产品说明书

Brefeldin A

Print
Chemical Structure| 20350-15-6 同义名 : BFA;Decumbin;Bredfeldin A;Synergisidin;NSC 244390;NSC 107456;NSC 89671;NSC 56310;Nectrolide;Ascotoxin;Cyanein
CAS号 : 20350-15-6
货号 : A156234
分子式 : C16H24O4
纯度 : 99%+
分子量 : 280.359
MDL号 : MFCD00083258
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(374.52 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 10 mg/mL(35.67 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
靶点

  • ATPase

    ATPase (HCT 116), IC50:0.2 μM
描述 Brefeldin A is a fungal lactone antibiotic produced by Penicillium brefeldianum usually used as a protein trafficking/secretion inhibitor in mammalian and other eukaryotic cells, without significant effect on protein synthesis. The main target of Brefeldin A may be Arf1, which is important to formation of protein transport vesicles[1][2][3]. Brefeldin A could induce the rapid redistribution of the ll0-kD protein and the movement of Golgi membrane into the ER within 15min at 2μg/ml in semipermeable cells[4]. Brefeldin A could induce a wide variety of human cancer cells to differentiation and apoptosis. It exhibited cytotoxicity to HCT 116 cells with IC50 value of 0.2μM, as well as induced DNA fragmentation and apoptotic morphological changes with IC50 values of 0.11 and 0.36 μM, respectively[5]. Brefeldin A combined with L755507 could improve the HDR efficiency, and exhibit enhanced insertion efficiency by 2-fold, with maximal effect at 0.1 μM[6].
作用机制 Brefeldin A inhibits protein trafficking and secretion by interfering with the function of the Golgi apparatus, which may due to the disruption of transport vesicle formation dependent on the assembly of the COPI coat by Arf1-GTP.[1][2][3]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
3T3-L1 5 μg/ml Function Assay 30 min mimics the effects of insulin and causes robust phosphorylation of Akt (Ser 473) and phosphorylation of AS160 (Thr 642 and Ser 588) 24843827
3T3-L1 5 μg/ml Function Assay 30 min recapitulates insulin action with respect to regulating Akt activity and AS160 phosphorylation 24843827
3T3-L1 5 μg/ml Function Assay 30 min causes reversible redistribution of GLUT4 24843827
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01742364 - Completed - -
NCT01742364 Tuberculosis Not Applicable Completed - South Africa ... 展开 >> SATVI, University of Cape Town Cape Town, South Africa, 7925 收起 <<
NCT03044509 - Recruiting December 2019 Switzerland ... 展开 >> Kantonspital Aarau Recruiting Aarau, Switzerland, 5001 Contact: Sara Bernhard-Stirnemann, Dr med    +41628384192    sara.bernhard@ksa.ch    Kinderspital Basel Recruiting Basel, Switzerland, 4031 Contact: Marina Beaufils-Hugot, PhD    +41617042953    marina.beaufils-hugot@ukbb.ch    Contact: Noemi Meier, Master    +41617042947    noemi.meier@ukbb.ch    Principal Investigator: Nicole Ritz, PD Dr med          Sub-Investigator: Ines Mack, Dr med          Sub-Investigator: Anja Jochmann, Dr med          Sub-Investigator: Daniel Trachsel, PD Dr med          Ospedale Regionale di Bellinzona Recruiting Bellinzona, Switzerland, 6500 Contact: Lisa Kottanattu, Dr med    +41918118538    lisa.kottanattu@eoc.ch    Inselspital Bern Recruiting Bern, Switzerland, 3010 Contact: Andrea Duppenthaler, Dr. med.    +41316329414    andrea.duppenthaler@insel.ch    Hôpital des enfants - HUG Recruiting Genève, Switzerland, 1205 Contact: Anne Mornand, Dr. med.    +41223724579    anne.mornand@hcuge.ch    Sub-Investigator: Marie Rohr, Dr. med.          Kinserspital Luzern Recruiting Luzern, Switzerland, 6016 Contact: Michael Buettcher, Dr med    +41412056657    michael.buettcher@luks.ch    Kinderspital St Gallen Recruiting St. Gallen, Switzerland, 9006 Contact: Jürg Barben, Prof Dr med    +41712437111    juerg.barben@kispisg.ch    Sub-Investigator: Christian Kahlert, Dr med          Kinderklinik Zürich Recruiting Zürich, Switzerland, 8032 Contact: Christoph Berger, Prof Dr med    +41442667840    christoph.berger@kispi.uzh.ch    Sub-Investigator: Christa Relly, Dr med 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.57mL

0.71mL

0.36mL

17.83mL

3.57mL

1.78mL

35.67mL

7.13mL

3.57mL
参考文献

[1]Donaldson JG, Finazzi D, et al. Brefeldin A inhibits Golgi membrane-catalysed exchange of guanine nucleotide onto ARF protein. Nature. 1992 Nov 26;360(6402):350-2.

[2]Orci L, Tagaya M, et al. Brefeldin A, a drug that blocks secretion, prevents the assembly of non-clathrin-coated buds on Golgi cisternae. Cell. 1991 Mar 22;64(6):1183-95.

[3]Donaldson JG, Lippincott-Schwartz J, et al. Guanine nucleotides modulate the effects of brefeldin A in semipermeable cells: regulation of the association of a 110-kD peripheral membrane protein with the Golgi apparatus. J Cell Biol. 1991 Feb;112(4):579-88.

[4]Donaldson JG, Lippincott-Schwartz J, et al. Guanine nucleotides modulate the effects of brefeldin A in semipermeable cells: regulation of the association of a 110-kD peripheral membrane protein with the Golgi apparatus. J Cell Biol. 1991 Feb;112(4):579-88.

[5]Zhu JW, Nagasawa H, et al. Elucidation of strict structural requirements of brefeldin A as an inducer of differentiation and apoptosis. Bioorg Med Chem. 2000 Feb;8(2):455-63.

[6]Yu C, Liu Y, et al. Small molecules enhance CRISPR genome editing in pluripotent stem cells. Cell Stem Cell. 2015 Feb 5;16(2):142-7.