Catalog Number: 1334
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
  • M.Wt:
    622.84
  • Formula:
    C35H58O9
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    88899-55-2
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.
Background References
  1. Chemistry and stucture activity relationships of bafilomycin A1, a potent and selective inhibitor of the vacuolar H+-ATPase.
    Gagliardi et al.
    Curr.Med.Chem., 1999;6:1197
  2. Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells.
    Yamamoto et al.
    Cell Struct.Funct., 1998;23:33
  3. Microtubules support production of starvation-induced autophagosomes but not their targeting and fusion with lysosomes.
    Fass et al.
    J.Biol.Chem., 2006;281:36303
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Bafilomycin A1 include:

25 Citations: Showing 1 - 10
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  1. Down regulated lncRNA MEG3 eliminates mycobacteria in macrophages via autophagy.
    Authors: Pawar Et al.
    Radiat Oncol 2016;6:19416
  2. Lysosomal two-pore channel subtype 2 (TPC2) regulates skeletal muscle autophagic signaling.
    Authors: Lin Et al.
    Sci Rep 2015;290:3377
  3. Calcium release through P2X4 activates calmodulin to promote endolysosomal membrane fusion.
    Authors: Cao Et al.
    Int J Mol Sci 2015;209:879
  4. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Clin Invest 2015;16:5555
  5. Cytosolic HMGB1 controls the cellular autophagy/apoptosis checkpoint during inflammation.
    Authors: Zhu Et al.
    J Biol Chem 2015;125:1098
  6. The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML.
    Authors: Obba Et al.
    J Cell Biol 2015;11:1114
  7. Release of monocyte migration signals by breast cancer cell lines after ablative and fractionated γ-irradiation.
    Authors: Hennel Et al.
    Mol Biol Cell 2014;9:85
  8. Identification of ML-9 as a lysosomotropic agent targeting autophagy and cell death.
    Authors: Kondratskyi Et al.
    Cell Death Dis 2014;5:e1193
  9. 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.
    Authors: Gutierrez Et al.
    J Biol Chem 2014;289:33568
  10. Chloroquine promotes IL-17 production by CD4+ T cells via p38-dependent IL-23 release by monocyte-derived Langerhans-like cells.
    Authors: Said Et al.
    J Immunol 2014;193:6135
  11. Polarized granzyme release is required for antigen-driven transendothelial migration of human effector memory CD4 T cells.
    Authors: Manes and Pober
    J Immunol 2014;193:5809
  12. Cell-intrinsic lysosomal lipolysis is essential for alternative activation of macrophages.
    Authors: Huang Et al.
    Nat Immunol 2014;15:846
  13. Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2.
    Authors: McAlpine Et al.
    Autophagy 2013;9:361
  14. Characteristics and requirements of basal autophagy in HEK 293 cells.
    Authors: Musiwaro Et al.
    Autophagy 2013;9:1407
  15. 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.
    Authors: Vincenzi Et al.
    PLoS One 2013;8:e65561
  16. Autophagy-mediated turnover of dynamin-related protein 1.
    Authors: Purnell and Fox
    BMC Neurosci 2013;14:86
  17. The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death.
    Authors: Robert Et al.
    Autophagy 2012;8:637
  18. Immunohistochemical detection of cytoplasmic LC3 puncta in human cancer specimens.
    Authors: Ladoire Et al.
    Autophagy 2012;8:1175
  19. West Nile virus growth is independent of autophagy activation.
    Authors: Beatman Et al.
    Virology 2012;433:262
  20. Negative regulation of signaling by a soluble form of toll-like receptor 9.
    Authors: Chockalingam Et al.
    Eur J Immunol 2011;41:2176
  21. Post-intoxication inhibition of botulinum neurotoxin serotype A within neurons by small-molecule, non-peptidic inhibitors.
    Authors: Ruthel Et al.
    Toxins (Basel) 2011;3:207
  22. Relieving autophagy and 4EBP1 from rapamycin resistance.
    Authors: Nyfeler Et al.
    Mol Cell Biol 2011;31:2867
  23. Notch post-translationally regulates β-catenin protein in stem and progenitor cells.
    Authors: Kwon Et al.
    Nat Cell Biol 2011;13:1244
  24. Beta1 integrin-dependent engulfment of Yersinia enterocolitica by macrophages is coupled to the activation of autophagy and suppressed by type III protein secretion.
    Authors: Deuretzbacher Et al.
    J Immunol 2009;183:5847
  25. Genome-wide siRNA-based functional genomics of pigmentation identifies novel genes and pathways that impact melanogenesis in human cells.
    Authors: Ganesan Et al.
    PLoS Genet 2008;4:e1000298
Expand to show all 25 Citations

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