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
• MDL number: MFCD02258932
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥93% (HPLC)
• Form: powder
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: ≥93% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C

Beschreibung

General description

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 Actions

Cell permeable: yes

Primary Target
host-membrane trafficking

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Use only fresh DMSO for reconstitution.

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable