Merck, 5306180001, Pin1 Inhibitor, DTM

General description
A cell permeable thiuram monosulfide based compound that acts as a competitive inhibitor of Pin1 (EC₅₀ = 4.1 µM, 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 µM) 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Pin1
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Yoon, W-J., et al. 2013. J. Cell Physiol.228, 2377.
Tatara, Y., et al. 2009.Biochem Biophys Res Commun.384, 394.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)