight: 230.21600
- Catalog: Signaling Pathways Cytoskeleton Myosin
- Create Date: 2018-06-10 14:52:12
- Modify Date: 2024-01-09 20:23:03
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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.
| Name | 5,8-dihydroxy-3-methyl-9H-benzo[f][2]benzofuran-4-one |
|---|---|
| Synonyms |
ms 444
5,8-dihydroxy-3-methyl-4-(9H)-naphtho(2,3-c)furanone MS-444 |
| Description | MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM. |
|---|---|
| Related Catalog | |
| Target |
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<0.05)[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]. |
| 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 IC50[2]. |
| Animal Admin | 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]. |
| References |
| Density | 1.452g/cm3 |
|---|---|
| Boiling Point | 448.7ºC at 760mmHg |
| Molecular Formula | C13H10O4 |
| Molecular Weight | 230.21600 |
| Flash Point | 225.2ºC |
| Exact Mass | 230.05800 |
| PSA | 70.67000 |
| LogP | 2.13440 |
| Vapour Pressure | 1.15E-08mmHg at 25°C |
| Index of Refraction | 1.673 |