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Brefeldin A

Brefeldin A (Cyanein) 属于大环内酯类抗生素，是一种 ATPase 抑制剂 (IC50=0.2 μM)。Brefeldin A 可以诱导肿瘤细胞分化和凋亡，也具有抑制自噬的活性。

CAS号

20350-15-6

分子式

C16H24O4

主要靶点

ATPase|Autophagy|Antibacterial|Antibiotic|CRISPR/Cas9|HSV|Mitophagy

仅限科研使用

Cat No : CM03062

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Synonyms

Decumbin|Cas9|Brefeldin A|BFA|Cyanein|CRISPR|CRISPR/Cas9|Antibiotic|ATPase (HCT 116)|Autophagy|Ascotoxin|inhibit|Mitochondrial Autophagy|Mitophagy|Inhibitor|HSV|Herpes simplex virus|布雷非德菌素 A|布雷菲德菌素 A

验证数据展示

  • CAS No.: 20350-15-6

    Brefeldin A
    CAS#: 20350-15-6

产品信息

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.

CAS号 20350-15-6
分子式 C16H24O4
主要靶点 ATPase|Autophagy|Antibacterial|Antibiotic|CRISPR/Cas9|HSV|Mitophagy
主要通路 微生物学|自噬|离子通道|自噬|微生物学|DNA 损伤和修复
分子量 280.36
纯度 99.91%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Store at low temperature,Keep away from moisture,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 Decumbin|Cas9|Brefeldin A|BFA|Cyanein|CRISPR|CRISPR/Cas9|Antibiotic|ATPase (HCT 116)|Autophagy|Ascotoxin|inhibit|Mitochondrial Autophagy|Mitophagy|Inhibitor|HSV|Herpes simplex virus|布雷非德菌素 A|布雷菲德菌素 A

靶点活性

ATPase (HCT 116 cells):0.2 μM|A549 cells proliferation:101.2 nM|HepG2 cells proliferation:239.1 nM|HeLa cells proliferation:171.9 nM

体内活性

方法：为检测体内抗肿瘤活性，将 Brefeldin A (15 mg/kg in 10% ricinus oil+5% DMSO+10% ethanol+75% physiologic saline) 腹腔注射给携带人结直肠癌肿瘤 HCT116 的 BALB/c 小鼠，每天一次，持续四周。 结果：Brefeldin A 在体内抑制 HCT116 肿瘤生长。[3] 方法：为检测体内抗肿瘤活性，将 Brefeldin A (16-64 mg/kg in distilled water containing 0.05% Tween 80) 腹腔注射给携带肿瘤 LOX IMVI 的 Athymic NCr nu/nu 小鼠，每天两次，持续五天。 结果：Brefeldin A 在体内显示出抗肿瘤活性，小鼠寿命增加 65%-100%，第 60 天幸存者增加 17%-50%。[4]

体外活性

方法：肿瘤细胞 HL60 、K562 和 HT-29 用 Brefeldin A (2 μM) 处理 72 h，使用 DNA filter elution assay 检测 DNA 片段。 结果：Brefeldin A 以不同的动力学诱导 DNA 断裂。HL60 细胞在 15 h 内观察到完整的 DNA 片段，而 K562 和 HT-29 细胞则需要 48-72 h。[1] 方法：人乳腺癌细胞 MDA-MB-231 用 Brefeldin A (0.05-1 μg/mL) 处理 24 h，使用 Western Blot 方法检测靶点蛋白表达水平。 结果：PARP 切割是细胞死亡的标志性事件，可以在 Brefeldin A 处理的悬浮 MDA-MB-231 细胞中检测到。[2]

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (14.27 mM);Ethanol:2.81 mg/mL (10.02 mM);DMSO:128.75 mg/mL (459.23 mM)

细胞实验

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)

参考文献

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

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