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Brefeldin A

产品编号 T6062 CAS 20350-15-6

别名: BFA, 布雷非德菌素 A, Ascotoxin, Cyanein, Decumbin

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。

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Brefeldin A, CAS 20350-15-6

规格	价格/CNY	货期
5 mg	￥ 414	现货
10 mg	￥ 698	现货
50 mg	￥ 2,470	现货
100 mg	￥ 3,859	现货
1 mL * 10 mM (in DMSO)	￥ 414	现货

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纯度: 99.26%

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天然产物信息

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

植物来源	天然产物 > 其他（植物来源） > 其他

产品描述	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.
靶点活性	ATPase (HCT 116 cells):0.2 μM
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]
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]
激酶实验	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.
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)

别名	BFA, 布雷非德菌素 A, Ascotoxin, Cyanein, Decumbin
分子量	280.36
分子式	C16H24O4
CAS No.	20350-15-6

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 2.8 mg/mL (10 mM)

DMSO: 14 mg/mL (50 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	3.5668 mL	17.8342 mL	35.6684 mL	89.1711 mL
	5 mM	0.7134 mL	3.5668 mL	7.1337 mL	17.8342 mL
	10 mM	0.3567 mL	1.7834 mL	3.5668 mL	8.9171 mL
DMSO	20 mM	0.1783 mL	0.8917 mL	1.7834 mL	4.4586 mL
DMSO	50 mM	0.0713 mL	0.3567 mL	0.7134 mL	1.7834 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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配液浓度

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

文献引用

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

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Brefeldin A

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溶解度

溶液配制表

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参考文献

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剂量换算

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