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GEF inhibitor
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
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Product Details
| Alternative Name |
BFA, Ascotoxin, Decumbin |
|---|---|
| Appearance |
White to off-white solid. |
| CAS |
20350-15-6 |
| Couple Target |
GEF |
| Couple Type |
Inhibitor |
| Formula |
C16H24O4 |
| MI |
14: 1369 |
| MW |
280.4 |
| Purity |
≥98% (HPLC) |
| Solubility |
Soluble in DMSO (20mg/ml), 100% ethanol (5mg/ml), methanol, acetone or ethyl acetate (1mg/ml). |
| Source |
Isolated from Eupenicillium brefeldianum. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- SMARCA4 regulates the NK-mediated killing of senescent cells: Reen, V., D’Ambrosio, M., et al.; Sci. Adv. 11, eadn2811 (2025), Abstract
- TL1A and IL-18 synergy promotes GM-CSF-dependent thymic granulopoiesis in mice: Ruiz Perez, M., Maueröder, C., et al.; Cell. Mol. Immunol. 21, 807 (2024), Abstract
- Oropouche virus glycoprotein topology and cellular requirements for glycoprotein secretion: N.S. Barbosa, et al.; J. Virol. 97, e0133122 (2023), Abstract
- Nicotinamide-Expanded Allogeneic Natural Killer Cells with CD38 Deletion, Expressing an Enhanced CD38 Chimeric Antigen Receptor, Target Multiple Myeloma Cells: Edri, A., Ben-Haim, N., et al.; Int. J. Mol. Sci. 24, (2023), Abstract
- PIM kinases regulate early human Th17 cell differentiation: T. Buchacher, et al.; Cell Rep. 42, 113469 (2023), Abstract
- Proteomic Profiling and Functional Analysis of B Cell-Derived Exosomes upon Pneumocystis Infection: D. Ma, et al.; J. Immunol. Res. 2022, 5187166 (2022), Abstract
- The ZFP36 family of RNA binding proteins regulates homeostatic and autoreactive T cell responses: M.E. Cook, et al.; Sci. Immunol. 7, eabo0981 (2022), Abstract
- Priming of myelin-specific T cells in the absence of dendritic cells results in accelerated development of Experimental Autoimmune Encephalomyelitis: Luu, T., Cheung, J. F., et al.; PLoS One 16, e0250340 (2021), Abstract
- Proteostasis regulators restore function of epilepsy-associated GABAA receptors: X. Di, et al.; Cell Chem. Biol. 28, 46 (2021), Abstract — Full Text
- TLR agonists enhance responsiveness of inflammatory innate immune cells in HLA-B*57-positive HIV patients: L. Dold, et al.; J. Mol. Med. (Berl.) 99, 147 (2021), Application(s): TLR activation of monocytes and NK cells, Abstract — Full Text
- Shp-2 is critical for ERK and metabolic engagement downstream of IL-15 receptor in NK cells: C. Niogret, et al.; Nat. Commun. 10, 1444 (2019), Abstract — Full Text
- Intracellular trafficking of begomoviruses in the midgut cells of their insect vector: Xia, W. Q., Liang, Y., et al.; PLoS Pathog. 14, e1006866 (2018), Abstract
- Mesenchymal stem cells alleviate experimental autoimmune cholangitis through immunosuppression and cytoprotective function mediated by galectin-9: J. Fan, et al.; Stem Cell Res. Ther. 9, 237 (2018), Abstract
- Mesenchymal stem cells induced CD4+ T cell apoptosis in treatment of lupus mice: S. Huang, et al.; Biochem. Biophys. Res. Commun. 507, 30 (2018), Abstract
- Puerarin attenuates smoke inhalation injury by regulation of Th1/Th2 expression and inhibition of Th17 cells in rats: F. Zhang, et al.; Int. Immunopharmacol. 28, 546 (2015), Application(s): Cell culture , Abstract
- Limited Applicability of GW9662 to Elucidate PPARγ-Mediated Fatty Acid Effects in Primary Human T-Helper Cells: Jaudszus, A., Lorkowski, S., et al.; Int. J. Inflam. 2014, 149628 (2014), Abstract
- Wnt5a directs polarized calcium gradients by recruiting cortical endoplasmic reticulum to the cell trailing edge: Witze, E. S., Connacher, M. K., et al.; Dev. Cell 26, 645 (2013), Abstract
- Evaluation of suppressive and pro-resolving effects of EPA and DHA in human primary monocytes and T-helper cells: Jaudszus, A., Gruen, M., et al.; J. Lipid Res. 54, 923 (2013), Abstract
- Arf6-dependent intracellular trafficking of Pasteurella multocida toxin and pH-dependent translocation from late endosomes: Repella, T. L., Ho, M., et al.; Toxins (Basel) 3, 218 (2011), Abstract
- Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005), Abstract
- NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003), Abstract — Full Text
- Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review, Abstract
- Brefeldin A: the advantage of being uncompetitive: P. Chardin & F. McCormick; Cell 97, 153 (1999), Abstract
- Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996), Abstract
- Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996), Abstract
- Activation of ADP-ribosylation factor by Golgi membranes. Evidence for a brefeldin A- and protease-sensitive activating factor on Golgi membranes: P.A. Randazzo, et al.; J. Biol. Chem. 268, 9555 (1993), Abstract
- Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993), Abstract
- Inhibition by brefeldin A of a Golgi membrane enzyme that catalyses exchange of guanine nucleotide bound to ARF: J.B. Helms & J.E. Rothman; Nature 360, 352 (1992), Abstract
- Brefeldin A inhibits Golgi membrane-catalysed exchange of guanine nucleotide onto ARF protein: J.G. Donaldson, et al.; Nature 360, 350 (1992), Abstract
- Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992), Abstract
- Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review), Abstract
- Brefeldin A, a drug that blocks secretion, prevents the assembly of non-clathrin-coated buds on Golgi cisternae: L. Orci, et al.; Cell 64, 1183 (1991), Abstract
- Guanine nucleotides modulate the effects of brefeldin A in semipermeable cells: regulation of the association of a 110-kD peripheral membrane protein with the Golgi apparatus: J.G. Donaldson, et al.; J. Cell Biol. 112, 579 (1991), Abstract
- Binding of ARF and beta-COP to Golgi membranes: possible regulation by a trimeric G protein: J.G. Donaldson, et al.; Science 254, 1197 (1991), Abstract
- Microtubule-dependent retrograde transport of proteins into the ER in the presence of brefeldin A suggests an ER recycling pathway: J. Lippincott-Schwartz, et al.; Cell 60, 821 (1990), Abstract
- Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988), Abstract — Full Text
- Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986), Abstract — Full Text
- Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
- Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958), Abstract
Last modified: May 29, 2024
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