Potent and selective inhibitor of vacuolar H+ATPases
Compound used to study autophagy in a variety of cells
Highly cited
Bafilomycin A1 is a macrolide antibiotic produced by Streptomyces with diverse biological activities. Bafilomycin A1 acts as a potent and selective inhibitor of vacuolar-type H+-ATPase (V-type) (IC50=0.04-0.4nmol/mg). Bafilomycin A1 is a valuable tool for distinguishing among different types of ATPases. Bafilomycin A1 inhibits endosomal acidification, lysosomal cholesterol trafficking, as well as autophagosome maturation and protein degradation. Bafilomycin A1 also blocks pH regulation in brain cells.
Product Details
Alternative Name:
NSC 381866
Formula:
C35H58O9
MW:
622.8
Source:
Streptomyces griseus
CAS:
88899-55-2
Purity:
≥95% (HPLC, TLC)
Appearance:
White powder to colorless film.
Solubility:
Soluble in DMSO (5mg/ml), 100% ethanol, or 100% methanol (5mg/ml).
Shipping:
Blue Ice
Long Term Storage:
-20°C
Use/Stability:
Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C.
Handling:
Protect from light.
Technical Info/Product Notes:
Typical concentrations for use in cell culture are 50-100nM. Note: Product is not sterile.
Regulatory Status:
RUO - Research Use Only
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Product Literature References
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Mono-ADP-ribosylation by PARP10 inhibits Chikungunya virus nsP2 proteolytic activity and viral replication: S. Krieg, et al.; Cell. Mol. Life Sci. 80, 72 (2023), Abstract;
ALFY localizes to early endosomes and cellular protrusions to facilitate directional cell migration: K. Soreng, et al.; J. Cell Sci. 135, jcs259138 (2022), Abstract; Full Text
Autophagy promotes cell survival by maintaining NAD levels: T. Kataura, et al.; Dev. Cell 57, 2584 (2022), Abstract;
Baicalein activates parkin-dependent mitophagy through NDP52 and OPTN: P. Ke, et al.; Cells 11, 1132 (2022), Abstract; Full Text
Basal autophagy is necessary for a pharmacologic PPARα transactivation: E.Y. Kim, et al.; Cells 11, 754 (2022), Abstract; Full Text
BNIP3L/NIX regulates both mitophagy and pexophagy: L.P. Wilhelm, et al.; EMBO J. 41, e111115 (2022), Abstract; Full Text
CFTR modulators restore acidification of autophago-lysosomes and bacterial clearance in cystic fibrosis macrophages: A. Badr, et al.; Front. Cell. Infect. Microbiol. 12, 819554 (2022), Abstract; Full Text
Compounds activating VCP D1 ATPase enhance both autophagic and proteasomal neurotoxic protein clearance: L. Wrobel, et al.; Nat. Commun. 13, 4146 (2022), Abstract;
Lipid droplet turnover at the lysosome inhibits growth of hepatocellular carcinoma in a BNIP3-dependent manner: D.E. Berardi, et al.; Sci. Adv. 8, eabo2510 (2022), Abstract; Full Text
NRF2 activation in autophagy defects suppresses a pharmacological transactivation of the nuclear receptor FXR: E.Y. Kim, et al.; Antioxidants 11, 370 (2022), Abstract; Full Text
Target protein localization and its impact on PROTAC-mediated degradation: L.M. Simpson, et al.; Cell Chem. Biol. 29, 1482 (2022), Abstract;
The cholesterol transport protein GRAMD1C regulates autophagy initiation and mitochondrial bioenergetics: M.Y.W. Ng, et al.; Nat. Commun. 13, 6283 (2022), Abstract; Full Text
Ubiquitylation of RIPK3 beyond-the-RHIM can limit RIPK3 activity and cell death: D. Frank, et al.; iScience 25, 104632 (2022), Abstract; Full Text
V. cholerae MakA is a cholesterol-binding pore-forming toxin that induces non-canonical autophagy: X. Jia, et al.; J. Cell Biol. 221, e202206040 (2022), Abstract; Full Text
ABCE1 Regulates RNase L-Induced Autophagy during Viral
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ALK inhibition activates LC3B-independent, protective autophagy in EML4-ALK positive lung cancer cells: A.M. Schläfli, et al.; Sci. Rep. 11, 9011 (2021), Abstract; Full Text
Analysis of lysosomal hydrolase trafficking and activity in human iPSC-derived neuronal models: L.K. Cuddy, et al.; STAR Protoc. 2, 100340 (2021), Abstract; Full Text
ATG4D is the main ATG8 delipidating enzyme in mammalian cells and protects against cerebellar neurodegeneration: I. Tamargo-Gomez, et al.; Cell Death Differ. 28, 2651 (2021), Abstract; Full Text
Contribution of Particle-Induced Lysosomal Membrane Hyperpolarization to Lysosomal Membrane Permeabilization: T. Ziglari, et al.; Int. J. Mol. Sci. 22, 2277 (2021), Abstract; Full Text
Ecd promotes U5 snRNP maturation and Prp8 stability: S. Erkelenz, et al.; Nucleic Acids Res. 49, 1688 (2021), Abstract; Full Text
GAK and PRKCD are positive regulators of PRKN-independent mitophagy: M.J. Munson, et al.; Nat. Commun. 12, 6101 (2021), Abstract; Full Text
Gasdermin D restricts Burkholderia cenocepacia infection in vitro and in vivo: S. Estfanous, et al.; Sci. Rep. 11, 855 (2021), Abstract; Full Text
Genotoxic stress-activated DNA-PK-p53 cascade and autophagy cooperatively induce ciliogenesis to maintain the DNA damage response: T. Chen, et al.; Cell Death Differ. 28, 1865 (2021), Abstract; Full Text
Glucose starvation induces autophagy via ULK1-mediated activation of PIKfyve in an AMPK-dependent manner: C. Karabiyik, et al.; Dev. Cell 56, 1961 (2021), Abstract;
GSK3B induces autophagy by phosphorylating ULK1: H.Y. Ryu, et al.; Exp. Mol. Med. 53, 369 (2021), Abstract;
Identification of a novel compound that simultaneously impairs the ubiquitin-proteasome system and autophagy: T.A. Giovannucci, et al.; Autophagy 5, 1554862 (2021), Abstract;
Intracellular localisation of Mycobacterium tuberculosis affects efficacy of the antibiotic pyrazinamide: P. Santucci, et al.; Nat. Commun. 12, 3816 (2021), Abstract; Full Text
Macrophage autophagy protects against hepatocellular carcinogenesis in mice: A. Deust, et al.; Sci. Rep. 11, 18809 (2021), Abstract;
Mitochondrial and Clearance Impairment in p.D620N VPS35 Patient-Derived Neurons: Z. Hanss, et al.; Mov. Disord. 36, 704 (2021), Application(s): Treatment of iPSCs-derived neurons, Abstract; Full Text
Neuronal autophagy regulates presynaptic neurotransmission by controlling the axonal endoplasmic reticulum: M. Kuijpers, et al.; Neuron 109, 299 (2021), Abstract; Full Text
Non-canonical glutamate signaling in a genetic model of migraine with aura: P.D. Parker, et al.; Neuron 109, 611 (2021), Abstract;
Perturbation of Cellular Redox Homeostasis Dictates Divergent Effects of Polybutyl Cyanoacrylate (PBCA) Nanoparticles on Autophagy: T. Sønstevold, et al.; Cells 10, 3432 (2021), Abstract;
Phenotypic Assay Leads to Discovery of Mitophagy Inducers with Therapeutic Potential for Parkinson’s Disease: I. Maestro, et al.; ACS Chem. Neurosci. 12, 4512 (2021), Abstract;
SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation: D.W. Sanders, et al.; Elife 10, e65962 (2021), Abstract; Full Text
TFEB phosphorylation on Serine 211 is induced by autophagy in human synovial fibroblasts and by p62/SQSTM1 overexpression in HEK293 cells: B. Relic, etr al.; Biochem. J. 478, 3099 (2021), Abstract;
The SZT2 Interactome Unravels New Functions of the KICSTOR Complex: C. Cattelani, et al.; Cells 10, 2711 (2021), Abstract;
The ULK1 kinase, a necessary component of the pro-regenerative and anti-aging machinery in Hydra: N. Suknovic, et al.; Mech. Ageing Dev. 194, 111414 (2021), Abstract;
Transcription- and phosphorylation-dependent control of a functional interplay between XBP1s and PINK1 governs mitophagy and potentially impacts Parkinson disease pathophysiology: W. El Manaa, et al.; Autophagy 17, 4363 (2021), Abstract;
A conserved ATG2‐GABARAP family interaction is critical for phagophore formation: M. Bozic, et al.; EMBO Rep. 21, e48412 (2020), Abstract; Full Text
A DNM2 centronuclear myopathy mutation reveals a link between recycling endosome scission and autophagy: C. Puri, et al.; Dev. Cell 53, 154 (2020), Abstract;
AMPK-dependent activation of the Cyclin Y/CDK16 complex controls autophagy: M. Dohmen, et al.; Nat. Commun. 11, 1032 (2020), Abstract; Full Text
Antibody RING-mediated destruction of endogenous proteins: A.F.M. Ibrahim, et al.; Mol. Cell 79, 155 (2020), Abstract; Full Text
Autophagic death of neural stem cells mediates chronic stress-induced decline of adult hippocampal neurogenesis and cognitive deficits: S. Jung, et al.; Autophagy 16, 512 (2020), Abstract; Full Text
CASP9 (caspase 9) is essential for autophagosome maturation through regulation of mitochondrial homeostasis: H. An, et al.; Autophagy 16, 1598 (2020), Abstract; Full Text
Cordycepin inhibits human gestational choriocarcinoma cell growth by disrupting centrosome homeostasis: C. Wang, et al.; Drug Des. Devel. Ther. 14, 2987 (2020), Abstract; Full Text
High levels of ROS impair lysosomal acidity and autophagy flux in glucose-deprived fibroblasts by activating ATM and erk pathways: S.B. Song, et al.; Biomolecules 10, 761 (2020), Abstract; Full Text
Inducible degradation of target proteins through a tractable affinity-directed protein missile system: L.M. Simpson, et al.; Cell Chem. Biol. 27, 1164 (2020), Abstract; Full Text
Interleukin (IL)-6: a friend or foe of pregnancy and parturition? Evidence from functional studies in fetal membrane cells: C. Omere, et al.; Front. Physiol. 11, 891 (2020), Abstract; Full Text
K63-linked ubiquitylation induces global sequestration of mitochondria: T.J.C. Richard, et al.; Sci. Rep. 10, 22334 (2020), Abstract; Full Text
Lysosomal dysfunction and autophagy blockade contribute to MDMA-induced neurotoxicity in SH-SY5Y neuroblastoma cells: I.H. Li, et al.; Chem. Res. Toxicol. 33, 903 (2020), Abstract;
MLKL trafficking and accumulation at the plasma membrane control the kinetics and threshold for necroptosis: A.L. Samson, et al.; Nat. Commun. 11, 3151 (2020), Abstract; Full Text
mTORC2 assembly is regulated by USP9X-mediated deubiquitination of RICTOR: L. Wrobel, et al.; Cell Rep. 33, 108564 (2020), Abstract;
Noncanonical inhibition of caspase-3 by a nuclear microRNA confers endothelial protection by autophagy in atherosclerosis: D. Santovito, et al. ; Sci. Transl. Med. 12, eaaz2294 (2020), Abstract;
Photocrosslinking activity-based probes for ubiquitin RING E3 ligases: S. Mathur, et al.; Cell Chem. Biol. 27, 74 (2020), Abstract; Full Text
Semi-automated quantitation of mitophagy in cells and tissues: L. Montava-Garriga, et al.; Mech. Ageing Dev. 185, 111196 (2020), Abstract; Full Text
Stretch, scratch, and stress: Suppressors and supporters of senescence in human fetal membranes: L.S. Richardson, et al.; Placenta 99, 27 (2020), Abstract; Full Text
Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis: A. Bensimon, et al.; Cell Chem. Biol. 27, 728 (2020), Abstract; Full Text
The insufficiency of ATG4A in macroautophagy: N. Nguyen, et al.; J. Biol. Chem. 295, 13584 (2020), Abstract; Full Text
ATG2 transports lipids to promote autophagosome biogenesis: D.P. Valverde, et al.; J. Cell Biol. 218, 1787 (2019), Abstract; Full Text
Autophagy mediates astrogenesis in adult hippocampal neural stem cells: S. Ha, et al.; Exp. Neurobiol. 28, 229 (2019), Abstract; Full Text
Bypassing pan-enterovirus host factor PLA2G16: J. Baggen, et al.; Nat. Commun. 10, 3171 (2019), Abstract; Full Text
Distinct functions of ATG16L1 isoforms in membrane binding and LC3B lipidation in autophagy-related processes: A.H. Lystad, et al.; Nat. Cell Biol. 21, 372 (2019), Abstract; Full Text
Docosahexaenoic acid inhibits both NLRP3 inflammasome assembly and JNK-mediated mature IL-1β secretion in 5-fluorouracil-treated MDSC: implication in cancer treatment: A. Dumont, et al.; Cell Death Dis. 10, 485 (2019), Abstract; Full Text
ER-targeted Beclin 1 supports autophagosome biogenesis in the absence of ULK1 and ULK2 kinases: T. Anwar, et al.; Cells 8, 475 (2019), Abstract; Full Text
Excess hepsin proteolytic activity limits oncogenic signaling and induces ER stress and autophagy in prostate cancer cells: R.Willbold, et al.; Cell Death Dis. 10, 601 (2019), Abstract; Full Text
Increased autophagy in EphrinB2-deficient osteocytes is associated with elevated secondary mineralization and brittle bone: C. Vrahnas, et al.; Nat. Commun. 10, 3436 (2019), Abstract; Full Text
Neuropathy-causing mutations in HSPB1 impair autophagy by disturbing the formation of SQSTM1/p62 bodies: M. Haidar, et al.; Autophagy 15, 1051 (2019), Abstract; Full Text
Prevention of crystalline silica-induced inflammation by the anti-malarial hydroxychloroquine: R. Burmeister, et al.; Inhal. Toxicol. 31, 274 (2019), Abstract; Full Text
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models: M.C. Silva, et al.; Elife 8, e45457 (2019), Abstract; Full Text
A stably self-renewing adult blood-derived induced neural stem cell exhibiting patternability and epigenetic rejuvenation: C. Sheng, et al.; Nat Commun. 9, 4047 (2018), Abstract; Full Text
Nonlinear relationship between ER Ca2+ depletion versus induction of the unfolded protein response, autophagy inhibition, and cell death: P. Szalai, et al.; Cell Calcium 76, 48 (2018), Abstract;
Oxidation of SQSTM1/p62 mediates the link between redox state and protein homeostasis: B. Carroll, et al.; Nat. Commun. 9, 256 (2018), Abstract; Full Text
The IAP family member BRUCE regulates autophagosome-lysosome fusion: P. Ebner, et al.; Nat. Commun. 9, 599 (2018), Abstract; Full Text
Senolytic drugs target alveolar epithelial cell function and attenuate experimental lung fibrosis ex vivo: M. Lehmann, et al.; Eur. Respir. J. 50, 1602367 (2017), Abstract; Full Text
Identification of V-ATPase as a molecular sensor of SOX11-levels and potential therapeutic target for mantle cell lymphoma: V.K. Emruli, et al.; BMC Cancer 16, 493 (2016), Application(s): Transient knock-down of V-ATPase, Abstract; Full Text
Legionella pneumophilaS1P-lyase targets host sphingolipid metabolism and restrains autophagy: M. Rolando, et al.; PNAS 113, 1901 (2016), Abstract; Full Text
Neutrophil and Alveolar Macrophage-Mediated Innate Immune Control of Legionella pneumophila Lung Infection via TNF and ROS: P. Ziltener, et al.; PLoS One 12, e1005591 (2016), Application(s): Cell culture, Abstract; Full Text
Resveratrol induces autophagy by directly inhibiting mTOR through ATP competition: D. Park, et al.; Sci. Rep. 6, 21772 (2016), Application(s): Cell culture, Abstract; Full Text
SQSTM1/p62 mediates crosstalk between autophagy and the UPS in DNA repair: G. Hewitt, et al.; Autophagy 12, 1917 (2016), Abstract; Full Text
Pharmacological Inhibition of ULK1 Blocks mTOR-Dependent Autophagy: K. J. Petherick, et al.; J. Biol. Chem. 290, 11376 (2015), Application(s): Cell Culture, Abstract; Full Text
Reliable LC3 and p62 autophagy marker detection in formalin fixed paraffin embedded human tissue by immunohistochemistry: A.M. Schläfli, et al.; Eur. J. Histochem. 59, 137 (2015), Application(s): Cell Culture, Abstract; Full Text
Revealing the fate of cell surface human P-glycoprotein (ABCB1): The Lysosomal Degradation Pathway: K. Katayama, et al.; Biochim. Biophys. Acta 1853, 2361 (2015), Application(s): Cell Culture, Abstract;
The role of cytoplasmic-to-lysosomal pH gradient in hydrophobic weak base drug sequestration in lysosomes: B. Zhitomirsky, et al.; Cancer Cell Microenviron. 2, e807 (2015), Application(s): Cell Culture, Fluorescence Microscopy, Full Text
Inhibition of GATE-16 attenuates ATRA-induced neutrophil differentiation of APL cells and interferes with autophagosome formation: D. Brigger, et al.; Biochem. Biophys. Res. Commun. 438, 283 (2013), Application(s): Fluorescence Microscopy, PCR, WB, Abstract;
The (pro)renin receptor ((P)RR) can act as a repressor of Wnt signalling: S.M. Bernhard, et al.; Biochem. Pharmacol. 84, 1643 (2012), Application(s): WB, Cell Lysis, Abstract;
Autophagy, bafilomycin and cell death: the "a-B-cs" of plecomacrolide-induced neuroprotection: J.J. Shacka, et al.; Autophagy 2, 228 (2006), Review, Abstract;
Bafilomycin A1-sensitive pathway is required for the maturation of cystic fibrosis transmembrane conductance regulator: T. Okiyoneda, et al.; Biochim. Biophys. Acta 1763, 1017 (2006), Abstract;
Reduced capacitative calcium entry correlates with vesicle accumulation and apoptosis: S. Jaydev, et al.; J. Biol. Chem. 274, 8261 (1999), Abstract;
Bafilomycins and concanamycins as inhibitors of V-ATPases and P-ATPases: S. Dröse & K. Altendorf; J. Exp. Biol. 200, 1 (1997), Abstract;
Inhibition of mitogen-induced DNA synthesis by bafilomycin A1 in Swiss 3T3 fibroblasts: A.J. Saurin, et al.; Biochem. J. 313, 65 (1996), Abstract;
Cell-type and amyloid precursor protein-type specific inhibition of A beta release by bafilomycin A1, a selective inhibitor of vacuolar ATPases: J. Knops, et al.; J. Biol. Chem. 270, 2419 (1995), Abstract; Full Text
Inositol trisphosphate-dependent and -independent Ca2+ mobilization pathways at the vacuolar membrane of Candida albicans: C.M. Calvert & D. Sanders; J. Biol. Chem. 270, 7272 (1995), Abstract; Full Text
Specific inhibitors of vacuolar type H(+)-ATPases induce apoptotic cell death: T. Nishihara, et al.; BBRC 212, 255 (1995), Abstract;
The vacuolar H(+)-ATPase inhibitor bafilomycin A1 differentially affects proteolytic processing of mutant and wild-type beta-amyloid precursor protein: C. Haass, et al.; J. Biol. Chem. 270, 6186 (1995), Abstract; Full Text
Active vacuolar H+ATPase is required for both endocytic and exocytic processes during viral infection of BHK-21 cells: H. Palokangas, et al.; J. Biol. Chem. 269, 17577 (1994), Abstract; Full Text
Bafilomycin inhibits proton flow through the H+ channel of vacuolar proton pumps: B.P. Crider, et al.; J. Biol. Chem. 269, 17379 (1994), Abstract; Full Text
A depolarization-stimulated, bafilomycin-inhibitable H+ pump in hippocampal astrocytes: C.A. Pappas & B.R. Ransom; Glia 9, 280 (1993), Abstract;
Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, blocks lysosomal cholesterol trafficking in macrophages: T. Furuchi, et al.; J. Biol. Chem. 268, 27345 (1993), Abstract; Full Text
Inhibitory effect of modified bafilomycins and concanamycins on P- and V-type adenosinetriphosphatases: S. Drose, et al.; Biochemistry 32, 3902 (1993), Abstract;
Bafilomycin A1 inhibits the targeting of lysosomal acid hydrolases in cultured hepatocytes: K. Oda, et al.; BBRC 178, 369 (1991), Abstract;
Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, inhibits acidification and protein degradation in lysosomes of cultured cells: T. Yoshimori, et al.; J. Biol. Chem. 266, 17707 (1991), Abstract; Full Text
Inhibition of osteoclast proton transport by bafilomycin A1 abolishes bone resorption: K. Sundqui, et al.; BBRC 168, 309 (1990), Abstract;
Kinetic studies of chromaffin granule H+-ATPase and effects of bafilomycin A1: H. Hanada, et al.; BBRC 170, 873 (1990), Abstract;
The cytotoxic action of diphtheria toxin and its degradation in intact Vero cells are inhibited by bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase: T. Umata, et al.; J. Biol. Chem. 265, 21940 (1990), Abstract; Full Text
The evolution of H+-ATPases [see comments]: N. Nelson & L. Taiz; TIPS 14, 113 (1989), (Review), Abstract;
Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells: E.J. Bowman, et al.; PNAS 85, 7972 (1988), Abstract;
Metabolic products of microorganisms. 224. Bafilomycins, a new group of macrolide antibiotics. Production, isolation, chemical structure and biological activity: G. Werner, et al.; J. Antibiot. 37, 110 (1984), Abstract;
