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Description

A cell permeable thiuram monosulfide based compound that acts as a competitive inhibitor of Pin1 (EC50 = 4.1 µ,M, Ki = 50 nM). Binds to the active site of the PPIase domain of Pin1 hydrophobically and blocks the active pocket. Shown to specifically inhibit peptidyl-prolyl cis/trans isomerase activity in HeLa cells. Inhibits the proliferation of HCT116 cells (EC50 = 10 µ,M) by arresting cell cycle at the G0 phase. Also shown to reduce the endogenous Runx2 protein levels in the MC3T3-E1 cells. Displays excellent solubility in DMSO (~100 mM)., A cell permeable thiuram monosulfide based compound that acts as a competitive inhibitor of Pin1 (EC50 = 4.1 µ,M, Ki = 50 nM). Binds to the active site of the PPIase domain of Pin1 hydrophobically and blocks the active pocket. Shown to specifically inhibit peptidyl-prolyl cis/trans isomerase activity in HeLa cells. Inhibits the proliferation of HCT116 cells (EC50 = 10 µ,M) by arresting cell cycle at the G0 phase. Also shown to reduce the endogenous Runx2 protein levels in the MC3T3-E1 cells. Displays excellent solubility in DMSO (~100 mM).Please note that the molecular weight for this compound is batch-specific due to variable water content.