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Bafilomycin A1 (Baf-A1)

Name: Bafilomycin A1 (Baf-A1)
Brand: Selleck Chemicals
SKU: S1413
Rating: 5 (457 reviews)

Catalog No.S1413 Purity:97%

Bafilomycin A1(Baf-A1) is a vacuolar H⁺-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.

Bafilomycin A1 (Baf-A1) Chemical Structure

CAS No. 88899-55-2

Purity & Quality Control

Batch: Purity: >97%

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Signaling Pathway

Proton Pump Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human H4 cells	Function assay	0.4 μM	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
RAW 264.7 cells	Function assay	100 nM		Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as increased nitric oxide production in infected cells at 100 nM	19307359
mouse RAW264.7 cells	Apoptosis assay	100 nM	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
human HeLa cells	Function assay	400 nM		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
RAW 264.7 cells	Bactericidal activity assay	100 nM	16 h	Bactericidal activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as decrease in bacterial growth yield at 100 nM after 16 hrs postinfection by flow cytometry in presence of 10 ug/ml of intracellular replication inhi	19307359
RAW 264.7 cells	Antimicrobial activity assay	100 nM		Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as increased nitric oxide production in infected cells at 100 nM	19307359
RAW 264.7 cells	Antimicrobial activity assay	100 nM	30 mins	Antimicrobial activity against Salmonella enterica Typhimurium 14028 infected in RAW 264.7 cells assessed as inhibition of bacterial replication at 100 nM treated 30 mins before infection measured after 2 to 16 hrs postinfection by flow cytometry	19307359
rat 3Y1 cells	Function assay			Induction of morphological changes in rat 3Y1 cells assessed as elongation of cells	29701963
human Huh7.5.1 cells	Antiviral activity		3 h	Antiviral activity against HCV genotype 2a JFH-1 in human Huh7.5.1 cells assessed as reduction of viral entry up to 3 hrs by luciferase assay	26396683
Click to View More Cell Line Experimental Data

Biological Activity

Description

Bafilomycin A1(Baf-A1) is a vacuolar H⁺-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.

Targets

H+-ATPase ^[1]
(Cell-free assay)

0.44 nM

In vitro
In vitro	Bafilomycin A1 is a toxic macrolide antibiotic derived from Streptomyces griseus. Bafilomycin A1 inhibits the short circuit current induced by the outer mantle epithelium (OME). The IC50 and maximum inhibition dose of Bafilomycin A1 are 0.17 μM and 0.5 μM, respectively. ^[2] In addition, Bilomycin A1 inhibits the acid influx with an IC50 value of 0.4 nM. Bafilomycin A1 inhibits the acidification dose-dependently resulting in a lower quenching, and thus a higher fluorescence. ^[3] Bafilomycin A1 prevents the vacuolization of Hela cells induced by H. pylori, with an inhibitory concentration giving 50% of maximal (ID50) of 4 nM. Bafilomycin A1 is also very efficient in restoring vacuolated cells to a normal appearance. ^[4] Bafilomycin A1 also affects the transport of endocytosed material from early to late endocytic compartments. Bafilomycin not only dissipates the low endosomal pH but also blocks transport from early to late endosomes in HeLa cells. ^[5] Bafilomycin A1 at doses of 0.1-1 μM completely inhibits the acidification of lysosomes revealed by the incubation with acridine orange in BNL CL.2 and A431 cells. ^[6] When Bafilomycin A1 is added to Hanks' balanced salt solution, endogenous protein degradation is strongly inhibited and numerous autophagosomes accumulated in H-4-II-E cells. Bafilomycin A1 also prevents the appearance of endocytosed HRP in autophagic vacuoles. ^[7]
Kinase Assay	ATPase enzyme activity assays
Kinase Assay	The ATPase enzyme assay medium contains 6 mM MgSO₄, 50 mM HEPES (pH 7.4), 200 mM Na₂SO₃ (V-ATPase activator), 0.5 mM sodium ortho-vanadate (P-ATPase inhibitor), 0.5 mM sodium azide (F-ATPase inhibitor) and 3 mM Na₂ATP. This medium (1.0 mL), with or without the addition of the V-type ATPase inhibitor bafilomycin A1, is incubated with the filtered homogenate (0.1 mL) for 60 minutes at 23–25 °C. The reaction is stopped by the addition of 1 mL of TCA 3%. Spectrometric blanks are prepared as for the enzyme assay with the exception that the tissue sample is added after the acid. Phosphate analysis is accomplished by adding 2 mL of 1-butanol and 0.2 mL molybdate solution (5 g ammonium molybdate, 22 mL H₂SO₄ to 100 mL). After vortexing for 15 seconds the solution is neutralised with 0.5 mL citrate solution (100 g/500 mL, pH 7.0) and again vortexed for 15 seconds. The solution is then centrifuged (2000 × g; 3 minutes) to separate the butanol phase and the absorbance of this phase is read at 400 nm. Standards of orthophosphate are prepared (0.1 μM–2.0 μM) and treated in the same way as the enzyme activity assays. Enzyme activity is expressed in μmol of orthophosphate liberated per hour and per milligram of protein. V-ATPase activity is considered to be the difference between the total ATPase activity measured in the presence of Na₂SO₃, sodium orthovanadate and sodium azide and the ATPase activity measured in the presence of these reagents and of the specific V-ATPases inhibitor Bafilomycin A1.
Cell Research	Cell lines	HeLa cells
	Concentrations	~20 nM
	Incubation Time	20 hours
	Method	H. pylori bacteria extract is treated with inhibitors, before addition to HeLa cells, as follows: DCCD 10 mM for 1 hour at 30 ºC; NBD-CI 100 μM for 1 hour at 30 ºC and the reaction is blocked with glycine 10 mM final concentration; NEM 275 μM for 1 hour at 30 ºC and the reaction is blocked by addition of β-mercaptoethanol 275 mM; Mg-ATP 14 μM for 1 hour at 0 ºC; 100 μM KNO₃ and 14 μM Mg-ATP for 1 hour at 30 μM; NaCO₃ 100 μM, pH 11 for 1 hour at 0 ºC. The bacterial extract is then added to cell with a 40-fold dilution at a final concentration of 0.65 mg/mL. Controls are HeLa cells incubated with untreated bacterial extracts and cells treated with inhibitor Bafilomycin A1 under the same conditions as bacterial extracts, at the same concentrations or after a 40-fold dilution. The vacuotating activity of the bacterial extracts is assayed.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	Ret / EGFR / p75 NGFR		21559479
	Growth inhibition assay	Cell viability		20534000
	Immunofluorescence	AIF LC3		25512644
	ELISA	TNF-alpha		26240140

In Vivo
In vivo	Bafilomycin A1 (1 μM and 0.1 μM) completely inhibits the resorptive activity of cultured osteoclasts. ^[8] Bafilomycin A1 dose-dependently inhibits the rate of Na+ uptake in young tilapia with a Ki of 0.16 μM. ^[9]
Animal Research	Animal Models	Young (approximately 9 days old) Mozambique tilapia, Oreochromis mossambicus
	Dosages	10 μM
	Administration	--

References

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Chemical Information & Solubility

Molecular Weight	622.83	Formula	C₃₅H₅₈O₉
CAS No.	88899-55-2	SDF	Download Bafilomycin A1 (Baf-A1) SDF
Smiles	CC1CC(=CC=CC(C(OC(=O)C(=CC(=CC(C1O)C)C)OC)C(C)C(C(C)C2(CC(C(C(O2)C(C)C)C)O)O)O)OC)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.3mg/ml (0.48mM)	Taking the 1 mL working solution as an example, add 50 μL 6 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (8.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	1.65mg/ml (2.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
How to dissolve it？

Answer:
S1413 Bafilomycin A1(Baf-A1) is soluble in DMSO at 6 mg/ml. Please do not use alcohols as solvent, because this compound will degrade in alcohols.

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