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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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
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。 |
靶点 |
|
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 |
Dose | Mice: 0.1 mg/kg, 1 mg/kg[4] (i.p.); 10 mg/kg[5] (intratumoral) |
Administration | i.p. |
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 |
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 |