Biochem/physiol Actions

Reversible: yes

Primary TargetPin1

Cell permeable: yes

General description

A cell permeable thiuram monosulfide based compound that acts as a competitive inhibitor of Pin1 (EC₅₀ = 4.1 µM, K_i = 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).

A cell permeable thiuram monosulfide based compound that acts as a competitive inhibitor of Pin1 (EC₅₀ = 4.1 µM, K_i = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Yoon, W-J., et al. 2013. J. Cell Physiol.228, 2377.Tatara, Y., et al. 2009.Biochem Biophys Res Commun.384, 394.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)