481417

CRAC Channel Inhibitor IV, EVP4593

The NF-κB Activation Inhibitor VIII, EVP4593 controls the biological activity of NF-κB. This small molecule/inhibitor is primarily used for Neuroscience applications.

• Sinónimos: CRAC Channel Inhibitor IV, EVP4593, N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
• Fórmula empírica (notación de Hill): C₂₂H₂₀N₄O
• Peso molecular: 356.42
• Número MDL: MFCD06411436
• Código UNSPSC: 12352200

Propiedades

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

Descripción

Descripción general

A cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-κB activation in Jurkat cells (IC₅₀ = 11 nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1 mg/kg, i.p.). In addition, it is shown to inhibit the store-operated calcium entry (SOC) pathway possibly by targeting TRPC1 containing heteromeric channels in Huntington Disease (HD) neurons (SK-N-SH cells transfected with mutant Huntingtin Htt-138Q) at 300 nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30 nM to 3 µM, which is consistent with TRPC1 knockdown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100 µM to 400 µM.

Envase

Packaged under inert gas

Advertencia

Toxicity: Regulatory Review (Z)

Reconstitución

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

Otras notas

Wu, J., et al. 2011. Chem Biol.18, 777.
Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 383.
Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 3869.

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