Sigma-Aldrich Pin1 Inhibitor Dtm

Assay

≥98% (HPLC)

Quality Level

100

Form

powder

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

yellow

Solubility

DMSO: 50 mg/mL

Storage Temp.

2-8°C

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.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
Pin1Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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