Cat. No.: HY-16592

Brefeldin A

(Synonyms: BFA; Cyanein; Decumbin)

170 Cited Publications

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Based on 170 publication(s) in Google Scholar

Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A inhibits HSV-1 and has anti-cancer activity.

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Pureté: 99.82%
CAS No.: 20350-15-6
Formule: C₁₆H₂₄O₄
Masse moléculaire:280.36

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Brefeldin A Chemical Structure

CAS No.: 20350-15-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (170)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
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Activité biologique

Description

Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus^[1]^[2]. Brefeldin A is also an autophagy and mitophagy inhibitor^[3]. Brefeldin A inhibits HSV-1 and has anti-cancer activity^[5].

IC₅₀ & Target^[5]^[6]

HSV-1

Voir tous les produits spécifiques à Isoform HSV :

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Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.039 μM Compound: BFA	Antiproliferative activity against human A-375 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human A-375 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
A549	GI₅₀	0.04 μM Compound: 1	Antiproliferative activity against human A549 cell line Antiproliferative activity against human A549 cell line	[PMID: 16789745]
A549	IC₅₀	0.056 μM Compound: BFA	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
Bel-7402	IC₅₀	0.024 μM Compound: BFA; 1	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 29524728]
Bel-7402	IC₅₀	0.17 μM Compound: 1; BFA	Antiproliferative activity against human Bel-7402 cells measured after 72 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells measured after 72 hrs by MTT assay	[PMID: 35849940]
Bel-7402	IC₅₀	0.07 μM Compound: BFA	Antiproliferative activity against human Bel-7402 cells by MTT assay Antiproliferative activity against human Bel-7402 cells by MTT assay	[PMID: 36089748]
Bel7402/5-FU	IC₅₀	0.82 μM Compound: BFA; 1	Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay	[PMID: 29524728]
DU-145	GI₅₀	0.13 μM Compound: 1	Antiproliferative activity against human prostate DU-145 cancer cell line Antiproliferative activity against human prostate DU-145 cancer cell line	[PMID: 11689077]
DU-145	IC₅₀	0.16 μM Compound: BFA	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
DU-145	GI₅₀	0.13 μM Compound: 1	Cytotoxicity against prostate DU-145 cancer cell cultures. Cytotoxicity against prostate DU-145 cancer cell cultures.	[PMID: 9719586]
ECa-109 cell line	IC₅₀	0.14 μM Compound: 1; BFA	Antiproliferative activity against human Eca-109 cells measured after 72 hrs by MTT assay Antiproliferative activity against human Eca-109 cells measured after 72 hrs by MTT assay	[PMID: 35849940]
HCT-116	GI₅₀	0.029 μM Compound: 1	Antiproliferative activity against human colon HCT116 cancer cell line Antiproliferative activity against human colon HCT116 cancer cell line	[PMID: 11689077]
HCT-116	GI₅₀	0.03 μM Compound: 1	Antiproliferative activity against HCT116 cell line Antiproliferative activity against HCT116 cell line	[PMID: 16789745]
HCT-116	GI₅₀	0.029 μM Compound: 1	Cytotoxicity against colon HCT116 cancer cell cultures. Cytotoxicity against colon HCT116 cancer cell cultures.	[PMID: 9719586]
HeLa	EC₅₀	5 μM Compound: Brefeldin A	Inhibition of Escherichia coli Stx1 in human HeLa cells assessed as stimulation of protein synthesis by measuring increase in [14C]-leucine incorporation incubated with cells for 1 hr prior to Stx1 addition and further incubated for 1 to 24 hrs and subseq Inhibition of Escherichia coli Stx1 in human HeLa cells assessed as stimulation of protein synthesis by measuring increase in [14C]-leucine incorporation incubated with cells for 1 hr prior to Stx1 addition and further incubated for 1 to 24 hrs and subseq	[PMID: 32648758]
HeLa	IC₅₀	0.07 μM Compound: 1; BFA	Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay	[PMID: 35849940]
HeLa	IC₅₀	0.044 μM Compound: BFA	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
HepG2	IC₅₀	0.35 μM Compound: 1; BFA	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 28494251]
HepG2	IC₅₀	0.18 μM Compound: 1; BFA	Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay	[PMID: 35849940]
HepG2	IC₅₀	0.08 μM Compound: BFA	Antiproliferative activity against human HepG2 cells by MTT assay Antiproliferative activity against human HepG2 cells by MTT assay	[PMID: 36089748]
HepG2	IC₅₀	0.12 μM Compound: BFA	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
HL-60	IC₅₀	0.025 μM Compound: BFA; 1	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 29524728]
HOP-62	GI₅₀	0.07 μM Compound: 1	Antiproliferative activity against human lung HOP-62 cancer cell line Antiproliferative activity against human lung HOP-62 cancer cell line	[PMID: 11689077]
HOP-62	GI₅₀	0.07 μM Compound: 1	Cytotoxicity against lung HOP-62 cancer cell cultures. Cytotoxicity against lung HOP-62 cancer cell cultures.	[PMID: 9719586]
HT-29	IC₅₀	0.16 μM Compound: 1; BFA	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28494251]
L02	IC₅₀	<0.0004 μM Compound: 1; BFA	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28494251]
L02	IC₅₀	<0.4 nM Compound: 1; BFA	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28494251]
L02	IC₅₀	<0.001 μM Compound: BFA; 1	Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay	[PMID: 29524728]
L02	IC₅₀	0.1 μM Compound: 1; BFA	Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay	[PMID: 35849940]
L02	IC₅₀	0.094 μM Compound: BFA	Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
MCF7	GI₅₀	0.02 μM Compound: 1	Antiproliferative activity against human MCF7 cell line Antiproliferative activity against human MCF7 cell line	[PMID: 16789745]
MDA-MB-231	IC₅₀	0.054 μM Compound: BFA	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by CCk-8 assay	[PMID: 37329677]
MDA-MB-435	GI₅₀	0.041 μM Compound: 1	Antiproliferative activity against human breast MDA-MB-435 cancer cell line Antiproliferative activity against human breast MDA-MB-435 cancer cell line	[PMID: 11689077]
MDA-MB-435	GI₅₀	0.041 μM Compound: 1	Cytotoxicity against breast MDA-MB-435 cancer cell cultures. Cytotoxicity against breast MDA-MB-435 cancer cell cultures.	[PMID: 9719586]
OVCAR-3	GI₅₀	0.032 μM Compound: 1	Antiproliferative activity against human ovarian OVCAR-3 cancer cell line Antiproliferative activity against human ovarian OVCAR-3 cancer cell line	[PMID: 11689077]
OVCAR-3	GI₅₀	0.03 μM Compound: 1	Antiproliferative activity against human OVCAR-3 cell line Antiproliferative activity against human OVCAR-3 cell line	[PMID: 16789745]
OVCAR-3	GI₅₀	0.032 μM Compound: 1	Cytotoxicity against ovarian OVCAR-3 cancer cell cultures. Cytotoxicity against ovarian OVCAR-3 cancer cell cultures.	[PMID: 9719586]
PANC-1	IC₅₀	0.08 μM Compound: 1; BFA	Antiproliferative activity against human PANC-1 cells measured after 72 hrs by MTT assay Antiproliferative activity against human PANC-1 cells measured after 72 hrs by MTT assay	[PMID: 35849940]
Panel NCI-60 (60 carcinoma cell lines)	GI₅₀	0.04 μM Compound: 1	Antiproliferative activity against NCI60 cell line Antiproliferative activity against NCI60 cell line	[PMID: 16789745]
PC-3	GI₅₀	0.05 μM Compound: 1	Antiproliferative activity against human PC3 cell line Antiproliferative activity against human PC3 cell line	[PMID: 16789745]
PC-3	IC₅₀	0.068 μM Compound: 1; BFA	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 28494251]
PC-3	IC₅₀	0.068 μM Compound: BFA; 1	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29524728]
SF-539	GI₅₀	0.04 μM Compound: 1	Antiproliferative activity against human CNS SF-539 cancer cell line Antiproliferative activity against human CNS SF-539 cancer cell line	[PMID: 11689077]
SF-539	GI₅₀	0.04 μM Compound: 1	Antiproliferative activity against human SF539 cell line Antiproliferative activity against human SF539 cell line	[PMID: 16789745]
SF-539	GI₅₀	0.04 μM Compound: 1	Cytotoxicity against CNS SF-539 cancer cell cultures. Cytotoxicity against CNS SF-539 cancer cell cultures.	[PMID: 9719586]
SN12C	GI₅₀	0.09 μM Compound: 1	Antiproliferative activity against human renal SN12C cancer cell line Antiproliferative activity against human renal SN12C cancer cell line	[PMID: 11689077]
SN12C	GI₅₀	0.09 μM Compound: 1	Antiproliferative activity against human SN12C cell line Antiproliferative activity against human SN12C cell line	[PMID: 16789745]
SN12C	GI₅₀	0.09 μM Compound: 1	Cytotoxicity against renal SN12C cancer cell cultures. Cytotoxicity against renal SN12C cancer cell cultures.	[PMID: 9719586]
UACC-62	GI₅₀	0.022 μM Compound: 1	Antiproliferative activity against human melanoma UACC-62 cancer cell line Antiproliferative activity against human melanoma UACC-62 cancer cell line	[PMID: 11689077]
UACC-62	GI₅₀	0.02 μM Compound: 1	Antiproliferative activity against human UACC62 cell line Antiproliferative activity against human UACC62 cell line	[PMID: 16789745]
UACC-62	GI₅₀	0.022 μM Compound: 1	Cytotoxicity against melanoma UACC-62 cancer cell cultures. Cytotoxicity against melanoma UACC-62 cancer cell cultures.	[PMID: 9719586]

In Vitro

Brefeldin A (BFA) treatment for 15 h or 40 h, causes dramatic swelling of the Endoplasmic Reticulum (ER) and shifts its localization to the periphery of normal rat kidney (NRK) cells. Prolonged Brefeldin A treatment results in marked disruption of the MT and actin cytoskeleton^[1]. ADP-ribosylation of BARS is mediated by formation of a conjugate between Brefeldin A and ADPR. BARS shows BAC binding when incubated with the medium from the BFA-treated CD38⁺ HeLa cells^[3]. Brefeldin A induces anchorage-independent cell death in MDA-MB-231 breast cancer cells, inhibits the formation of MDA-MB-231 colonies in 3D and 2D cultures and inhibits the migration and MMP 9 (Matrix Metallopeptidase 9) activity of MDA-MB-231^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 20350-15-6
Appearance Solid
Masse moléculaire 280.36
Formule C₁₆H₂₄O₄
Color White to off-white
SMILES

O[C@@H]1C[C@]2([H])[C@@](/C=C/CCC[C@H](C)OC(/C=C/[C@H]2O)=O)([H])C1
Synonyms

BFA; Cyanein; Decumbin
Structure Classification
- Antibiotics
- Macrolide Antibiotics
Initial Source
- Microorganisms
Penicillium
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (170)

All Cell Proliferation/Viability AssayWBIPRT-PCR

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Signal Transduct Target Ther

Incorporation of a Toll-like receptor 2/6 agonist potentiates mRNA vaccines against cancer and infectious diseases. [Abstract]

2023 Jul 17;8(1):273. PMID: 37455272
Nature

Microglia-neuron crosstalk through Hex-GM2-MGL2 maintains brain homeostasis. [Abstract]

2025 Oct;646(8086):913-924. PMID: 40769205
Cell

STING signaling modulation by COPII cargo recognition. [Abstract]

2026 May 14;189(10):2971-2987.e19. PMID: 41887218
Cell

Systemic immune activity occurs during human immune system maturation. [Abstract]

2025 Dec 11;188(25):7291-7308.e23. PMID: 41161316
Nat Biotechnol

A rapid imaging-based screen for induced-proximity degraders identifies a potent degrader of oncoprotein SKP2. [Abstract]

2025 Sep 10. PMID: 40931108
Cell Metab

Uridine depletion impairs CD8⁺ T cell antitumor activity through N-glycosylation. [Abstract]

2025 Dec 29:S1550-4131(25)00530-3. PMID: 41468885
Immunity

A chemical agonist and the Golgi-resident lipid PI4P activate STING by inducing transmembrane helix rearrangement. [Abstract]

2025 Dec 5:S1074-7613(25)00506-0. PMID: 41352342
Cancer Discov

A High-Fiber Plant-Based Diet in Myeloma Precursor Disorders - Results from the NUTRIVENTION Clinical Trial and Preclinical Vk*MYC Model. [Abstract]

2025 Dec 4. PMID: 41342739
Adv Mater

Fueling IgA-Dominated Humoral Immunity with an Intranasal Hybrid Tumor Vaccine to Opsonize and Strike Epithelial Breast Cancer. [Abstract]

2025 Sep;37(35):e2500631. PMID: 40589412
Nat Cancer

Palmitoylation of GPX4 via the targetable ZDHHC8 determines ferroptosis sensitivity and antitumor immunity. [Abstract]

2025 May;6(5):768-785. PMID: 40108413
Nat Metab

Hydrogen sulfide produced by the gut microbiota impairs host metabolism via reducing GLP-1 levels in male mice. [Abstract]

2024 Aug;6(8):1601-1615. PMID: 39030389

Brefeldin A purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Aug;6(8):1601-1615. [Abstract]

Brefeldin A (0.5 μg/mL; 12 h) significantly induces the expression of Xbp1s and reduces the expression of Gcg in GLUTag and GLARE cells.
Nat Biomed Eng

Modular nucleic acid-based construct for delivery of immunostimulatory agonists and oncogene-silencing oligonucleotides in tumours. [Abstract]

2026 Jun 3. PMID: 42236980
Nat Biomed Eng

Low-input deep learning platform for citrullinated peptide identification, autoantigen discovery and rheumatoid arthritis treatment stratification. [Abstract]

2026 Mar 3. PMID: 41776034
Cell Mol Immunol

Oncolytic virus M1 reinvigorates CD8+ T-cell immunity against glioblastoma through B-cell-dependent antigen cross-presentation in the spleen. [Abstract]

2026 Apr;23(4):349-366. PMID: 41781696
Cell Host Microbe

Microbiota-derived urocanic acid triggered by tyrosine kinase inhibitors potentiates cancer immunotherapy efficacy. [Abstract]

2025 Jun 11;33(6):915-931.e9. PMID: 40441145
Cancer Res

Extracellular Vesicle-Packaged miR-99a Reprograms Fibroblasts to Create an Inflammatory Niche that Drives Colorectal Cancer Metastasis. [Abstract]

2025 Sep 24. PMID: 40991395
Cancer Res

Androgen Signaling Contributes to Sex Differences in Cancer by Inhibiting NF-κB Activation in T Cells and Suppressing Anti-Tumor Immunity. [Abstract]

2023 Mar 15;83(6):906-921. PMID: 36634207
Cancer Res

Interaction with CD68 and Regulation of GAS6 Expression by Endosialin in Fibroblasts Drives Recruitment and Polarization of Macrophages in Hepatocellular Carcinoma. [Abstract]

2020 Sep 15;80(18):3892-3905. PMID: 32591411
Nat Microbiol

Multi-omics analyses of airway host-microbe interactions in chronic obstructive pulmonary disease identify potential therapeutic interventions. [Abstract]

2022 Sep;7(9):1361-1375. PMID: 35995842
Autophagy

Organelle contact reorganization drives calcium-dependent autophagy under proteostatic stress. [Abstract]

2026 Jun 6:1-20. PMID: 42152515
Autophagy

Trans-Golgi network-associated noncanonical autophagy depends on the V-ATPase-ATG16L1 axis and mediates IL1B secretion. [Abstract]

2025 Dec 8. PMID: 41361996
Autophagy

PLK2-mediated phosphorylation of SQSTM1 S349 promotes aggregation of polyubiquitinated proteins upon proteasomal dysfunction. [Abstract]

2024 Oct;20(10):2221-2237. PMID: 39316746

Brefeldin A purchased from MedChemExpress. Usage Cited in: Autophagy. 2024 Oct;20(10):2221-2237. [Abstract]

Brefeldin A (100 nM; 6 h) promotes upregulation of PLK2 protein in MDA-MB-231 cells.
Nat Commun

Microbiome modulation uncouples efficacy and toxicity induced by immune checkpoint blockade in mouse multiple myeloma. [Abstract]

2025 Nov 24;16(1):10384. PMID: 41285849
Nat Commun

Clustering of NLRP3 induced by membrane or protein scaffolds promotes inflammasome assembly. [Abstract]

2025 May 27;16(1):4887. PMID: 40425567
Nat Commun

Berberine-inspired ionizable lipid for self-structure stabilization and brain targeting delivery of nucleic acid therapeutics. [Abstract]

2025 Mar 10;16(1):2368. PMID: 40064874
Nat Commun

The adaptor protein AP-3β disassembles heat-induced stress granules via 19S regulatory particle in Arabidopsis. [Abstract]

2025 Feb 27;16(1):2039. PMID: 40016204
Nat Commun

Phytoalexin sakuranetin attenuates endocytosis and enhances resistance to rice blast. [Abstract]

2024 Apr 23;15(1):3437. PMID: 38653755
Nat Commun

Oncolytic viruses engineered to enforce cholesterol efflux restore tumor-associated macrophage phagocytosis and anti-tumor immunity in glioblastoma. [Abstract]

2023 Jul 20;14(1):4367. PMID: 37474548
ACS Nano

Combinatorial Design of Fatty Acid-Incorporated Plasmid Lipid Nanoparticles Drives Dendritic Cell Hyperactivation for Enhanced Cancer Immunotherapy. [Abstract]

2026 May 5;20(17):13196-13212. PMID: 42003370
Trends Biotechnol

Highly efficient prime editors for mammalian genome editing based on porcine retrovirus reverse transcriptase. [Abstract]

2025 Aug 30:S0167-7799(25)00314-2. PMID: 40885667
Gut Microbes

Synergistic activity of Enterococcus Faeciu m-induced ferroptosis via expansion of IFN-γ+CD8+ T cell population in advanced hepatocellular carcinoma treated with sorafenib. [Abstract]

2024 Jan-Dec;16(1):2410474. PMID: 39353096
J Nanobiotechnology

Targeting heptad repeats and fusion peptide: nanoparticle vaccine elicits mucosal immune response against SARS-CoV-2 variants. [Abstract]

2025 Jul 3;23(1):483. PMID: 40611257
Theranostics

Microbial and genetic-based framework identifies drug targets in inflammatory bowel disease. [Abstract]

2021 Jun 1;11(15):7491-7506. PMID: 34158863

Brefeldin A purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jun 1;11(15):7491-7506. [Abstract]

Brefeldin A (BFA, 0.01-50 μM; 24 h) shows less cytotoxicity in SW480 human colon cancer cell line (IC₅₀=4.652 µM) than that in DLD-1 cells (IC₅₀=0.167 µM).

Brefeldin A purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jun 1;11(15):7491-7506. [Abstract]

Brefeldin A (BFA; 2.5-10 mg/kg; i.p., every other day for two doses) suppresses cGAS expression in DSS-induced acute colitis mice.
Acta Pharm Sin B

Macrophage P2Y6R activation aggravates psoriatic inflammation through IL-27-mediated Th1 responses. [Abstract]

2024 Oct;14(10):4360-4377. PMID: 39525587
J Clin Invest

A CD4+ T lymphocyte-specific TCR/GSDMD/IL-2 axis facilitates antitumor immunity. [Abstract]

2025 Aug 1;135(15):e191119. PMID: 40759573
J Exp Clin Cancer Res

Membrane RRM2-positive cells represent a malignant population with cancer stem cell features in intrahepatic cholangiocarcinoma. [Abstract]

2024 Sep 6;43(1):255. PMID: 39243109
Adv Sci (Weinh)

Biomimetic Macrophage Cell Membrane-Based Nanoparticles for Effective Treatment of Glioblastoma Through Boron Neutron Capture Therapy Combined With Immunotherapy. [Abstract]

2026 Jun 22:e76216. PMID: 42328759
Adv Sci (Weinh)

CCDC41 Drives Oocyte Meiotic Progression by Promoting Rab11a/Rab7-Positive Vesicle Fusion with Target Membranes. [Abstract]

2025 Dec 2:e04665. PMID: 41331237
Adv Sci (Weinh)

Repurposing Cardiac Glycosides to Potentiate CD47 Blockade through Calreticulin-mediated Phagocytic Effects for Lung Cancer Treatment. [Abstract]

2025 Sep 23:e08245. PMID: 40985476
Adv Sci (Weinh)

siRNA/CS-PLGA Nanoparticle System Targeting Knockdown Intestinal SOAT2 Reduced Intestinal Lipid Uptake and Alleviated Obesity. [Abstract]

2024 Oct;11(40):e2403442. PMID: 39297413

Brefeldin A purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(40):e2403442. [Abstract]

Brefeldin A significantly promotes CD36 ubiquitination in Caco2 cells.
MedComm (2020)

CREB3 suppresses hepatocellular carcinoma progression by depressing AKT signaling through competitively binding with insulin receptor and transcriptionally activating RNA-binding motif protein 38. [Abstract]

2024 Jul 1;5(7):e633. PMID: 38952575
Adv Sci (Weinh)

Aspirin-Mediated Acetylation of SIRT1 Maintains Intestinal Immune Homeostasis. [Abstract]

2024 May;11(19):e2306378. PMID: 38482749
Adv Sci (Weinh)

Manganese Mineralization of Pathogenic Viruses as a Universal Vaccine Platform. [Abstract]

2023 Nov;10(33):e2303615. PMID: 37867242
Cell Rep Med

Fungal metabolite-based immunotherapy overcomes tumor-associated macrophage immunosuppression. [Abstract]

2026 Jun 16;7(6):102833. PMID: 42173096
Sci Adv

Identification of VISTA regulators in macrophages mediating cancer cell survival. [Abstract]

2024 Nov 29;10(48):eadq8122. PMID: 39602545
Med

MHC-II-restricted neoantigen vaccine reverses immune microenvironment and overcomes resistance to immune-checkpoint inhibitors in cold tumors. [Abstract]

2026 Jan 9;7(1):100936. PMID: 41308654
Carbohydr Polym

Astragalus polysaccharides alleviate DSS-induced ulcerative colitis in mice by restoring SCFA production and regulating Th17/Treg cell homeostasis in a microbiota-dependent manner. [Abstract]

2025 Feb 1;349(Pt A):122829. PMID: 39643403
Cell Death Dis

YIF1A activates mTORC1 signaling to promote cellular senescence. [Abstract]

2026 Jun 23. PMID: 42336842
Cell Death Dis

AMPK regulates ARF1 localization to membrane contact sites to facilitate fatty acid transfer between lipid droplets and mitochondria. [Abstract]

2025 Aug 18;16(1):623. PMID: 40825999
Cell Death Dis

FTO controls CD8+ T cell survival and effector response by modulating m6A methylation of Fas. [Abstract]

2025 Apr 15;16(1):301. PMID: 40234389
Cell Death Dis

Single-cell transcriptome profiles the heterogeneity of tumor cells and microenvironments for different pathological endometrial cancer and identifies specific sensitive drugs. [Abstract]

2024 Aug 7;15(8):571. PMID: 39112478
Cell Death Dis

The mechanism of m6A methyltransferase METTL3-mediated autophagy in reversing gefitinib resistance in NSCLC cells by β-elemene. [Abstract]

2020 Nov 11;11(11):969. PMID: 33177491
Cell Death Dis

NMT1 inhibition modulates breast cancer progression through stress-triggered JNK pathway. [Abstract]

2018 Nov 16;9(12):1143. PMID: 30446635
Cancer Lett

Induction of EnR stress by Melatonin enhances the cytotoxic effect of Lapatinib in HER2-positive breast cancer. [Abstract]

2021 Oct 10:518:82-93. PMID: 34153400
J Immunother Cancer

Structural changes from wild-type define tumor-rejecting neoantigens. [Abstract]

2025 Oct 22;13(10):e013148. PMID: 41125532
J Immunother Cancer

T cells of colorectal cancer patients' stimulated by neoantigenic and cryptic peptides better recognize autologous tumor cells. [Abstract]

2022 Dec;10(12):e005651. PMID: 36460334
EBioMedicine

Exercise-derived peptide protects against pathological cardiac remodeling. [Abstract]

2022 Aug:82:104164. PMID: 35843176
Mater Today Bio

Molybdenum disulfide induces growth inhibition and autophagy-dependent hepatocyte cell death through directly binding and regulating the activity of MST2. [Abstract]

2025 Oct 8:35:102394. PMID: 41142426
Adv Healthc Mater

Lipoprotein-Based Nanocatalyst Enables Targeted Treatment of APAP-Induced Liver Injury via Enhanced Macropinocytosis. [Abstract]

2025 Sep;14(25):e2500507. PMID: 40411876
Adv Healthc Mater

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Endoplasmic reticulum stress inhibits AR expression via the PERK/eIF2α/ATF4 pathway in luminal androgen receptor triple-negative breast cancer and prostate cancer. [Abstract]

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A reduction-sensitive lipophilic dihydroartemisinin prodrug in a self-microemulsifying drug delivery system for treating breast cancer lung metastasis via intestinal lymphatic transport. [Abstract]

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Immunotherapy Inhibits Tumor Cholesterol Synthesis via the IFN-γ-ΙRF1-SREBF2 Axis. [Abstract]

2025 Dec 9. PMID: 41364085
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FAM135B Deficiency Inhibits Cytotoxic T-Cell Activity in Triple-negative Breast Cancer by Blocking the IFI16-dependent STING Pathway. [Abstract]

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ENPP1 governs the metabolic regulation of effector T cells in autoimmunity by detecting cytosolic mitochondrial DNA. [Abstract]

2025 Jun 13;44(6):115851. PMID: 40516055
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Translocational attenuation mediated by the PERK-SRP14 axis is a protective mechanism of unfolded protein response. [Abstract]

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The ubiquitin E3 ligase TRIM10 promotes STING aggregation and activation in the Golgi apparatus. [Abstract]

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Brefeldin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Mar 26;42(4):112306. [Abstract]

Brefeldin A (BFA) slightly reduces the ubiquitination of STING in HEK293T cells (transfection with Myc-STING, FLAG-TRIM10, and HA-Ub for 24 h).
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Fenofibrate potentiates the therapeutic efficacy of EZH2 inhibitors on melanoma via TRIM21- and OTUD4-mediated EZH2 ubiquitination. [Abstract]

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Grain-sized moxibustion activates dendritic cells to enhance the antitumor immunity of cancer vaccines. [Abstract]

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Fundam Res

Mannan-decorated STING-activating vaccine carrier for spatial coordinative stimulating antigen-specific immune responses. [Abstract]

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2025 Jun 21. PMID: 40542952
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Autophagy promotes aortic adventitial fibrosis via the IL-6/Jak1 signaling pathway in Takayasu's arteritis. [Abstract]

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Extracellular Glutamine Promotes Intestinal Porcine Epithelial Cell Proliferation via Arf1-mTORC1 Pathway Independently of Rag GTPases. [Abstract]

2023 Oct 4;71(39):14251-14262. PMID: 37738360
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2024 Jan:219:115957. PMID: 38049007
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LAMC2 mitigates ER stress by enhancing ER-mitochondria interaction via binding to MYH9 and MYH10. [Abstract]

2024 Jan;31(1):43-57. PMID: 37891404
Precis Clin Med

Repurposable drugs for SARS-CoV-2 and influenza sepsis with scRNA-seq data targeting post-transcription modifications. [Abstract]

2021 Aug 28;4(4):215-230. PMID: 34993416
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Bivalent mRNA vaccines against three SARS-CoV-2 variants mediated by new ionizable lipid nanoparticles. [Abstract]

2023 Jul 25:642:123155. PMID: 37402442
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Novel mechanisms of metformin-induced vasorelaxation of mesenteric arterioles via endothelium-dependent hyperpolarization to treat murine colitis. [Abstract]

2025 Sep 15:1003:177900. PMID: 40617384
Pharmaceuticals (Basel)

β-Elemene Reverses Gefitinib Resistance in NSCLC Cells by Inhibiting lncRNA H19-Mediated Autophagy. [Abstract]

2024 May 14;17(5):626. PMID: 38794196
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UBE2C-PI3K/AKT-mediated upregulation of MTHFD2 promotes tumor progression in hepatocellular carcinoma. [Abstract]

2026 Feb 1:170:116081. PMID: 41456492
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Tanshinone IIA alleviates myocarditis in Trex1-D18N lupus-like mice by inhibiting the interaction between STING and SEC24C. [Abstract]

2025 May 27:156:114659. PMID: 40252465
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Stress on the Endoplasmic Reticulum Impairs the Photosynthetic Efficiency of Chlamydomonas. [Abstract]

2024 Dec 11;25(24):13304. PMID: 39769069
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Fecal microbiota transplantation regulates the microbiota-gut-spinal cord axis to promote recovery after spinal cord injury. [Abstract]

2024 Jan 5:126:111212. PMID: 37979452
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The Deficiency of SCARB2/LIMP-2 Impairs Metabolism via Disrupted mTORC1-Dependent Mitochondrial OXPHOS. [Abstract]

2022 Aug 3;23(15):8634. PMID: 35955761
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Resolvin E1 Inhibits Corneal Allograft Rejection in High-Risk Corneal Transplantation. [Abstract]

2018 Aug 1;59(10):3911-3919. PMID: 30073362
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Lipid droplets and small extracellular vesicles interplay in Japanese encephalitis virus non-lytic release. [Abstract]

2026 Jun 10;17(6):e0042326. PMID: 42159429
Front Pharmacol

Pharmacological suppression of Nedd4-2 rescues the reduction of Kv11.1 channels in pathological cardiac hypertrophy. [Abstract]

2022 Aug 17:13:942769. PMID: 36059970
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Drug repurposing DMSO from an old solvent to a new candidate for the treatment of colitis and sepsis in male mice. [Abstract]

2026 May 23:136:103155. PMID: 42235215
Mol Pharm

SARS-CoV-2 NSP2 as a Potential Delivery Vehicle for Proteins. [Abstract]

2024 Mar 4;21(3):1149-1159. PMID: 38288708
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Trivalent mRNA Vaccine against SARS-CoV-2 and Variants with Effective Immunization. [Abstract]

2023 Oct 2;20(10):4971-4983. PMID: 37699256
PLoS Pathog

IL-2-mTORC1 signaling coordinates the STAT1/T-bet axis to ensure Th1 cell differentiation and anti-bacterial immune response in fish. [Abstract]

2022 Oct 25;18(10):e1010913. PMID: 36282845
PLoS Pathog

Endothelin receptors promote schistosomiasis-induced hepatic fibrosis via splenic B cells. [Abstract]

2020 Oct 19;16(10):e1008947. PMID: 33075079
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Dual Specificity Phosphatase 4 Enhances Immunotherapy Response by Inhibiting TGF-β1 Secretion in Hepatocellular Carcinoma. [Abstract]

2026 Apr 19;18(8):1289. PMID: 42073612
Neoplasia

Activation of PERK/eIF2α/ATF4 signaling inhibits ERα expression in breast cancer. [Abstract]

2025 Jul:65:101165. PMID: 40252311
Eur J Med Res

Invisible appliance promotes bone reconstruction via modulating the periodontal immune microenvironment. [Abstract]

2025 May 12;30(1):378. PMID: 40350478
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Drug Repurposing Applications to Overcome Male Predominance via Targeting G2/M Checkpoint in Human Esophageal Squamous Cell Carcinoma. [Abstract]

2022 Nov 28;14(23):5854. PMID: 36497337
Cell Signal

COL1A1 promotes clear cell renal cell carcinoma progression through the Wnt/β-catenin signaling pathway. [Abstract]

2026 Feb:138:112259. PMID: 41270811
J Cell Mol Med

RTP4 Suppresses Colorectal Cancer Progression via MHC-I-Mediated CD8+ T Cell Infiltration and Enhances Immunotherapy Response. [Abstract]

2025 Oct;29(20):e70915. PMID: 41126439
J Cell Mol Med

Knockdown of Golgi phosphoprotein 73 blocks the trafficking of matrix metalloproteinase-2 in hepatocellular carcinoma cells and inhibits cell invasion. [Abstract]

2019 Apr;23(4):2399-2409. PMID: 30677226

Brefeldin A purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Apr;23(4):2399-2409. [Abstract]

MHCC-97H cells are treated with BFA (2.5 μg/mL) for 0, 0.5, 1, 2, 6, and 12 h. The expression of GP73 and intracellular MMP-2 is measured using immunoblotting.
Clin Exp Med

B3GNT7 preserves intestinal barrier integrity: a key defense mechanism against acute pancreatitis progression. [Abstract]

2026 May 31. PMID: 42218343
Poult Sci

Brefeldin A inhibits duck plague virus replication by impairing virion envelopment. [Abstract]

2026 Jan 23;105(4):106509. PMID: 41619483
iScience

AF6 regulates intestinal IgA via crosstalk between intestinal epithelial cells and immune cells in inflammatory bowel disease. [Abstract]

2025 May 13;28(7):112658. PMID: 40687779
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Lithium ameliorates Niemann-Pick C1 disease phenotypes by impeding STING/SREBP2 activation. [Abstract]

2023 Apr 8;26(5):106613. PMID: 37128603
Immunother Adv

Abnormal glucose and lipid metabolism promotes disrupted differentiation of T and B cell subsets in Behçet's disease. [Abstract]

2025 Mar 24;5(1):ltaf010. PMID: 40297266
FASEB J

Extracellular HSP90 promotes differentiation of lens epithelial cells to fiber cells by activating LRP1-YAP-PROX1 axis. [Abstract]

2023 Feb;37(2):e22783. PMID: 36705056
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Fish NF-κB couples TCR and IL-17 signals to regulate ancestral T-cell immune response against bacterial infection. [Abstract]

2021 Apr;35(4):e21457. PMID: 33689192
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Brefeldin A inhibits colorectal cancer growth by triggering Bip/Akt-regulated autophagy. [Abstract]

2019 Apr;33(4):5520-5534. PMID: 30668917

Brefeldin A purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Apr;33(4):5520-5534. [Abstract]

Apoptotic effects induced by BFA are examined in CRC cells.

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The interaction of Beclin 1 with Bcl-2 or ATG14L after BFA treatment is determined by coimmunoprecipitation assay.

Brefeldin A purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Apr;33(4):5520-5534. [Abstract]

CRC cells are treated with vehicle, BFA (100 nM), 3-MA (10 mM), or in combination for 24 h. Immunoblot analysis is used to detect LC3 turnover.
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Transcription factor networks drive perforin activity in the anti-bacterial immune response of tilapia. [Abstract]

2024 Nov:154:109975. PMID: 39427837
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Inducible IL-2 production and IL-2+ cell expansion are landmark events for T-cell activation of teleost. [Abstract]

2024 May:148:109515. PMID: 38499218
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Fish requires FasL to facilitate CD8+ T-cell function and antimicrobial immunity. [Abstract]

2025 Jun 1;214(6):1219-1235. PMID: 40073091
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FGL1 in plasma extracellular vesicles is correlated with clinical stage of lung adenocarcinoma and anti-PD-L1 response. [Abstract]

2024 Mar 12;216(1):68-79. PMID: 38146642
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Increased SLAMF7+CD8+ T cells are associated with the pathogenesis of experimental autoimmune pancreatitis in mice. [Abstract]

2023 Nov;23(7):767-776. PMID: 37661465
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The correlation between Omentin-1 levels and Th17/Treg imbalance in patients with periodontitis (Stage Ⅱ/Ⅲ, Grade B/C) and its diagnostic value. [Abstract]

2026 Jun 22. PMID: 42332681
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Proximity Proteomics and Biochemical Analysis Reveal a Noncanonical Function for UFM1-Specific Protease 1 in the p62 Body Formation. [Abstract]

2023 Jul 7;22(7):2352-2363. PMID: 37285312
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A novel 2B4 receptor leads to worse pregnancy outcomes by facilitating TNF-α and IFN-γ production in dNK cells during Toxoplasma gondii infection. [Abstract]

2022 Sep 24;15(1):337. PMID: 36153598
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Tracking the spatiotemporal journey of chitosan nanoparticles across ear physiological barriers: Mechanisms and pathways. [Abstract]

2026 Jan 9;54(3):100233. PMID: 41764965
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mRNA-laden lipid nanoparticle-enabled humanized CD19 CAR-T-cell engineering for the eradication of leukaemic cells. [Abstract]

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2025 Nov 11. PMID: 41216763
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Images showing the morphology of axons after 2.0 mT of 50 Hz MF exposure for 3 days, 1 h per day. Histograms showing the average axon length per neuron, the average axon branch length per neuron and the average number of branches per axon in the sham and exposure groups. Neurons were treated with 1.0 µg/mL brefeldin A at DIV2 as a positive control.
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Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (356.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 11.11 mg/mL (39.63 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5668 mL

17.8342 mL

35.6684 mL

5 mM

0.7134 mL

3.5668 mL

7.1337 mL

10 mM

0.3567 mL

1.7834 mL

3.5668 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline