Gliotoxin

Biological Activity

Gliotoxin is an immunosuppressive agent; blocks phagocytosis, cytokine production and proliferation of T and B cells. Non-competitively inhibits chymotrypsin-like activity of 20S proteasome; prevents degradation of IκBα, an endogenous blocker of NF-κB. Inhibits leukotriene B₄ (LTB₄) biosynthesis via inhibition of LTA₄ hydrolase. Also inhibits farnesyltransferase and geranylgeranyltransferase I (IC₅₀ values are 80 and 17 μM respectively) and displays antitumor activity against breast cancer in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Gliotoxin and related epipolythiodioxopiperazines.
   Waring and Beaver
   Gen.Pharmacol., 1996;27:1311
2. In vitro and in vivo effects of gliotoxin, a fungal metabolite: efficacy against dextran sodium sulfate-induced colitis in rats.
   Fitzpatrick et al.
   Dig.Dis.Sci., 2000;45:2327
3. Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumour activity against breast cancer in vivo.
   Vigushin et al.
   Med.Oncol., 2004;21:21
4. Gliotoxin from Aspergillus fumigatus abrogates leukotriene B₄ formation through inhibition of leukotriene A₄ hydrolase.
   König et al.
   Cell Chem.Biol., 2019;26:524

Product Datasheets