5.09306

Late Endosome Trafficking Inhibitor, EGA

• Synonym(e): Late Endosome Trafficking Inhibitor, EGA, 4-Bromobenzaldehyde-N-(2,6-dimethylphenyl)semicarbazone, ( E)-2-(4-Bromobenzylidene)-N-(2,6-dimethylphenyl)hydrazinecarboxamide
• Empirische Formel (Hill-System): C₁₆H₁₆BrN₃O
• CAS-Nummer: 415687-81-9
• Molekulargewicht: 346.22
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥93% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 5 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
host-membrane trafficking

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Use only fresh DMSO for reconstitution.

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable