Brefeldin A

Biological Activity

Brefeldin A is a reversible inhibitor of protein translocation from the endoplasmic reticulum (ER) to the Golgi apparatus. Blocks binding of ADP-ribosylation factor (ARF1) to the Golgi apparatus and inhibits GDP-GTP exchange, leading to activation of ER stress signaling pathways. Can be used to induce autophagy in mammalian cells. Also enhances CRISPR-mediated homology-directed repair (HDR) efficiency ~2-fold when applied at 100 nM, in human induced pluripotent stem cells (iPSCs). Antifungal.

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. Type I and type III interferons drive redundant amplification loops to induce a transcriptional signature in influenza-infected airway epithelia.
   Crotta S, Davidson S, Mahlakoiv T, Desmet C, Buckwalter M, Albert M, Staeheli P, Wack A
   PLoS Pathog, 2013;9(11):e1003773.
2. Systematic genetic mapping of necroptosis identifies SLC39A7 as modulator of death receptor trafficking
   A Fauster, M Rebsamen, KL Willmann, A César-Razq, E Girardi, JW Bigenzahn, F Schischlik, S Scorzoni, M Bruckner, J Konecka, K Hörmann, LX Heinz, K Boztug, G Superti-Fu
   Cell Death Differ., 2018;0(0):.
3. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
   Fox JT, Sakamuru S, Huang R
   Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
4. Role of calcium and EPAC in norepinephrine-induced ghrelin secretion.
   Mani B, Chuang J, Kjalarsdottir L, Sakata I, Walker A, Kuperman A, Osborne-Lawrence S, Repa J, Zigman J
   Endocrinology, 2014;155(1):98-107.
5. Small molecules enhance CRISPR genome editing in pluripotent stem cells.
   Yu et al.
   Cell Stem Cell, 2015;16:142
6. Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival.
   Ding et al.
   J.Biol.Chem., 2007;282:4702
7. Action of brefeldin A blocked by activation of a pertussis-toxin-sensitive G protein.
   Ktistakis et al.
   Nature, 1992;356:344
8. Isolation of a brefeldin A-inhibited guanine nucleotide-exchange protein for ADP ribosylation factor (ARF)1 and ARF3 that contains a Sec7-like domain.
   Morinaga et al.
   Proc.Natl.Acad.Sci.U.S.A., 1996;93:12856
9. Identification of a brefeldin A-insensitive guanine nucleotide-exchange protein for ADP-ribosylation factor in bovine brain.
   Tsai et al.
   Proc.Natl.Acad.Sci.U.S.A., 1994;91:3063

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