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Brefeldin A

Catalog No. T6062   CAS 20350-15-6
Synonyms: BFA, Ascotoxin, Cyanein, Decumbin

Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.

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Brefeldin A Chemical Structure
Brefeldin A, CAS 20350-15-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 48.00
10 mg In stock $ 58.00
50 mg In stock $ 198.00
100 mg In stock $ 360.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.89%
Purity: 99.26%
Purity: 99.2%
Purity: 96.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.
Targets&IC50 ATPase (HCT 116 cells):0.2 μM
In vitro METHODS: Tumor cells HL60, K562 and HT-29 were treated with Brefeldin A (2 μM) for 72 h. DNA fragments were detected by DNA filter elution assay.
RESULTS: Brefeldin A induced DNA fragmentation with different kinetics. intact DNA fragments were observed in HL60 cells within 15 h, whereas 48-72 h was required for K562 and HT-29 cells. [1]
METHODS: Human breast cancer cells MDA-MB-231 were treated with Brefeldin A (0.05-1 μg/mL) for 24 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: PARP cleavage, a hallmark event of cell death, could be detected in Brefeldin A-treated suspension MDA-MB-231 cells. [2]
In vivo In HF4.9 and HF28RA cells, Brefeldin A (25 ng/mL) completely inhibits cell growth. Similarly, in HF1A3 cells, Brefeldin A (75 ng/mL) fully inhibits cell growth.
Kinase Assay ELISA-based active site binding assay: Samples (lysed cells or tissue homogenates) are treated for 1 h at room temperature with the biotinylated active site probe PR-584 (5-15 μM). Samples are denatured by addition of SDS (0.9% final) and heating to 100 °C for 5 min. The denatured samples are transferred to a 96-well or 384-well filter plat, mixed with streptavidin-sepharose beads (2.5-5 μL packed beads/well), and incubated for 1 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer (PBS, 1% bovine serum albumin, 0.1% Tween-20) by vacuum filtration. The beads are incubated overnight at 4 °C on a plate shaker with the following antibodies recognizing the six catalytic subunits diluted into ELISA buffer: β5, β1, and β2 diluted 1:3000, LMP7 and LMP2 diluted 1:5000, and MECL-1 diluted 1:1000. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and incubated with HRP-conjugated secondary antibody diluted 1:5000 in ELISA buffer and incubated 2 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and developed for chemiluminsecence signal using the supersignal ELISA pico substrate following the manufacturer's instructions. Luminescence is measured on a plate reader and converted to ng of proteasome or μg/ml of lysate by comparison with 20S proteasome or untreated cell lysate standard curves. For proteasome inhibitor studies, active site probe binding values are expressed as the percent of binding relative to DMSO treated cells.
Cell Research HF1A3, HF4.9 cell viability upon the treatments is tested using double staining of cells with YO-PRO 1/PI and SYTO16/PI probes. To access cell proliferation, cells are treated with 0–100 ng/mL Brefeldin A in complete medium for 20 hours before adding 1 μCi/mL [methyl-3H]-thymidine for additional 4 hours at 37 °C. The incorporated radioactive thymidine is quantified by scintillation counting with Microbeta counter. To examine long-term effects of Brefeldin A treatment, cells are seeded at initial concentration 105 cells/mL and treated with 0-75 ng/mL Brefeldin A for up to 5 days. At the time indicated, a sample of cells is removed and viable cell number is assessed by standard Trypan Blue exclusion assay.(Only for Reference)
Synonyms BFA, Ascotoxin, Cyanein, Decumbin
Molecular Weight 280.36
Formula C16H24O4
CAS No. 20350-15-6

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 2.8 mg/mL (10 mM)

DMSO: 14 mg/mL (50 mM)

TargetMolReferences and Literature

1. Shao RG, et al. Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53. Exp Cell Res. 1996 Sep 15;227(2):190-6. 2. Tseng CN, et al. Brefeldin A reduces anchorage-independent survival, cancer stem cell potential and migration of MDA-MB-231 human breast cancer cells. Molecules. 2014 Oct 29;19(11):17464-77. 3. Zhou L, et al. Brefeldin A inhibits colorectal cancer growth by triggering Bip/Akt-regulated autophagy. FASEB J. 2019 Apr;33(4):5520-5534. 4. Sausville EA, et al. Antiproliferative effect in vitro and antitumor activity in vivo of brefeldin A. Cancer J Sci Am. 5. Wlodkowic D, et al. Leuk Res. 2007, 31(12), 1687-1700. 6. Wang J, et al. Erythroleukemia cells acquire an alternative mitophagy capability. Sci Rep. 2016 Apr 19;6:24641. 7. Zhang Y, Hu H, Liu W, et al. Amino acids and RagD potentiate mTORC1 activation in CD8+ T cells to confer antitumor immunity[J]. Journal for ImmunoTherapy of Cancer. 2021, 9(4): e002137. 8. Bai R, Li L, Liu M, et al. Paper Based 3D Scaffold for Multiplexed Single Cell Secretomic Analysis[J]. Analytical chemistry. 2018, 90(9): 5825-5832. 9. Ma X, Zou F, Yu F, et al. Nanoparticle Vaccines Based on the Receptor Binding Domain (RBD) and Heptad Repeat (HR) of SARS-CoV-2 Elicit Robust Protective Immune Responses[J]. Immunity. 2020

TargetMolCitations

1. Ma X, Zou F, Yu F, et al. Nanoparticle Vaccines Based on the Receptor Binding Domain (RBD) and Heptad Repeat (HR) of SARS-CoV-2 Elicit Robust Protective Immune Responses. Immunity. 2020, 53(6): 1315-1330. e9. 2. Luo Q, Liu Q, Cheng H, et al. Nondegradable ubiquitinated ATG9A organizes Golgi integrity and dynamics upon stresses. Cell reports. 2022, 40(7): 111195. 3. Bai R, Li L, Liu M, et al. Paper Based 3D Scaffold for Multiplexed Single Cell Secretomic Analysis. Analytical chemistry. 2018, 90(9): 5825-5832. 4. Yu T, Ling Q, Xu M, et al. ORF8 protein of SARS‐CoV‐2 reduces male fertility in mice. Journal of Medical Virology. 2022 5. Zhang X, Wu S, Liu J, et al.A Mosaic Nanoparticle Vaccine Elicits Potent Mucosal Immune Response with Significant Cross‐Protection Activity against Multiple SARS‐CoV‐2 Sublineages.Advanced Science.2023: 2301034. 6. He X, Zhang X, Wu B, et al.The receptor binding domain of SARS-CoV-2 Omicron subvariants targets Siglec-9 to decrease its immunogenicity by preventing macrophage phagocytosis.Nature Immunology.2024: 1-11.

Related compound libraries

This product is contained In the following compound libraries:
Natural Product Library for HTS Microbial Natural Product Library Traditional Chinese Medicine Monomer Library Natural Product Library Membrane Protein-targeted Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Viral Compound Library Anti-Inflammatory Traditional Chinese Medicine Compound Library Ion Channel Inhibitor Library

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Keywords

Brefeldin A 20350-15-6 Autophagy DNA Damage/DNA Repair Membrane transporter/Ion channel Microbiology/Virology ATPase Mitophagy HSV CRISPR/Cas9 Antibiotic Inhibitor BFA inhibit Herpes simplex virus Ascotoxin Mitochondrial Autophagy Cyanein Decumbin inhibitor

 

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