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Bafilomycin A1

现货
Catalog No.
A8627
V-ATPase抑制剂
组合的产品项目
规格价格库存 数量
500ug
¥ 1,105.00
Ship with 10-15 days
1mg
¥ 2,106.00
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5mg
¥ 8,840.00
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Background

Bafilomycin A1 is a selective inhibitor of vacuolar H+ ATPases (V-ATPases) with I50 values of 4-400 nmol/mg 1.

Bafilomycin A1 was treated to different types of membrane ATPases with the dependent I50 of 400 nmol/mg, 4 nmol/mg and 50 nmol/mg for the vacuolar ATPases of a fungus (N. crassa), a plant (Z. mays), and an animal (bovine abrenal medulla). In addition, the inhibitory effect of bafilomycin A1 on vacuolar ATPases was further determined by testing its influence on H+-pumping activity. H+ translocation was completely inhibited by 10 nM bafilomycin A1 1. Other study has shown that bafilomycin A1 strongly inhibited the pit-forming activity of osteoclasts. The subcellular localization of V-ATPase in osteoclasts was been treated with or without bafilomycin A1 by immunoelectron microscopy. These results suggested that disruption of V-ATPase localization to the ruffled border by bafilomycin A1 resulted in the lack of acidification of the dentine surface 2.

Notes: I50 values is umol of bafilomycin AI per mg of protein giving 50% inhibition of ATPase activity.

References:
1. Bowman E J, Siebers A, Altendorf K. Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells[J]. Proceedings of the National Academy of Sciences, 1988, 85(21): 7972-7976.
2. Takami M, Suda K, Sahara T, et al. Involvement of vacuolar H+-ATPase in incorporation of risedronate into osteoclasts[J]. Bone, 2003, 32(4): 341-349.

文献引用

1. Xinchun Li, Li Zhong, et al. "Phosphorylation of IRS4 by CK1γ2 promotes its degradation by CHIP through the ubiquitin/lysosome pathway" Theranostics, 2018, Vol. 8, Issue13.
2. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525
3. Boyd Tressler, Andrea Michelle. "Mechanisms of Extracellular Nucleotide Accumulation During Regulated Cell Death in Tumor Cells."rave.ohiolink.edu,May 2016.
4. Liu, Shuangxin, et al. "Bovine parathyroid hormone enhances osteoclast bone resorption by modulating V-ATPase through PTH1R." International journal of molecular medicine (2015). PMID:26647715
5. Boyd-Tressler, Andrea, et al. "Chemotherapeutic Drugs Induce ATP Release via Caspase-gated Pannexin-1 Channels and a Caspase/Pannexin-1-Independent Mechanism." Journal of Biological Chemistry (2014): jbc-M114. PMID:25112874

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at -20°C
M.Wt622.84
Cas No.88899-55-2
FormulaC35H58O9
SolubilitySoluble in DMSO
Chemical Name(3Z,5E,7R,8S,9S,11E,13E,15S,16R)-16-[(2S,3R,4S)-4-[(2R,4R,5S,6R)-2,4-dihydroxy-5-methyl-6-propan-2-yloxan-2-yl]-3-hydroxypentan-2-yl]-8-hydroxy-3,15-dimethoxy-5,7,9,11-tetramethyl-1-oxacyclohexadeca-3,5,11,13-tetraen-2-one
SDFDownload SDF
Canonical SMILESCC1CC(=CC=CC(C(OC(=O)C(=CC(=CC(C1O)C)C)OC)C(C)C(C(C)C2(CC(C(C(O2)C(C)C)C)O)O)O)OC)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HeLa细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0 ~ 20 nM

实验结果

Bafilomycin A1呈剂量依赖性地抑制由幽门螺杆菌诱导的Hela细胞空泡化,在4 nM浓度下具有50%作用,在12.5 nM浓度下具有完全抑制。 此外,Bafilomycin A1还能有效促进空泡化细胞恢复至正常外观。

动物实验 [2]:

动物模型

年轻淡水罗非鱼

给药剂量

0 ~ 10-5 mol/L;30分钟

实验结果

在年轻的罗非鱼中,Bafilomycin A1呈剂量依赖性地抑制Na+摄取率,其Ki值为1.6 × 10-7 mol/L。 在低至10-8 mol/L的浓度下,Bafilomycin A1的抑制效应为20%。直到浓度达到10-6 mol/L之前,其抑制效应呈线性递增,然后保持在90 %左右。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Papini E, Bugnoli M, De Bernard M, Figura N, Rappuoli R, Montecucco C. Bafilomycin A1 inhibits Helicobacter pylori-induced vacuolization of HeLa cells. Mol Microbiol. 1993 Jan;7(2):323-7.

[2]. Fenwick JC, Wendelaar Bonga SE, Flik G. In vivo bafilomycin-sensitive Na(+) uptake in young freshwater fish. J Exp Biol. 1999 Dec;202 Pt 24:3659-66.

生物活性

描述 Bafilomycin A1是一种选择性的和可逆的空泡H+ ATPases(V-ATPases)抑制剂,IC50值介于4-400 nM之间。
靶点 V-ATPases          
IC50 4-400 nM          

质量控制

质量控制和MSDS

批次:

化学结构

Bafilomycin A1

相关生物数据

Bafilomycin A1
Bafilomycin A1 was able to decrease lysosomal/vesicular acid loading in Jurkat cells under the experimental conditions (STS+zVAD) used to stimulate ATP release [1].
1. Boyd-Tressler A, Penuela S, Laird D W, et al. Chemotherapeutic Drugs Induce ATP Release via Caspase-gated Pannexin-1 Channels and a Caspase/Pannexin-1-Independent Mechanism. Journal of Biological Chemistry, 2014: jbc. M114. 590240.

相关生物数据

Bafilomycin A1

相关生物数据

Bafilomycin A1

相关生物数据

Bafilomycin A1