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巴佛洛霉素A1 /Bafilomycin A1 {[allProObj[0].p_purity_real_show]}

货号:A614767 同义名: BafA1;NSC 381866

Bafilomycin A1 is an inhibitor of vacuolar H+-ATPase with IC50 of 0.44 nM.

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Bafilomycin A1 化学结构 CAS号:88899-55-2
Bafilomycin A1 化学结构
CAS号:88899-55-2
Bafilomycin A1 3D分子结构
CAS号:88899-55-2
Bafilomycin A1 化学结构 CAS号:88899-55-2
Bafilomycin A1 3D分子结构 CAS号:88899-55-2
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Bafilomycin A1 纯度/质量文件 产品仅供科研

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ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

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PFK-015 ++

PFKFB3, IC50: 207 nM

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ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

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ROC-325 99%+
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Autophagy, IC50: 40 nM

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Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Proton Pump 其他靶点 纯度
Zinc pyrithione 98+%
PF 03716556 ++++

H+/K+-ATPase, pIC50: ~6.5

98%
Lansoprazole 98%
Esomeprazole Magnesium 98%+
Rabeprazole 99%+
Ilaprazole TOPK 97%
Bafilomycin A1 ++++

H+-ATPase, IC50: 0.44 nM

95%
Pantoprazole sodium 98%
(R)-Lansoprazole 98%
Tenatoprazole 99%+
Omeprazole 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Bafilomycin A1 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]

Bafilomycin A1 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
mouse RAW264.7 cells 100 nM Apoptosis assay 16 h Induction of apoptosis in mouse RAW264.7 cells assessed as late apoptotic cells at 100 nM after 16 hrs using annexin V-propidium iodide staining by flow cytometry 19307359

Bafilomycin A1 动物研究

Dose Mice: 0.1 mg/kg, 1 mg/kg[4] (i.p.); 10 mg/kg[5] (intratumoral)
Administration i.p.

Bafilomycin A1 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.

Bafilomycin A1 实验方案

计算器
存储液制备 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

Bafilomycin A1 技术信息

CAS号88899-55-2
分子式C35H58O9
分子量 622.83
别名 BafA1;NSC 381866
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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