产品号 #73012_C
蛋白质运输抑制剂；抑制含sec7的鸟嘌呤交换因子（GEF）
总览
Brefeldin A 是一种由多种真菌（包括 Eupenicillium brefeldianum）产生的内酯类抗生素（Klausner 等人）。它通过间接抑制ADP -核糖基化因子（ARF）可逆地干扰高尔基体和内质网介导的蛋白质运输和分泌；（Klausner等；Helms & Rothman；Robinson等；Morinaga等；Moss & Vaughan；Nebenführ 等；Ktistakis等)。Brefeldin A在ARF-GDP- sec7界面与含sec7的鸟嘌呤交换因子（GEF）结合，阻止释放GDP和激活ARF所需的构象变化（Mossessova等人）。
细胞系发育
·在小鼠胚胎干细胞中，增强成簇规律间隔短回文重复序列（CRISPR介导的同源定向修复（HDR） （Yu等人）。
癌症研究
·诱导人类白血病（HL60, K562）和结肠癌（HT-29）细胞系的细胞凋亡（Shao等人）。
·可降低 Colo 205 结直肠癌干细胞系的存活率，诱导其凋亡并抑制其克隆生成活力（Tseng 等人）。
细胞类型
癌细胞及细胞系，多能干细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
应用
抗生素
研究领域
癌症，细胞系制备，干细胞生物学
CAS 编号
20350-15-6
化学式
C₁₆H₂₄O₄
纯度
≥98%
靶点
GEF
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
Resources and Publications
Educational Materials (2)
Publications (11)
Small molecules enhance CRISPR genome editing in pluripotent stem cells. Cell stem cell 2015 FEB
Abstract
The bacterial CRISPR-Cas9 system has emerged as an effective tool for sequence-specific gene knockout through non-homologous end joining (NHEJ), but it remains inefficient for precise editing of genome sequences. Here we develop a reporter-based screening approach for high-throughput identification of chemical compounds that can modulate precise genome editing through homology-directed repair (HDR). Using our screening method, we have identified small molecules that can enhance CRISPR-mediated HDR efficiency, 3-fold for large fragment insertions and 9-fold for point mutations. Interestingly, we have also observed that a small molecule that inhibits HDR can enhance frame shift insertion and deletion (indel) mutations mediated by NHEJ. The identified small molecules function robustly in diverse cell types with minimal toxicity. The use of small molecules provides a simple and effective strategy to enhance precise genome engineering applications and facilitates the study of DNA repair mechanisms in mammalian cells.
Brefeldin a effectively inhibits cancer stem cell-like properties and MMP-9 activity in human colorectal cancer Colo 205 cells. Molecules (Basel, Switzerland) 2013
Abstract
Cancer stem cells (CSCs) are a small subset of cancer cells with indefinite potential for self-renewal and the capacity to drive tumorigenesis. Brefeldin A (BFA) is an antibiotic that is known to block protein transport and induce endoplasmic reticulum (ER) stress in eukaryotic cells, but its effects on colorectal CSCs are unknown. We investigated the inhibitory effect of BFA on human colorectal cancer Colo 205 cells. We found that BFA effectively reduced the survival of suspension Colo 205 cells (IC₅₀ = ˜15 ng/mL) by inducing apoptosis, and inhibited the clonogenic activity of Colo 205 CSCs in tumorsphere formation assay and soft agar colony formation assay in the same nanogram per milliliter range. We also discovered that at such low concentrations, BFA effectively induced endoplasmic reticulum (ER) stress response as indicated by the increased mRNA expression of ER stress-related genes, such as glucose-regulated protein 78 (GRP78), X-box binding protein 1 (XBP1), and C/EBP homologous protein (CHOP). Finally, we found that BFA reduced the activity of matrix metallopeptidase 9 (MMP-9). These findings suggest that BFA can effectively suppress the progression of colorectal cancer during the tumorigenesis and metastasis stages. These results may lead to the development of novel therapies for the treatment of colorectal cancer.
The endosomal system of plants: charting new and familiar territories. Plant physiology 2008 AUG
Abstract
更多信息
| Species | Human, Mouse, Non-Human Primate, Other, Rat |
|---|---|
| Cas Number | 20350-15-6 |
| Chemical Formula | C₁₆H₂₄O₄ |
| Purity | ≥ 98% |
| Target | GEF |
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