4-Methylumbelliferone

4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects. IC50 & Target: hyaluronic acid^[1] In Vitro: 4-Methylumbelliferone (4-MU) affects several key steps of angiogenesis, including endothelial cell proliferation, adhesion, tube formation, and extracellular matrix remodeling. Half-maximal inhibitory concentrations (IC₅₀) values in the proliferation assay are 0.65±0.04 and 0.37±0.03 mM for human microvascular endothelial cells (HMEC) and RF-24 endothelial cells, respectively. 4-Methylumbelliferone (2 mM) treatment for 24 h induces apoptosis in 13% of HMEC and 5% of RF-24 cells. The number of adherent endothelial cells decreases by >20% after 24 h of treatment with 1 mM 4-Methylumbelliferone. Minimal inhibitory concentrations in the tube formation assay are 2 and 0.5 mM 4-Methylumbelliferone for HMEC and RF-24, respectively. Matrix metalloproteinase-2 expression is differentially altered upon 4-Methylumbelliferone treatment in both tested endothelial cell lines^[1].