Bafilomycin A1

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Cat.No. 1334 - Bafilomycin A1 | C35H58O9 | CAS No. 88899-55-2
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: ≥98% (HPLC)
Citations (25)

Biological Activity

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.

Technical Data

M. Wt 622.84
Formula C35H58O9
Storage Desiccate at -20°C
Purity ≥98% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 62.28 100

Preparing Stock Solutions

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

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.61 mL 8.03 mL 16.06 mL
5 mM 0.32 mL 1.61 mL 3.21 mL
10 mM 0.16 mL 0.8 mL 1.61 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet


References are publications that support the products' biological activity.

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

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

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

25 Citations for Bafilomycin A1

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

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

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

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

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

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

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

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

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

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

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

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

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