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Brefeldin A

现货
Catalog No.
B1400
ATP酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
5mg
¥ 500.00
现货
25mg
¥ 1,900.00
现货
100mg
¥ 4,700.00
现货

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Background

Brefeldin A (BFA) is an inhibitor of ATPase with IC50 value of 0.2 μM [1]
ATPase is a chemical enzyme which is essential in the ADP/ATP exchange which process provides chemical potential energy. ATP supplies the energy for many physiological activities such as importing metabolites necessary for cell metabolism, exporting toxins, wastes, and solutes that can hinder cellular processes, cell proliferation, ER stress and so forth [2].
Treatment with BFA could attenuate stimulus-dependent hyperalgesia phenomenon via inhibiting vesicular exocytosis which process is important for ATP release [3]. When tested with cell line HEK293 cells (stably express wild-type (wt) CRELD2), BFA treatment nearly abolished the secretion of wtCRELD2 completely via inhibiting the transportation of proteins from the ER to the Golgi apparatus [4]. In MCF-7 cells and Hela cells, treatment with BFA induced p53 expression via inhibiting ATP which enhanced ER stress [5]. When treated with colorectal cancer cell line HCT116 cells, BFA treatment induced cells apoprosis by inhibiting ATP which functioned in the process of cellular vesicle trafficking [1].
BFA also is reported as an inhibitor for GTP/GDP exchange in a dose-dependent way, which is important in vesicular trafficking [6].
References:
[1] P.M. Wierzbicki, M. Kogut, J. Ruczynski, K. Siedlecka-Kroplewska, L. Kaszubowska, A. Rybarczyk, M. Alenowicz, P. Rekowski, Z. Kmiec, Protein and siRNA delivery by transportan and transportan 10 into colorectal cancer cell lines, Folia Histochem Cytobiol, (2014).
[2] M. Westerterp, A.E. Bochem, L. Yvan-Charvet, A.J. Murphy, N. Wang, A.R. Tall, ATP-binding cassette transporters, atherosclerosis, and inflammation, Circulation research, 114 (2014) 157-170.
[3] E.K. Joseph, P.G. Green, J.D. Levine, ATP release mechanisms of endothelial cell-mediated stimulus-dependent hyperalgesia, The journal of pain : official journal of the American Pain Society, 15 (2014) 771-777.
[4] K. Oh-hashi, Y. Kanamori, Y. Hirata, K. Kiuchi, Characterization of V-ATPase inhibitor-induced secretion of cysteine-rich with EGF-like domains 2, Cell biology and toxicology, 30 (2014) 127-136.
[5] W.C. Lin, Y.C. Chuang, Y.S. Chang, M.D. Lai, Y.N. Teng, I.J. Su, C.C. Wang, K.H. Lee, J.H. Hung, Endoplasmic reticulum stress stimulates p53 expression through NF-kappaB activation, PLoS One, 7 (2012) e39120.
[6] D. Prieto, P. Corchete, Transport of flavonolignans to the culture medium of elicited cell suspensions of Silybum marianum, Journal of plant physiology, 171 (2014) 63-68.

文献引用

1. Brian D. Rutter. "CONTENTS AND FUNCTIONS OF EXTRACELLULAR VESICLES ISOLATED FROM PLANTS." Indiana University. 2019.
2. Zhang M, Sun H, et al. "COPI-Mediated Nuclear Translocation of EGFRvIII Promotes STAT3 Phosphorylation and PKM2 Nuclear Localization." Int J Biol Sci. 2019 Jan 1;15(1):114-126. PMID:30662352
3. Liu C, Zhang Y, Ren H. "Actin Polymerization Mediated by AtFH5 Directs the Polarity Establishment and Vesicle Trafficking for Pollen Germination in Arabidopsis." Mol Plant. 2018 Nov 5;11(11):1389-1399. PMID:30296598
4. Rutter BD, Innes RW. "Extracellular Vesicles Isolated from the Leaf Apoplast Carry Stress-Response Proteins." Plant Physiol. 2017 Jan;173(1):728-741. doi:10.1104/pp.16.01253. PMID:27837092

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt280.36
Cas No.20350-15-6
FormulaC16H24O4
Solubility≥4.67mg/mL in DMSO
Chemical Name(1S,2E,7S,10E,12R,13R,15S)-12,15-dihydroxy-7-methyl-8-oxabicyclo[11.3.0]hexadeca-2,10-dien-9-one
SDFDownload SDF
Canonical SMILESCC1CCCC=CC2CC(CC2C(C=CC(=O)O1)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1-4]:

细胞系

结直肠癌细胞系HCT116细胞,MCF-7细胞,Hela细胞,正常大鼠肾细胞(NRK),MDA-MB-231细胞

溶解方法

该化合物在DMSO中的溶解度大于4.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应时间

5 μg/ml,1 μg/ml;3-40 h;37℃

应用

在正常大鼠肾细胞中,BFA治疗15小时或40小时引起内质网(ER)的剧烈肿胀,并将其定位转移到细胞周边。BFA影响高尔基体结构和肌动蛋白组织。BFA诱导MDA-MB-231悬浮培养细胞死亡,EC50为0.016 μg/ mL。BFA通过下调乳腺CSC标记CD44和抗凋亡蛋白Bcl-2和Mcl-1,有效抑制MDA-MB-231细胞的克隆形成和迁移以及基质金属蛋白酶-9(MMP-9)活性,BFA可逆转上皮-间质转化。在MCF-7细胞和Hela细胞中, BFA(1 μg/ml)诱导p53表达。在结直肠癌细胞系HCT116细胞中,BFA诱导细胞凋亡。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Alvarez C, et al. Brefeldin A (BFA) disrupts the organization of the microtubule and the actin cytoskeletons. Eur J Cell Biol. 1999 Jan;78(1):1-14.

[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]. W.C. Lin, Y.C. Chuang, Y.S. Chang, M.D. Lai, Y.N. Teng, I.J. Su, C.C. Wang, K.H. Lee, J.H. Hung, Endoplasmic reticulum stress stimulates p53 expression through NF-kappaB activation, PLoS One, 7 (2012) e39120.

[4]. P.M. Wierzbicki, M. Kogut, J. Ruczynski, K. Siedlecka-Kroplewska, L. Kaszubowska, A. Rybarczyk, M. Alenowicz, P. Rekowski, Z. Kmiec, Protein and siRNA delivery by transportan and transportan 10 into colorectal cancer cell lines, Folia Histochem Cytobiol, (2014).

质量控制

化学结构

Brefeldin A

相关生物数据

Brefeldin A

相关生物数据

Brefeldin A