Bafilomycin A1

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Description: H+-ATPase (vacuolar) inhibitor
Chemical Name: (3Z,5E,7R,8S,9S,11E,13E,15S,16R)-8-Hydroxy-16-[(1S,2R,3S)-2-hydroxy-1-methyl-3-[(2R,4R,5S,6R)-tetrahydro-2,4-dihydroxy-5-methyl-6-(1-methylethyl)-2H-pyran-2-yl]butyl]-3,15-dimethoxy-5,7,9,11-tetramethyloxacyclohexadeca-3,5,11,13-tetraen-2-one
Purity: ≥95% (HPLC)
Citations (52)
Reviews (3)

Biological Activity for Bafilomycin A1

Bafilomycin A1 is a highly potent, selective inhibitor of vacuolar H+-ATPases (IC50 = 0.6 - 1.5 nM in bovine chromaffin granules). Selective for v-ATPase over other ATP hydrolyzing enzymes such as F-ATPases and the H+/K+-ATPase (P-ATPase). Thought to inhibit autophagy either by blocking autophagosome-lysosome fusion (in H4IIE cells), or by blocking lysosomal degradation. Bafilomycin A1 accelerates wound healing in db/db mice. Low dose Bafilomycin A1 attenuates patient-derived CD34+CD19+ leukemia stem cells (LSC) and inhibits LSC proliferation in an animal model. Bafilomycin A1 impairs Zika virus infection in vitro.

Technical Data for Bafilomycin A1

M. Wt 622.84
Formula C35H58O9
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 88899-55-2
PubChem ID 72311
Smiles O[C@H]([C@H](C)/C=C(C)/C=C1OC)[C@@H](C)C/C(C)=C/C=C\[C@H](OC)C([C@@H](C)[C@H]([C@@H]([C@@]2(O)C[C@@H](O)[C@H](C)[C@@H]([C@H](C)C)O2)C)O)OC/1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Bafilomycin A1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 4.98 8

Preparing Stock Solutions for Bafilomycin A1

The following data is based on the product molecular weight 622.84. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.08 mM 20.07 mL 100.35 mL 200.69 mL
0.4 mM 4.01 mL 20.07 mL 40.14 mL
0.8 mM 2.01 mL 10.03 mL 20.07 mL
4 mM 0.4 mL 2.01 mL 4.01 mL

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Product Datasheets for Bafilomycin A1

Certificate of Analysis / Product Datasheet
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References for Bafilomycin A1

References are publications that support the biological activity of the product.

Gagliardi et al (1999) Chemistry and stucture activity relationships of bafilomycin A1, a potent and selective inhibitor of the vacuolar H+-ATPase. Curr.Med.Chem. 6 1197 PMID: 10519916

Yamamoto et al (1998) Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells. Cell Struct.Funct. 23 33 PMID: 9639028

Fass et al (2006) Microtubules support production of starvation-induced autophagosomes but not their targeting and fusion with lysosomes. J.Biol.Chem. 281 36303 PMID: 16963441

Mauthe et al (2018) Chloroquine inhibits autophagic flux by decreasing autophagosome-lysosome fusion. Autophagy 14 1435 PMID: 29940786

Wang et al (2020) Bafilomycin A1 accelerates chronic refractory wound healing in db/db mice. Biomed.Res.Int. 6265701 PMID: 32714982

Xu et al (2020) Bafilomycin A1 targets patient-derived CD34 + CD19 + leukemia stem cells. Haematologica 105 e17 PMID: 31097633

Sabino et al (2019) Bafilomycin A1 and U18666A efficiently impair ZIKV infection in vitro. Viruses 11 524 PMID: 31174294

If you know of a relevant reference for Bafilomycin A1, please let us know.

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Keywords: Bafilomycin A1, Bafilomycin A1 supplier, H+-ATPase, vacuolar, inhibitors, inhibits, Hydrogen-ATPase, Ion, Transporters, Pumps, BafilomycinA1, antibiotics, Antibiotics, Autophagy, 1334, Tocris Bioscience

52 Citations for Bafilomycin A1

Citations are publications that use Tocris products. Selected citations for Bafilomycin A1 include:

Huang et al (2014) Cell-intrinsic lysosomal lipolysis is essential for alternative activation of macrophages. Nat Immunol 15 846 PMID: 25086775

Gutierrez et al (2014) The anticancer agent di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT) overcomes prosurvival autophagy by two mechanisms: persistent induction of autophagosome synthesis and impairment of lysosomal integrity. J Biol Chem 289 33568 PMID: 25301941

Manes and Pober (2014) Polarized granzyme release is required for antigen-driven transendothelial migration of human effector memory CD4 T cells. J Immunol 193 5809 PMID: 25367116

Said et al (2014) Chloroquine promotes IL-17 production by CD4+ T cells via p38-dependent IL-23 release by monocyte-derived Langerhans-like cells. J Immunol 193 6135 PMID: 25385822

Kondratskyi et al (2014) Identification of ML-9 as a lysosomotropic agent targeting autophagy and cell death. Cell Death Dis 5 e1193 PMID: 24763050

Musiwaro et al (2013) Characteristics and requirements of basal autophagy in HEK 293 cells. Autophagy 9 1407 PMID: 23800949

Kwon et al (2011) Notch post-translationally regulates β-catenin protein in stem and progenitor cells. Nat Cell Biol 13 1244 PMID: 21841793

Nyfeler et al (2011) Relieving autophagy and 4EBP1 from rapamycin resistance. Mol Cell Biol 31 2867 PMID: 21576371

Ruthel et al (2011) Post-intoxication inhibition of botulinum neurotoxin serotype A within neurons by small-molecule, non-peptidic inhibitors. Toxins (Basel) 3 207 PMID: 22069707

Chockalingam et al (2011) Negative regulation of signaling by a soluble form of toll-like receptor 9. Eur J Immunol 41 2176 PMID: 21604257

Ganesan et al (2008) Genome-wide siRNA-based functional genomics of pigmentation identifies novel genes and pathways that impact melanogenesis in human cells. PLoS Genet 4 e1000298 PMID: 19057677

Boulakirba et al (2018) IL-34 and CSF-1 display an equivalent macrophage differentiation ability but a different polarization potential. Sci Rep 8 256 PMID: 29321503

Persaud et al (2018) Dynamin inhibitors block activation of mTORC1 by amino acids independently of dynamin. J Cell Sci 131 PMID: 29150487

Hennel et al (2014) Release of monocyte migration signals by breast cancer cell lines after ablative and fractionated γ-irradiation. Mol Biol Cell 9 85 PMID: 24666643

Vincenzi et al (2013) Pulsed electromagnetic fields increased the anti-inflammatory effect of A2A and A3 adenosine receptors in human T/C-28a2 chondrocytes and hFOB 1.19 osteoblasts. PLoS One 8 e65561 PMID: 23741498

Purnell and Fox (2013) Autophagy-mediated turnover of dynamin-related protein 1. BMC Neurosci 14 86 PMID: 23937156

McAlpine et al (2013) Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2. Autophagy 9 361 PMID: 23291478

Deuretzbacher et al (2009) Beta1 integrin-dependent engulfment of Yersinia enterocolitica by macrophages is coupled to the activation of autophagy and suppressed by type III protein secretion. J Immunol 183 5847 PMID: 19812190

Sagrillo-Fagundes et al (2019) Melatonin: The smart molecule that differentially modulates autophagy in tumor and normal placental cells. PLoS One 14 e0202458 PMID: 30629581

Nabissi et al (2016) Cannabinoids synergize with carfilzomib, reducing multiple myeloma cells viability and migration. Oncotarget 7 77543 PMID: 27769052

Kim et al (2015) Docosahexaenoic Acid Induces Cell Death in Human Non-Small Cell Lung Cancer Cells by Repressing mTOR via AMPK Activation and PI3K/Akt Inhibition. Biomed Res Int 2015 239764 PMID: 26339598

Hsu et al (2015) Cardiolipin remodeling by TAZ/tafazzin is selectively required for the initiation of mitophagy. Autophagy 11 643 PMID: 25919711

Hirasawa et al (2009) Extrasynaptic release of GABA by retinal DArgic neurons. J Neurophysiol 102 146 PMID: 19403749

Esposito et al (2021) TGF-β-induced DACT1 biomolecular condensates repress Wnt signalling to promote bone metastasis. Nat.Cell.Biol. 23 257 PMID: 33723425

Lee et al (2019) Absence of Cytosolic 2-Cys Prx Subtypes I and II Exacerbates TNF-α-Induced Apoptosis via Different Routes. Cell Rep 26 2194 PMID: 30784599

Su et al (2019) Anti-MET VHH Pool Overcomes MET-Targeted Cancer Therapeutic Resistance. Mol Cancer Ther 18 100 PMID: 30361332

Nassour et al (2019) Autophagic cell death restricts chromosomal instability during replicative crisis. Nature 565 659 PMID: 30675059

Huang et al (2019) The HGF-MET axis coordinates liver cancer metabolism and autophagy for chemotherapeutic resistance. Autophagy 1 PMID: 30786811

DeJesus et al (2016) Functional CRISPR screening identifies the ufmylation pathway as a regulator of SQSTM1/p62. Elife 5 PMID: 27351204

Holler et al (2016) Trehalose upregulates progranulin expression in human and mouse models of GRN haploinsufficiency: a novel therapeutic lead to treat frontotemporal dementia. Mol Neurodegener 11 46 PMID: 27341800

Gomes-da-Silva et al (2019) Recruitment of LC3 to damaged Golgi apparatus. Cell Death Differ 26 1467 PMID: 30349077

Verstegen et al (2014) Phosphorylation of synapsin I by cyclin-dependent kinase-5 sets the ratio between the resting and recycling pools of synaptic vesicles at hippocampal synapses. J Neurosci 34 7266 PMID: 24849359

Beatman et al (2012) West Nile virus growth is independent of autophagy activation. Virology 433 262 PMID: 22939285

Sica et al (2019) Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate. Cell Rep 27 820 PMID: 30995479

Ho et al (2019) Age-dependent accumulation of oligomeric SNCA/α-synuclein from impaired degradation in mutant LRRK2 knockin mouse model of Parkinson disease: role for therapeutic activation of chaperone-mediated autophagy (CMA). Autophagy 1 PMID: 30983487

Vidakovics et al (2019) Junín virus induces autophagy in human A549 cells. PLoS One 14 e0218730 PMID: 31216340

Hughes and Appel (2019) Oligodendrocytes express synaptic proteins that modulate myelin sheath formation. Nat Commun 10 4125 PMID: 31511515

Choi et al (2016) Hypoxia promotes noncanonical autophagy in nucleus pulposus cells independent of MTOR and HIF1A signaling. Autophagy 12 1631 PMID: 27314664

Obba et al (2015) The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML. J Cell Biol 11 1114 PMID: 26029847

Cao et al (2015) Calcium release through P2X4 activates calmodulin to promote endolysosomal membrane fusion. Int J Mol Sci 209 879 PMID: 26101220

Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. J Clin Invest 16 5555 PMID: 25768340

Zhu et al (2015) Cytosolic HMGB1 controls the cellular autophagy/apoptosis checkpoint during inflammation. J Biol Chem 125 1098 PMID: 25642769

Lin et al (2015) Lysosomal two-pore channel subtype 2 (TPC2) regulates skeletal muscle autophagic signaling. Sci Rep 290 3377 PMID: 25480788

Ladoire et al (2012) Immunohistochemical detection of cytoplasmic LC3 puncta in human cancer specimens. Autophagy 8 1175 PMID: 22647537

Robert et al (2012) The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death. Autophagy 8 637 PMID: 22498477

Pawar et al (2016) Down regulated lncRNA MEG3 eliminates mycobacteria in macrophages via autophagy. Radiat Oncol 6 19416 PMID: 26757825

Liu et al (2017) Lack of evidence for involvement of TonEBP and hyperosmotic stimulus in induction of autophagy in the nucleus pulposus. Sci Rep 7 4543 PMID: 28674405

Niessen et al (2017) Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors. Cell Chem Biol 24 1388 PMID: 28965727

Kondratskyi et al (2017) Ferroquine, the next generation antimalarial drug, has antitumor activity. Sci Rep 7 15896 PMID: 29162859

Jacquin et al (2017) Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation. Autophagy 13 854 PMID: 28296541

Dai et al (2017) Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK. Autophagy 13 1435 PMID: 28613987

Yuan et al (2018) A role for proteolytic regulation of δ-catenin in remodeling a subpopulation of dendritic spines in the rodent brain. J Biol Chem 293 11625 PMID: 29875160

Do you know of a great paper that uses Bafilomycin A1 from Tocris? Please let us know.

Reviews for Bafilomycin A1

Average Rating: 4.3 (Based on 3 Reviews.)

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By Xiaogang Wang on 06/24/2021
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Human Macrophages

We used BafA inhibitor to investigate the autophagy induced by bacterial toxins. To confirm whether BafA1 works, human macrophages were treated with or without 100 nM BafA for 1 h, and the levels of LC3-I and LC3-II within human macrophages were determined by western blot using LC3 antibody. As expected (shown in figure), treatment of cells with BafA1 resulted in an increased level of LC3-I and LC3-II, suggesting that the fusion of autophagosomes and lysosomes was blocked and resulted in the accumulation of autophagosomes.

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By shubham dubey on 05/28/2021
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: H9C2

Treated H9C2 cells to check the autophagy.

review image

Good autophagy inhibitor.
By JING HE on 03/27/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HT29

HT29 cells transfected with ad-mRFP-GFP-LC3 adenovirus after incubation with or without LPS and Baf A1 at different time points.

review image