Retro-2

A cell-permeable tricyclic imine compound that inhibits the endosome-to-Golgi retrograde transport, but not cellular uptake, of CtxB (Cholera toxin B chain), StxB (Shiga-like toxin B chain), and the plant toxin ricin from castor seed in HeLa cells (20 µM), without affecting cellular uptake and trafficking of Tf (Transferrin), EGF, and vesicular stomatitis virus glycoprotein VSVG^ts045. Retro-2 is demonstrated to selectively affect the cellular distribution of SNARE proteins Synt5 and Synt6, but not 24 other Golgi and endocytic pathway proteins. Retro-2 pretreatment is shown to effectively protect against ricin-, Stx1-, and Stx2-induced cytotoxicity in HeLa cultures in vitro (Fold of protection against 4 h toxin incubation = 2.7, 22, and 65, respectively, with 0.5 h 20 µM Retro-2 pretreatment), as well as ricin-induced (2 µg/kg by nasal spray) fatality in mice in vivo (0 mortality with one 200 mg/kg i.p. dose 1h prior to toxin exposure).

Toxicity: Standard Handling (A)

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

It is recommended to prepare a stock solution for 3 month use each time and store the unreconstituted material in solid form, protected from moisture and preferably under inert gas, for best long-term stability during storage.

Stechmann, B., et al. 2010. Cell141, 231.

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