布雷非德菌素 A

CAS: 20350-15-6 货号: B408392 分子式: C16H24O4 分子量: 280.36 Beilstein号: 25191 EC号: 606-528-3
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
B408392-1ml
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¥399.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 7 篇同行评审文献引用。

概述

Brefeldin A可溶于DMSO(20mg/ml),乙醇(5mg/ml)和甲醇(10mg/ml)。 使用说明: 1. Brefeldin A常见使用浓度范围为1-50μM。具体的最佳工作浓度请参考相关文献,或根据实验目的,以及所培养的特定细 胞和组织,通过实验进行摸索和优化。Brefeldin A,是一种常用的蛋白转运抑制剂,特异性地可逆地阻断蛋白质从内质网(ER)转运到高尔基体 (Golgi)。Brefeldin A处理后,高尔基体会很快被破坏,并融合到内质网上,该过程呈现能量、温度和微管依赖性。在哺乳动物和酵母中,Brefeldin A对蛋白从内质网向高尔基体转运的抑制可能是通过一类可以激活Afr1p GTPase的GTP-exchange factors来实现的。Arf1p在通过招募coat proteins到细胞内膜形成转运小泡(transport vesicles)的过程中起重要作用。Brefeldin A是一种真菌代谢产物,最初曾被用作抗病毒试剂,现在主要用于研究蛋白转运。Brefeldin A也常被用于抑制细胞因子等蛋白的分泌,并用于增强分泌蛋白的免疫染色检测。Brefeldin A 可激活神经鞘磷脂循环(sphingomyelin cycle),还可诱导一些肿瘤细胞发生凋亡。

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%

规格

英文别名
4H-Cyclopent[f]oxacyclotridecin-4-one, 1,6,7,8,9,11a,12,13,14,14a-decahydro-1,13-dihydroxy-6-methyl-, (1R,2E,6S,10E,11aS,13S,14aR)-
规格或纯度
10mM in DMSO
英文名称
Brefeldin A
生化机理
Brefeldin A是一种内酯类抗生素,也是蛋白质转运的ATP酶抑制剂,在HCT 116细胞中的IC50为0.2 μM,可诱导癌细胞分化和凋亡。它还能提高 HDR(同源定向修复)的效率,是 CRISPR 介导的 HDR 的增强剂。Brefeldin A 还是一种自噬和有丝分裂抑制剂。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
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
UN Number
分子量
280.36
Beilstein号
25191
Reaxy-Rn
30543489
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=30543489&ln=

技术文档

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高级数据

化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 100 mg/mL (139.33 mM);    
比旋光度
93° (C=2,MeOH)
熔点
201-205°C
安全和危险性(GHS)
信号词
危险
危险声明

H301: 吞咽会中毒

WGK Germany
3
RTECS
GY8410000
Merck Index
1369
个人防护装备
dust mask type N95 (US),Eyeshields,Faceshields,Gloves
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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找到1个结果

批号(Lot Number) 证书类型 货号
G2621460 分析证书 B408392
技术文档和文章
小分子抑制剂科研选型指南:最小证据链与场景化验证框架(含选型矩阵、案例卡片与产品表1–表4)
Small-Molecule Inhibitors: A Practical Guide for Research Selection — A Minimal Evidence Chain and Scenario-Based Validation Framework (Including a Selection Matrix, Case Cards, and Product Tables 1–4)
白介素29(IL-29/IFN-λ1):分子特征、信号网络与科研应用体系
Interleukin-29 (IL-29/IFN-λ1): Molecular Features, Signaling Networks, and a Systematic Framework for Research Applications
弗林蛋白酶(Furin)的结构特征、底物识别与科研应用综述
Furin: A Review of Its Structural Features, Substrate Recognition, and Research Applications
糖蛋白激素家族的分子特征、信号偏向性与体内动力学
Glycoprotein Hormone Family: Molecular Features, Signaling Bias, and In Vivo Pharmacokinetics
内质网应激下错误折叠蛋白的ERAD、ER-phagy与细胞命运调控
ERAD, ER-phagy, and Cell-Fate Regulation of Misfolded Proteins Under Endoplasmic Reticulum Stress
此产品的引用文献
溶液计算器

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本产品采用干冰配冷袋冷冻运输。收货后请立即拆包,并按上述储存条件保存;处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 20350-15-6,分子式为 C16H24O4,分子量为 280.36 g/mol。
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