Description
InformationML364 is a small molecule inhibitor of thedeubiquitinase USP2with an IC50 of 1.1 µM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.TargetsUSP8 (Cell-free assay); USP2 (Cell-free assay) 0.95 µM; 1.1 µMIn vitroML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 µM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 µM ML364.Cell Research(from reference)Cell lines:LnCAP cells and MCF7 cells Concentrations:0-20 µM Incubation Time:24 h