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Bafilomycine A1, un antibiotique macrolide isolé par des espèces Streptomyces, est un inhibiteur spécifique de ATPase (V-ATPase) de type vacuolaire H+. Bafilomycine A1 inhibe l'autophagie et induit l'apoptosis.
Bafilomycin A1, ein aus der Spezies Streptomyces isoliertes Makrolidantibiotikum, ist ein spezifischer Inhibitor der vacuolar-type H+ ATPase (V-ATPase). Bafilomycin A1 hemmt die autophagy und induziert die apoptosis.
Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H+-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
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Treatment with 249C or the autophagy inhibitor Bafilomycin A1 (BafA1; 30 nM), but not with the autophagy inducer rapamycin, resulted in upregulation of autophagy markers SQSTM1/p62 and LC3-I/II over time.
Treatment with 249C or the autophagy inhibitor Bafilomycin A1 (BafA1; 30 nM), but not with the autophagy inducer rapamycin, resulted in upregulation of autophagy markers SQSTM1/p62 and LC3-I/II over time.
Immunofluorescence (IF) images of phagocytosis and elimination of SC2-P (red) in the absence or presence of CIPS in THP-1 differentiated macrophages. The lysosomal inhibitor Bafilomycin A1 (BM; 100 nM; 6 h) is added to macrophages 6 h before the end of culture.
The levels of mitochondrial proteins including TIM23, TOM20, and TOM22 decreased along with decreased O-GlcNAcylation levels, which can be inhibited by BafA1.
GL261 and U251 cells are treated with 3-MA (5 mM), BafA1 (10 nM), AG-205 (10 µM), or RAPA (20 nM) for 1 h followed by IR or IR plus UTMD treatment for another 24 h.
Bafilomycin A1 (Baf; 50 nM) treatment significantly increases the percentage of both RFP+-GFP+-LC3 puncta and LC3 puncta in PDLSCs at 12 and 24 h during osteogenic induction, while there is no significant difference in the percentage of RFP+-GFP+-LC3 puncta or LC3 puncta between the Baf-treated I-PDLSCs and cells without the Baf treatment.
In response to the Bafilomycin A1 (Baf; 50 nM) treatment, increases LC3 II expression is observed in PDLSCs, and significant differences between the Baf-treated PDLSCs and cells without the Baf treatment are observed at 6 h and 12 h during osteogenic induction.
Representative images of cells with GFP or GFP-LC3 puncta, and the average number of GFP-LC3 puncta per cell in stable RFP-GFP-LC3 U87 cells treated with Justicidin A (JA) (0.13 μM), Justicidin B (JB) (0.13 μM), or Justicidin C (JC) (4 μM) in the presence or absence of Compound C (2.5 μM), SCH772984 (10 μM), LY294002 (25 μM), or Bafilomycin A1 (1 nM) for 24 h.
Western blot detection of YAP expression in HEK293T cells transfected with siControl or siATP6V0d2, followed by treatment with 100 nM Bafilomycin A1 (BafA1) for 6 h.
HeLa cells transfected with the ORF10-GFP plasmid and pEGFP-N1 are stimulated by poly(I:C) transfection and are then treated with MG132 (5 μM), Bafilomycin A1 (Baf A1; 5 nM), or Chloroquine (CQ; 40 μM) for 24 h.
Viability determined by cell counts of P, SA, and SAR iPSC-HSPCs treated with the V-ATPase inhibitor Bafilomycin A1 (Baf A1; 10 nM; 48 hours) compared with untreated cells.
Confocal microscopy analysis of the MVB marker CD63 in Coro1a‐Flag or Coro1a‐K233R‐Flag overexpressing HeLa cells treated with DMSO or 20 nM Bafilomycin A1 (Baf A1) for 12 h.
Representative western blot images of LC3 (LC3I and LC3II) in primary PTC are isolated from WT and TRPC6-/- mice after treatment with H2O2 (0.5 mM 12 h) in the presence and absence of Bafilomycin A1 (BAF) (20 nM).
Western analysis of the effect of GIT1 overexpression in increasing the LC3-II level under basal or starvation conditions with or without Bafilomycin A1 (Baf, 10 nM) in HEK293T cells.
Western analysis of the effect of GIT1 knockdown in lowering the LC3-II level under non-starvation or starvation conditions (1 h) with or without Bafilomycin A1 (Baf, 10 nM) in osteoclasts.
Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H+-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis[1][2][3].
IC50 & Target
Macrolide
Cellular Effect
Cell Line
Type
Value
Description
References
A549
EC50
0.6 nM
Compound: Baf A1
Cytoprotection activity against diphtheria toxin-induced cytotoxicity against human A549 cells assessed as effect on protein synthesis incubated for 20 hrs followed by replacement of [14c]-Leucine containing medium and measured after 4 hrs by liquid scint
Cytoprotection activity against diphtheria toxin-induced cytotoxicity against human A549 cells assessed as effect on protein synthesis incubated for 20 hrs followed by replacement of [14c]-Leucine containing medium and measured after 4 hrs by liquid scint
Bafilomycin A1 is treated to different types of membrane ATPases with the 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). The I50 values refer as μmol of Bafilomycin A1 per mg of protein giving 50% inhibition of ATPase activity[1].
Bafilomycin A1 ((-)-Bafilomycin A1) disrupts autophagic flux by inhibiting both V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion[2].
Bafilomycin A1 at a low concentration (1 nM) effectively and specifically inhibits and kills pediatric B-cell acute lymphoblastic leukemia cells. It targets both early and late stages of the autophagy pathway, mitochondria and induces caspase-independent apoptosis. Bafilomycin A1 induces the binding of Beclin 1 to Bcl-2, which further inhibits autophagy and promotes apoptotic cell death[5].
The growth of the BEL-7402 hepatocellular carcinoma and HO-8910 ovarian cancer cell lines are retarded and the metastatic potential is inhibited by Bafilomycin A1. Transmission electron microscopy and assays of capsase-3 and -9 suggest that Bafilomycin A1 induces apoptosis[6].
Bafilomycin A1 inhibits the growth of a variety of cultured cells dose-dependently, including golden hamster embryo and NIH-3T3 fibroblasts, whether or not they are transformed, and PC12 and HeLa cells. The IC50 of Bafilomycin A1 for inhibition of cell growth ranges from 10 to 50 nM[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bafilomycin A1 Related Antibodies
In Vivo
Chronic treatment with low-dose Bafilomycin A1 (0.1 mg/kg) slightly inhibits the tumor volume, but the final tumor volume does not differ significantly from the control. However, chronic treatment with high dose Bafilomycin A1 (1 mg/kg) inhibits the tumor growth significantly, compared with controls, after 21 days[8].
Bafilomycin A1 (0.1 mg/kg or 1 mg/kg; i.p. daily for 3 days) extends the survival of B-cell acute lymphoblastic leukemia (B-ALL) xenograft mice with advanced disease[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DMSO : 50 mg/mL (80.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.01 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (12.5 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Cells are harvested using 0.05% trypsin and suspended in culture medium containing 10% FCS, and 200 µL suspension is added to each well of a 96-well plate. Cells are cultured for 20 h for adhesion. Bafilomycin A1 is added to the wells at the final concentrations of 200, 400 and 800 nM, in triplicate. At 24, 48 and 72 h, 20 µl WST-1 is added to the cells. Following incubation at 37°C for 4 h, the plates are read to determine the optical density (OD) at 435 nm with 675 nm reference using a spectrophotometer[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Tumor-bearing mice are divided randomly into three experimental groups: a low-dose Bafilomycin A1 (0.1 mg/kg per day)-treated group (n=5), a high-dose Bafilomycin A1 (1 mg/kg per day)-treated group (n=5),and a control group (n=5). Tumor size is measured and tumor volume doubling time is calculated[4].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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