Bafilomycin A1

Cat. No. 1334

Bafilomycin A1 C35H58O9 [88899-55-2]

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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

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

Soluble to 100 mM in DMSO
>98 %
Desiccate at -20°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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.

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.

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

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

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.

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

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.

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

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.

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.

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

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

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.

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.

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

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.

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

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.

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

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.

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.

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

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