1. Membrane Transporter/Ion Channel Autophagy Anti-infection Apoptosis
  2. Proton Pump Autophagy Antibiotic Bacterial Apoptosis
  3. Bafilomycin A1

Bafilomycin A1  (Synonyms: BafA1)

Cat. No.: HY-100558 Purity: 98.67%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Bafilomycin A1 Chemical Structure

Bafilomycin A1 Chemical Structure

CAS No. : 88899-55-2

Size Price Stock Quantity
100 μg USD 84 In-stock
500 μg USD 250 In-stock
1 mg USD 420 In-stock
5 mg USD 1050 In-stock
10 mg USD 1980 In-stock
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100 mg   Get quote  

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Customer Review

Based on 469 publication(s) in Google Scholar

Top Publications Citing Use of Products

452 Publications Citing Use of MCE Bafilomycin A1

IF
WB
Proliferation Assay

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Nature. 2022 Aug;608(7922):413-420.  [Abstract]

    Huh7 cells and ASGR1 KO cells are treated with 20 nM Bafilomycin A1 for 2 h.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Nat Biotechnol. 2022 Dec;40(12):1834-1844.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Nat Biotechnol. 2022 Dec;40(12):1834-1844.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Nat Nanotechnol. 2022 Sep;17(9):993-1003.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 May 3;8(1):40.  [Abstract]

    The levels of mitochondrial proteins including TIM23, TOM20, and TOM22 decreased along with decreased O-GlcNAcylation levels, which can be inhibited by BafA1.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2022 Feb 14;9(1):9.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Sep;288:121743.

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Sep;288:121743.

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Feb 17;6(1):67.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 May 4;33(5):971-987.e6.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Jan;19(1):67-78.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2021 Jun 3;28(6):1074-1089.e7.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2021 Oct;10(12):e12153.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Oct 9;9(10):1032.  [Abstract]

    Western blot showing SQSTM1 and LC3 levels in LN229 cells after treatment with 200 μM NSC 697855 (NTZ) and 200 nM Bafilomycin A1 (BAF) for 48 h.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Oct 3;9(10):1015.  [Abstract]

    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).

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Dec 13;9(12):1195.  [Abstract]

    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.

    Bafilomycin A1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Dec 13;9(12):1195.  [Abstract]

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    In Vitro

    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.

    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.

    Molecular Weight

    622.83

    Formula

    C35H58O9

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    C[C@H]([C@](O[C@@H]1C(C)C)(C[C@@H](O)[C@@H]1C)O)[C@H](O)[C@@H]([C@](OC(/C(OC)=C/C(C)=C\[C@@H](C)[C@@H](O)[C@@H](C)C2)=O)([H])[C@H](/C=C/C=C2\C)OC)C

    Structure Classification
    Initial Source

    Streptomyces griseus strains

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    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
    Concentration Solvent Mass 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
    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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    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 μL DMSO 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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.
     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.
    Purity & Documentation

    Purity: 99.43%

    References
    Cell Assay
    [2]

    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.

    Animal Administration
    [4]

    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.

    References

    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.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6056 mL 8.0279 mL 16.0557 mL 40.1394 mL
    5 mM 0.3211 mL 1.6056 mL 3.2111 mL 8.0279 mL
    10 mM 0.1606 mL 0.8028 mL 1.6056 mL 4.0139 mL
    15 mM 0.1070 mL 0.5352 mL 1.0704 mL 2.6760 mL
    20 mM 0.0803 mL 0.4014 mL 0.8028 mL 2.0070 mL
    25 mM 0.0642 mL 0.3211 mL 0.6422 mL 1.6056 mL
    30 mM 0.0535 mL 0.2676 mL 0.5352 mL 1.3380 mL
    40 mM 0.0401 mL 0.2007 mL 0.4014 mL 1.0035 mL
    50 mM 0.0321 mL 0.1606 mL 0.3211 mL 0.8028 mL
    60 mM 0.0268 mL 0.1338 mL 0.2676 mL 0.6690 mL
    80 mM 0.0201 mL 0.1003 mL 0.2007 mL 0.5017 mL
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      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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