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.

• Synonyme(s) : CRAC Channel Inhibitor IV, EVP4593, N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
• Formule empirique (notation de Hill): C₂₂H₂₀N₄O
• Poids moléculaire : 356.42
• Numéro MDL: MFCD06411436
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 100 mg/mL, clear, yellow
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Regulatory Review (Z)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3