|(3Z,5Z,7R,8S,9S,11E,13E,15S,16R)-16-((2S,3R,4S)-4-((2R,4R,5S,6R)-2,4-二羟基-6-异丙基-5-甲基四氢-2H-吡喃-2-基)-3-羟基戊基-2-基)-8-羟基-3,15-二甲氧基-5,7,9,11-四甲基氧杂环十六烷-3,5, 11,13-四烯-2-酮|CsnPharm

CAS No.: 88899-55-2

Bafilomycin A1/巴佛洛霉素A1 Catalog No. CSN10374

Synonyms: BafA1;NSC-381866;巴佛洛霉素A1

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

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 0.1 mg/kg, 1 mg/kg^[4] (i.p.); 10 mg/kg^[5] (intratumoral)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.1 mg/kg, 1 mg/kg^[4] (i.p.); 10 mg/kg^[5] (intratumoral)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6056 mL
- 8.0279 mL
- 16.0557 mL
- 5 mM
- 0.3211 mL
- 1.6056 mL
- 3.2111 mL
- 10 mM
- 0.1606 mL
- 0.8028 mL
- 1.6056 mL

技术信息

CAS号

88899-55-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C35H58O9

运输

蓝冰

分子量

622.83

别名

BafA1;NSC-381866;巴佛洛霉素A1

溶解度

DMSO	6.0 mg/mL (9.6 mM)

动物实验配方

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