5.09306

Late Endosome Trafficking Inhibitor, EGA

• Synonyme(s) : Late Endosome Trafficking Inhibitor, EGA, 4-Bromobenzaldehyde-N-(2,6-dimethylphenyl)semicarbazone, ( E)-2-(4-Bromobenzylidene)-N-(2,6-dimethylphenyl)hydrazinecarboxamide
• Formule empirique (notation de Hill): C₁₆H₁₆BrN₃O
• Numéro CAS: 415687-81-9
• Poids moléculaire : 346.22
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥93% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 5 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

A cell-permeable semicabazone compound that prevents B. anthrax Lethal toxin/LT (EC₅₀ = 1.7 µM in RAW264.7 cultures; EC_max = 6 µM in murine BMDM cultures), diphtheria toxin/DT, P. aeruginosa ExoA, and H. ducreyi cytolethal distending toxin (Hd-CDT) from exerting their cytotoxic activity, but not endocytic uptake, by blocking endosomal trafficking/maturation into acidified late endosomes, while exhibiting no cytoprotective efficacy against ricin & E. coli Ec-CDT that do not require acidified endosomes for intoxication. Likewise, EGA is also shown to inhibit low-pH-dependent viral infectivity by Armstrong strain of LCMV, A/WSN/33 strain of influenza virus, but not low-pH-independent infection of Nipah virus NiV or MLV. Although the exact molecular target remains unknown, EGA does not act as a pH neutralizing agent, nor does it inhibit endosomal recycling or trafficking to phagocytic compartments.

A cell-permeable semicarbazone compound that prevents B. anthrax Lethal toxin/LT (Protective Antigen/PA & LF/Lethal Factor complex; EC₅₀ = 1.7 µM in RAW264.7 cultures; EC_max = 6 µM in murine BMDM cultures), diphtheria toxin (DT), LF-DT A chain fusion LFnDTA/PA complex, P. aeruginosa ExoA, and H. ducreyi cytolethal distending toxin (Hd-CDT) from exerting their cytotoxic activity, but not endocytic uptake, by blocking endosomal trafficking/maturation into acidified late endosomes, while exhibiting no cytoprotective efficacy against toxins that do not require acidified endosomes for intoxication, such as ricin & E. coli Ec-CDT. Likewise, EGA is also shown to inhibit low-pH-dependent viral infectivity by Armstrong strain of LCMV, A/WSN/33 strain of influenza virus, vesicular stomatitis virus VSV-pseudotyped lentivirus & VSV-pseudotyped MLV, but not low-pH-independent infection of Nipah virus NiV or MLV. Although the exact molecular target remains unknown, EGA does not act as a pH neutralizing agent, nor does it inhibit endosomal recycling or trafficking to phagocytic compartments.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
host-membrane trafficking

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Use only fresh DMSO for reconstitution.

Autres remarques

Gillespie, E.J., et al. 2013. Proc. Natl. Acad. Sci. USA110, E4904.

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
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable