21-O-デ(3-カルボキシ-1-オキソ-2-プロペニル)-2-デメチル-2-メトキシ-24-メチルヒグロリジン 化学特性,用途語,生産方法
説明
Bafilomycin A
1 is a fungal metabolite that has been found in
Streptomyces and has diverse biological activities. It is an inhibitor of vacuolar H
+-ATPases (V-ATPases; K
i = 0.5 nM in
N. crassa vacuolar membranes) and is greater than 1,000-fold selective for V-ATPases over Na
+/K
+-, Ca
2+-, and H
+-ATPases. Bafilomycin A
1 (100 nM) inhibits autophagosome maturation and protein degradation in H-4-II-E cells. It inhibits chloroquine-induced apoptosis in primary cerebellar granule neurons (CGNs) but not chloroquine-induced inhibition of macroautophagy. Bafilomycin A
1 (100 nM) reduces viral yield in the culture supernatant of Vero E6 and Huh7 cells, as well as HEK293T cells expressing human angiotensin-converting enzyme 2 (ACE2), infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). It also reduces lung RNA copy numbers and viral pneumonia in
ACE2 transgenic mice infected with SARS-CoV-2 when administered at a dose of 0.1 mg/kg.
化学的特性
white to off-white powder
使用
Bafilomycin A1 is a member of a potent family of macrocyclic lactones with broad spectrum biological activity, including activity against bacteria, yeast, fungi, nematodes, insects and tumour cell lines. Bafilomycin A1 is an inhibitor of vacuolar-type ATPase.
定義
ChEBI: The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.
一般的な説明
A macrolide antibiotic that acts as a specific inhibitor of vacuolar-type H
+-ATPase (V-type; K
i = 500 pM). A valuable tool for distinguishing among different types of ATPases. Blocks lysosomal cholesterol trafficking in macrophages and is known to interfere with pH regulation in brain cells. Exhibits cytotoxic effects on a number of cell lines in a cell viability assay. Reported to selectively inhibit β-secretase, an enzyme involved in the processing of amyloid precursor protein (APP). The InSolution format with a purity of ≥97% by HPLC in 90% DMSO is also available (Cat. No.
508409).
生物活性
Highly potent, selective inhibitor of vacuolar H + -ATPases (IC 50 = 500 pM as measured in chromaffin granule membranes). Selective over other ATP hydrolyzing enzymes such as F-ATPases, Ca 2+ -ATPases, Na + /K + -ATPases and plasma membrane H + -ATPases.
21-O-デ(3-カルボキシ-1-オキソ-2-プロペニル)-2-デメチル-2-メトキシ-24-メチルヒグロリジン 上流と下流の製品情報
原材料
準備製品