5.30618

Pin1 Inhibitor, DTM

• Sinónimos: Pin1 Inhibitor, DTM, PPIase-Parvulin Inhibitor II
• Fórmula empírica (notación de Hill): C₁₂H₂₀N₂S₃
• Número de CAS: 725-32-6
• Peso molecular: 288.50
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Análisis: ≥98% (HPLC)
• Nivel de calidad: 100
• formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 50 mg/mL
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
Pin1

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable