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Bafilomycin A1

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Chemical Structure| 88899-55-2 同义名 : BafA1;NSC 381866
CAS号 : 88899-55-2
货号 : A614767
分子式 : C35H58O9
纯度 : 95%
分子量 : 622.83
MDL号 : MFCD06795130
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(80.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Proton Pump

    H+-ATPase, IC50:0.44 nM
描述 Bafilomycin A1, a macrolide antibiotic, is a potent and selective inhibitor of V-type H+-ATPase, and could disrupt pH regulation[1][2]. Bafilomycin A1 also showed moderate inhibition on ElE2 ATPases like K+-dependent (Kdp) ATPase from Escherichia coli, the Na+,K+-ATPase from ox brain, and the Ca2+-ATPase from sarcoplasmic reticulum, but F1Fo ATPases from bacteria and mitochondria are not affected by Bafilomycin A1[1]. Bafilomycin A1 can disrupt both autophagosome-lysosome fusion and autolysosome acidification constitute late steps in the autophagic process necessary to maintain functional autophagic flux and cellular homeostasis. Bafilomycin A1 induced a significant increase in cytosolic calcium concentration and disrupted Ca-P60A/SERCA-mediated fusion[3].
作用机制 Bafilomycin A1 disrupts autophagic flux by independently inhibiting V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion.[3]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human H4 cells 0.4 μM Function assay 24 h Induction of light chain 3-GFP level in human H4 cells at 0.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control 18024584
human HeLa cells 400 nM Function assay Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 400 nM 18391949
human MCF7 cells Function assay 4 h Inhibition of rapamycin-induced autophagy in human MCF7 cells expressing EGFP-LC3 assessed as decrease in EGFP levels at 100 nM after 4 hrs by Western blotting relative to control 20028134
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.03mL

1.61mL

0.80mL

16.06mL

3.21mL

1.61mL
参考文献

[1]Bowman EJ, Siebers A, et al. Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells. Proc Natl Acad Sci U S A. 1988 Nov;85(21):7972-6.

[2]van Schalkwyk DA, Chan XW, et al. Inhibition of Plasmodium falciparum pH regulation by small molecule indole derivatives results in rapid parasite death. Biochem Pharmacol. 2010 May 1;79(9):1291-9.

[3]Mauvezin C, Neufeld TP, et al. Bafilomycin A1 disrupts autophagic flux by inhibiting both V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion. Autophagy. 2015;11(8):1437-8.

[4]Yuan N, Song L, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015 Mar;100(3):345-56.

[5]Yan Y, Jiang K, et al. Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways. Sci Rep. 2016 Nov 15;6:37052.