10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 7 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Brefeldin A Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis . It could also improve the HDR(homology-directed repair) efficiency and b
In vitro
Brefeldin A is a fungal metabolite and blocks the forward transport between the endoplasmic reticulum and Golgi apparatus, Brefeldin A causes an impaired distribution of the membrane proteins. When HCT 116 human colon cancer cell is treated with Brefeldin A, morphological changes indicating cell differentiation are observed. Brefeldin A exerts its cytotoxic effects mainly by inducing differentiation and apoptosis in tumor cells. The treatment of the strips with 20 μg/mL Brefeldin A for 6 hours completely abolishes the relaxation induced by bradykinin in the presence of 10mM indomethacin and 30 μM L-NOARG. The treatment with 20 μg/mL Brefeldin A substantially abolishes the bradykinin-induced decreases in [Ca2+]i and tension in the range of concentrations between 1 nM and 1 mM. Brefeldin A has no effect on the [Ca2+]i elevation in endothelial cells induced by bradykinin or substance P. Addition of the fungal metabolite Brefeldin A does not affect the spontaneous phospholipid-dependent GTPS binding to myr-rARF1 but totally abolishs the retinal isotonic extract (RIE)-catalyzed exchange, with half-maximal inhibition at 2 μM Brefeldin A. Brefeldin A prevents a wide variety of membrane traffic pathways. Brefeldin A inhibits an ADP-ribosylation factor-specific guanine nucleotide exchange activity present in Golgi membranes or in brain cytosol. The complete prevention by Brefeldin A strongly suggests that the retinal extract contains an ARF-specific guanine nucleotide exchange factor. Retinal isotonic extract (RIE)-catalyzed GTPS release from both ADP-ribosylation factors (ARFs) is only partly inhibited by Brefeldin A, even at 300 μM. Brefeldin A induces fusion of the Golgi apparatus with the ER. Brefeldin A abolishes the inhibitory effect of the CERT inhibitor HPA-12. Brefeldin A treatment, which induces fusion of the Golgi apparatus and the ER, rescues the limonoid-induced prevention of sphingomyelin biosynthesis. BFA treatment of CHO cells causes a 2 to 3 fold increase in sphingomyelin synthesis. Apart from B-CLL cells, Brefeldin A reportedly causes apoptosis in multiple myeloma (U266, NCI-H929), Jurkat, HeLa, leukaemia (HL60, K562, BJAB), colon (HT-29) and prostate, as well as adenoid cystic sarcoma cells. The administration of 25 ng/mL of Brefeldin A completely blocks growth of HF4.9 and HF28RA cells, whereas higher Brefeldin A doses (75 ng/mL) are required to achieve the same effect in HF1A3 cells. Cell proliferation is inhibited within 24 hours in a dose-dependent manner and, depending on the cell line, almost complete cessation of 3H-thymdine incorporation is observed at 50-75 ng/mL of Brefeldin A (26%, 76%, 87% inhibition at 50 ng/ml and 75%, 87%, 92% inhibition at 75 ng/mL for HF1A3, HF4.9 and HF28RA cells respectively. Brefeldin A-induced cell killing is in a dose-dependent manner using YO-PRO 1/PI assay. Brefeldin A could improve the HDR(homology-directed repair) efficiency. It is an enhancer of CRISPR-mediated HDR.
In vivo
Cell Data
cell lines：
Concentrations：0 ng/mL -75 ng/mL
Incubation Time：5 days
Powder Purity:≥99%
| Isomeric SMILES | C[C@H]1CCC/C=C/[C@@H]2C[C@@H](C[C@H]2[C@@H](/C=C/C(=O)O1)O)O |
|---|---|
| WGK Germany | 3 |
| RTECS | GY8410000 |
| UN Number | 2811 |
| Molecular Weight | 280.36 |
| Beilstein | 25191 |
| Reaxy-Rn | 30543489 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=30543489&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →| Solubility | Solubility (25°C) In vitro Water: 100 mg/mL (139.33 mM); |
|---|---|
| Specific Rotation[α] | 93° (C=2,MeOH) |
| Melt Point(°C) | 201-205°C |
| 1. Jianbo Li, Yaru Xu, Jieke Zhang, Qinglian Li, Chenxu Wang, Zhe Wu, Weijing Yang, Meng Xu, Zhenzhong Zhang, Lei Wang, Jinjie Zhang. (2023) Bioinspired fine-tuning of the mechanical rigidity of SNEDDS for the efficient crossing of multiple gastrointestinal barriers. JOURNAL OF CONTROLLED RELEASE, [PMID:37625600] [10.1016/j.jconrel.2023.08.044] |
| 2. Jinhui Lu, Xiaomeng Zhu, Meng Zhang, Xunchan Jiang, Wei Guo, Feng Jiang, Feng Cao. (2023) In vitro and in vivo assessment of structural integrity for HPCD complex@Liposome nanocomposites from ocular surface to the posterior segment of the eye. CARBOHYDRATE POLYMERS, [PMID:37230631] [10.1016/j.carbpol.2023.120960] |
| 3. Wu Wenting, Ding Quan, Zhou Zhiwei, Kuang Wenliang, Jiang Lipeng, Liu Peng, Ai Weiping, Zhu Weifeng. (2023) Transcellular Transport Behavior of the Intact Polymeric Mixed Micelles with Different Polymeric Ratios. AAPS PHARMSCITECH, 24 (2): (1-16). [PMID:36792796] [10.1208/s12249-022-02454-y] |
| 4. Yang Sun, Tiancong Liu, Weiliang Bai. (2022) MAF bZIP Transcription Factor B (MAFB) Protected Against Ovalbumin-Induced Allergic Rhinitis via the Alleviation of Inflammation by Restoring the T Helper (Th) 1/Th2/Th17 Imbalance and Epithelial Barrier Dysfunction. Journal of Asthma and Allergy, [PMID:35250280] [10.2147/JAA.S335560] |
| 5. Zhiyi Wang, Jingyi Zhang, Jilei Huang, Gan Sha, Xinyue Song, Xue Cao, Zhenchen Yan, Chuanhe Liu, Siping Chen, Ziying Li, Xiuqin Huang, Qingjun Xie, Xin Yang, Guohui Zhou, Tong Zhang. (2025) Plant negative-strand RNA virus phosphoprotein condensates exploit host trafficking and lipid synthesis for viral factory assembly. Science Advances, 11 (34): [PMID:40834074] [10.1126/sciadv.adx7905] |
| 6. Xianzheng Sang, Yichao Ye, Chengzi Yang, Xiaoxiang Hou, Yangu Guo, Hantong Shi, Chunhui Wang, Wen Chen, Danfeng Zhang, Lijun Hou. (2026) Microglia as a key mediator in rosuvastatin-associated cognitive impairment. NEUROTOXICOLOGY, [PMID:41690424] [10.1016/j.neuro.2026.103405] |
| 7. Zhibao Zhang, Mingyi Tan, Xin Liu, Wenhua Wang, Xiang Chen, Cong Peng, Shuang Zhao, Lisha Wu. (2026) Activation of Unfolded Protein Response Pathways Promotes Keratinocyte Differentiation and Ameliorates Psoriasis Phenotypes. CELL STRESS & CHAPERONES, [PMID:41765076] [10.1016/j.cstres.2026.100163] |
