5.38339

HuR-ARE Interaction Inhibitor, CMLD-2

• Sinónimos: HuR-ARE Interaction Inhibitor, CMLD-2, 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one
• Fórmula empírica (notación de Hill): C₃₁H₃₁NO₆
• Peso molecular: 513.58
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

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

Descripción

Descripción general

A cell-permeable, 2H-chromen-2-one based compound that competitively binds to Hu antigen R (HuR; K_i = 350 nM) and disrupts the interaction of HuR and adenine- and uridine-rich element (ARE) of target mRNAs. Displays dose-dependent binding to full-length HuR protein and to RRM1/2 fragment. Exhibits cytotoxicity towards tumor cells and reduces their viability (IC₅₀ = 28.9 and 18.2 µM for HCT-116 and MioPaCa2 cells, respectively). Has much reduced effect on normal WI-38 and CCD 841 CoN cells. Shown to induce cleavage of poly (ADP-ribose) polymerase and pro-caspase 3 (~ 50 µM) and reduce the half-life of Bcl-2, Msi1, and XIAP in HCT-116 cells (~20 µM) treated with actinomycin D (5 µg/ml).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
HuR

Reversible: yes

Target K_i: 350 nM for HuR binding

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

Wu, X., et al. 2015. ACS Chem. Biol.10, 1476.

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