Brefeldin A - STING Trafficking Inhibitor

InvitroFit™ PRR inhibitor

ABOUT

Inhibitor of STING trafficking

Brefeldin A (BFA) is a fungal macrocyclic lactone and a potent, reversible inhibitor of intracellular vesicle formation and protein trafficking between the endoplasmic reticulum (ER) and the Golgi apparatus [1]. BFA and its analogs are promising inhibitors in drug development due to a number of key features such as apoptosis‑inducing properties as well as antitumor, antifungal, and antiviral effects [2]. Interestingly, despite effectively impairing NLRP3 inflammasome activation, BFA does not block the release of IL-1β, for which the secretion mechanism remains elusive [3].

 

Mode of action:

The blocking of intracellular vesicle movement in BFA-treated cells causes the rapid accumulation of proteins in the ER, thereby disrupting the trafficking of many proteins. Hence, BFA is commonly utilized as an inhibitor of protein secretion in cellular assays.

BFA also effectively inhibits the secretion of cytokines by blocking the trafficking of upstream signaling proteins. BFA inhibits type I interferon (IFN) production by blocking the dissociation of activated STING (stimulator of interferon genes) from the ER. This prevents the movement of STING to the ER-Golgi intermediate compartment (ERGIC), where it activates the TBK1-IRF3 signaling axis, and ultimately triggers the expression of IFNs [4].

Key Features of Brefeldin A:

  • Brefeldin A is a potent inhibitor of protein trafficking from the ER to the Golgi apparatus.
  • Brefeldin A inhibits the translocation of STING to the ERGIC, thereby blocking STING-induced type I IFN production.
  • InvitroFit™: each lot of Brefeldin A is highly pure (≥95%) and functionally tested.


References:

1. Chardin, P. & McCormick, F. 1999. Brefeldin A: the advantage of being uncompetitive. Cell 97, 153-155.
2. Paek, S. M. 2018. Recent Synthesis and Discovery of Brefeldin A Analogs. Mar Drugs 16.
3. Hong, S. et al., 2019. Brefeldin A-sensitive ER-Golgi vesicle trafficking contributes to NLRP3-dependent caspase-1 activation. FASEB J 33, 4547-4558.
4. Dobbs, N. et al., 2015. STING Activation by Translocation from the ER Is Associated with Infection and Autoinflammatory Disease. Cell Host Microbe 18, 157-168.

All products are for research use only, and not for human or veterinary use.

InvitroFit™

InvitroFit™ is a high-quality standard specifically adapted for in vitro studies of inhibitors. InvitroFit™ products are highly pure (≥95%) and guaranteed free of bacterial contamination, as confirmed using HEK Blue™ TLR2 and HEK Blue™ TLR4 cellular assays. Each lot is rigorously tested for functional activity using validated (or proprietary) cellular models. This grade ensures reliability and reproducibility for your research applications.

SPECIFICATIONS

Specifications

Synonyms
BFA
CAS number
20350-15-6
Chemical formula

C16H24O4

Molecular weight
280.36 g/mol
Purity
≥ 95% (UHPLC)
Solubility

10 mg/ml in DMSO

Working concentration

1 - 10 μM for cell culture assays

Endotoxin

Negative (tested using EndotoxDetect™ assay)

Tested applications

In vitro cellular assays

Quality control

Each lot is functionally tested and validated using cellular assays.

CONTENTS

Contents

  • Product: 
    Brefeldin A
  • Cat code: 
    inh-bfa
  • Quantity: 
    10 mg
Notes:

Brefeldin A is provided as an evaporated translucent film.

Shipping & Storage

  • Shipping method:  Room temperature
  • Storage:

    • -20 °C
    Stability: The reconstituted product is stable up to 3 months at -20 °C.

    Caution:

    • Avoid repeated freeze-thaw cycles

Details

Chemical structure of Brefeldin A: 

Chemical structure of Brefeldin A

DOCUMENTS

Documents

Brefeldin A

Technical Data Sheet

Safety Data Sheet

Validation Data Sheet

Certificate of analysis

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