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 ActivityHighly 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.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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
Microtubules support production of starvation-induced autophagosomes but not their targeting and fusion with lysosomes.
Fass et al.
Chemistry and stucture activity relationships of bafilomycin A1, a potent and selective inhibitor of the vacuolar H+-ATPase.
Gagliardi et al.
Citations for Bafilomycin A1
The citations listed below are publications that use Tocris products. Selected citations for Bafilomycin A1 include:
51 Citations: Showing 1 - 10
The HGF-MET axis coordinates liver cancer metabolism and autophagy for chemotherapeutic resistance.
Authors: Huang Et al.
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).
Authors: Ho Et al.
Autophagic cell death restricts chromosomal instability during replicative crisis.
Authors: Nassour Et al.
Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate.
Authors: Sica Et al.
Cell Rep 2019;27:820
Absence of Cytosolic 2-Cys Prx Subtypes I and II Exacerbates TNF-α-Induced Apoptosis via Different Routes.
Authors: Lee Et al.
Cell Rep 2019;26:2194
Recruitment of LC3 to damaged Golgi apparatus.
Authors: Gomes-da-Silva Et al.
Cell Death Differ 2019;26:1467
Anti-MET VHH Pool Overcomes MET-Targeted Cancer Therapeutic Resistance.
Authors: Su Et al.
Mol Cancer Ther 2019;18:100
Junín virus induces autophagy in human A549 cells.
Authors: Vidakovics Et al.
PLoS One 2019;14:e0218730
Melatonin: The smart molecule that differentially modulates autophagy in tumor and normal placental cells.
Authors: Sagrillo-Fagundes Et al.
PLoS One 2019;14:e0202458
Oligodendrocytes express synaptic proteins that modulate myelin sheath formation.
Authors: Hughes and Appel
Nat Commun 2019;10:4125
IL-34 and CSF-1 display an equivalent macrophage differentiation ability but a different polarization potential.
Authors: Boulakirba Et al.
Sci Rep 2018;8:256
A role for proteolytic regulation of δ-catenin in remodeling a subpopulation of dendritic spines in the rodent brain.
Authors: Yuan Et al.
J Biol Chem 2018;293:11625
Dynamin inhibitors block activation of mTORC1 by amino acids independently of dynamin.
Authors: Persaud Et al.
J Cell Sci 2018;131
Lack of evidence for involvement of TonEBP and hyperosmotic stimulus in induction of autophagy in the nucleus pulposus.
Authors: Liu Et al.
Sci Rep 2017;7:4543
Ferroquine, the next generation antimalarial drug, has antitumor activity.
Authors: Kondratskyi Et al.
Sci Rep 2017;7:15896
Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.
Authors: Niessen Et al.
Cell Chem Biol 2017;24:1388
Pharmacological modulators of autophagy activate a parallel noncanonical pathway driving unconventional LC3 lipidation.
Authors: Jacquin Et al.
Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK.
Authors: Dai Et al.
Cannabinoids synergize with carfilzomib, reducing multiple myeloma cells viability and migration.
Authors: Nabissi Et al.
Down regulated lncRNA MEG3 eliminates mycobacteria in macrophages via autophagy.
Authors: Pawar Et al.
Radiat Oncol 2016;6:19416
Functional CRISPR screening identifies the ufmylation pathway as a regulator of SQSTM1/p62.
Authors: DeJesus Et al.
Hypoxia promotes noncanonical autophagy in nucleus pulposus cells independent of MTOR and HIF1A signaling.
Authors: Choi Et al.
Trehalose upregulates progranulin expression in human and mouse models of GRN haploinsufficiency: a novel therapeutic lead to treat frontotemporal dementia.
Authors: Holler Et al.
Mol Neurodegener 2016;11:46
Lysosomal two-pore channel subtype 2 (TPC2) regulates skeletal muscle autophagic signaling.
Authors: Lin Et al.
Sci Rep 2015;290:3377
Calcium release through P2X4 activates calmodulin to promote endolysosomal membrane fusion.
Authors: Cao Et al.
Int J Mol Sci 2015;209:879
Docosahexaenoic Acid Induces Cell Death in Human Non-Small Cell Lung Cancer Cells by Repressing mTOR via AMPK Activation and PI3K/Akt Inhibition.
Authors: Kim Et al.
Biomed Res Int 2015;2015:239764
Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
Authors: Lin Et al.
J Clin Invest 2015;16:5555
Cytosolic HMGB1 controls the cellular autophagy/apoptosis checkpoint during inflammation.
Authors: Zhu Et al.
J Biol Chem 2015;125:1098
Cardiolipin remodeling by TAZ/tafazzin is selectively required for the initiation of mitophagy.
Authors: Hsu Et al.
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
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
Identification of ML-9 as a lysosomotropic agent targeting autophagy and cell death.
Authors: Kondratskyi Et al.
Cell Death Dis 2014;5:e1193
Phosphorylation of synapsin I by cyclin-dependent kinase-5 sets the ratio between the resting and recycling pools of synaptic vesicles at hippocampal synapses.
Authors: Verstegen Et al.
J Neurosci 2014;34:7266
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
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
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
Cell-intrinsic lysosomal lipolysis is essential for alternative activation of macrophages.
Authors: Huang Et al.
Nat Immunol 2014;15:846
Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2.
Authors: McAlpine Et al.
Characteristics and requirements of basal autophagy in HEK 293 cells.
Authors: Musiwaro Et al.
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
Autophagy-mediated turnover of dynamin-related protein 1.
Authors: Purnell and Fox
BMC Neurosci 2013;14:86
The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death.
Authors: Robert Et al.
Immunohistochemical detection of cytoplasmic LC3 puncta in human cancer specimens.
Authors: Ladoire Et al.
West Nile virus growth is independent of autophagy activation.
Authors: Beatman Et al.
Negative regulation of signaling by a soluble form of toll-like receptor 9.
Authors: Chockalingam Et al.
Eur J Immunol 2011;41:2176
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
Relieving autophagy and 4EBP1 from rapamycin resistance.
Authors: Nyfeler Et al.
Mol Cell Biol 2011;31:2867
Notch post-translationally regulates β-catenin protein in stem and progenitor cells.
Authors: Kwon Et al.
Nat Cell Biol 2011;13:1244
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
Extrasynaptic release of GABA by retinal DArgic neurons.
Authors: Hirasawa Et al.
J Neurophysiol 2009;102:146
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
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HT29 cells transfected with ad-mRFP-GFP-LC3 adenovirus after incubation with or without LPS and Baf A1 at different time points.