Bafilomycin A1 (Baf-A1)

製品コードS1413 バッチS141310

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C35H58O9
分子量 622.83 CAS No. 88899-55-2
Solubility (25°C)* 体外  
 
 
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.300mg/ml (0.48mM) Taking the 1 mL working solution as an example, add 50 μL 6 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

生物活性

製品説明 バフィロマイシン A1 (Bafilomycin A1(Baf-A1)) は液胞 H+-ATPase 阻害剤で、IC50 は 0.44 nM です。 バフィロマイシン A1 は、オートファジー (autophagy) を阻害する一方で、アポトーシス (apoptosis) を誘導することがわかっています。
in vitro Bafilomycin A1 (Baf-A1) is a toxic macrolide antibiotic derived from Streptomyces griseus, which inhibits the short circuit current induced by the outer mantle epithelium (OME). The IC50 and maximum inhibition dose are 0.17 μM and 0.5 μM, respectively. [2] In addition, it inhibits the acid influx with an IC50 value of 0.4 nM. This compound inhibits the acidification dose-dependently resulting in a lower quenching, and thus a higher fluorescence. [3] It prevents the vacuolization of Hela cells induced by H. pylori, with an inhibitory concentration giving 50% of maximal (ID50) of 4 nM, and is also very efficient in restoring vacuolated cells to a normal appearance. [4] Bafilomycin A1 also affects the transport of endocytosed material from early to late endocytic compartments, not only dissipating the low endosomal pH but also blocking transport from early to late endosomes in HeLa cells. [5] At doses of 0.1-1 μM, it completely inhibits the acidification of lysosomes revealed by the incubation with acridine orange in BNL CL.2 and A431 cells. [6] When added to Hanks' balanced salt solution, endogenous protein degradation is strongly inhibited and numerous autophagosomes accumulated in H-4-II-E cells. It also prevents the appearance of endocytosed HRP in autophagic vacuoles. [7]
in vivo Bafilomycin A1 (Baf-A1) (1 μM and 0.1 μM) completely inhibits the resorptive activity of cultured osteoclasts. [8] It also dose-dependently inhibits the rate of Na+ uptake in young tilapia with a Ki of 0.16 μM. [9]

プロトコル(参考用のみ)

キナーゼアッセイ ATPase enzyme activity assays
The ATPase enzyme assay medium contains 6 mM MgSO4, 50 mM HEPES (pH 7.4), 200 mM Na2SO3 (V-ATPase activator), 0.5 mM sodium ortho-vanadate (P-ATPase inhibitor), 0.5 mM sodium azide (F-ATPase inhibitor) and 3 mM Na2ATP. This medium (1.0 mL), with or without the addition of the V-type ATPase inhibitor bafilomycin A1 (Baf-A1), is incubated with the filtered homogenate (0.1 mL) for 60 minutes at 23–25 °C. The reaction is stopped by the addition of 1 mL of TCA 3%. Spectrometric blanks are prepared as for the enzyme assay with the exception that the tissue sample is added after the acid. Phosphate analysis is accomplished by adding 2 mL of 1-butanol and 0.2 mL molybdate solution (5 g ammonium molybdate, 22 mL H2SO4 to 100 mL). After vortexing for 15 seconds the solution is neutralised with 0.5 mL citrate solution (100 g/500 mL, pH 7.0) and again vortexed for 15 seconds. The solution is then centrifuged (2000 × g; 3 minutes) to separate the butanol phase and the absorbance of this phase is read at 400 nm. Standards of orthophosphate are prepared (0.1 μM–2.0 μM) and treated in the same way as the enzyme activity assays. Enzyme activity is expressed in μmol of orthophosphate liberated per hour and per milligram of protein. V-ATPase activity is considered to be the difference between the total ATPase activity measured in the presence of Na2SO3, sodium orthovanadate and sodium azide and the ATPase activity measured in the presence of these reagents and of this compound.
細胞アッセイ 細胞株 HeLa cells
濃度 ~20 nM
反応時間 20 hours
実験の流れ

H. pylori bacteria extract is treated with inhibitors, before addition to HeLa cells, as follows: DCCD 10 mM for 1 hour at 30 ºC; NBD-CI 100 μM for 1 hour at 30 ºC and the reaction is blocked with glycine 10 mM final concentration; NEM 275 μM for 1 hour at 30 ºC and the reaction is blocked by addition of β-mercaptoethanol 275 mM; Mg-ATP 14 μM for 1 hour at 0 ºC; 100 μM KNO3 and 14 μM Mg-ATP for 1 hour at 30 μM; NaCO3 100 μM, pH 11 for 1 hour at 0 ºC. The bacterial extract is then added to cell with a 40-fold dilution at a final concentration of 0.65 mg/mL. Controls are HeLa cells incubated with untreated bacterial extracts and cells treated with Bafilomycin A1 (Baf-A1) under the same conditions as bacterial extracts, at the same concentrations or after a 40-fold dilution. The vacuotating activity of the bacterial extracts is assayed.
動物実験 動物モデル Young (approximately 9 days old) Mozambique tilapia, Oreochromis mossambicus
投薬量 10 μM
投与方法 --

参考

  • https://pubmed.ncbi.nlm.nih.gov/9684329/
  • https://pubmed.ncbi.nlm.nih.gov/15596387/
  • https://pubmed.ncbi.nlm.nih.gov/17576165/
  • https://pubmed.ncbi.nlm.nih.gov/8446034/
  • https://pubmed.ncbi.nlm.nih.gov/9811698/
  • https://pubmed.ncbi.nlm.nih.gov/1832676/
  • https://pubmed.ncbi.nlm.nih.gov/9639028/
  • https://pubmed.ncbi.nlm.nih.gov/7817803/
  • https://pubmed.ncbi.nlm.nih.gov/10574743/
  • https://pubmed.ncbi.nlm.nih.gov/14713959/

カスタマーフィードバック

Data from [Data independently produced by , , Chem Sci, 2017, 8(3):1915-1921]

Data from [Data independently produced by , , Cancer Lett, 2018, 431:85-95]

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2018, 37(1):251]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cytosolic acetyl-coenzyme A is a signalling metabolite to control mitophagy [ Nature, 2025, 10.1038/s41586-025-09745-x] PubMed: 41225001
Oncogenic RAS induces a distinctive form of non-canonical autophagy mediated by the P38-ULK1-PI4KB axis [ Cell Res, 2025, 10.1038/s41422-025-01085-9] PubMed: 40055523
Host FSTL1 defines the impact of stem cell therapy on liver fibrosis by potentiating the early recruitment of inflammatory macrophages [ Signal Transduct Target Ther, 2025, 10(1):81] PubMed: 40050288
Alterations in PD-L1 succinylation shape anti-tumor immune responses in melanoma [ Nat Genet, 2025, 57(3):680-693] PubMed: 40069506
ACSS2 drives senescence-associated secretory phenotype by limiting purine biosynthesis through PAICS acetylation [ Nat Commun, 2025, 16(1):2071] PubMed: 40021646
BiDAC-dependent degradation of plasma membrane proteins by the endolysosomal system [ Nat Commun, 2025, 16(1):4345] PubMed: 40346034
Rab27a regulates the transport of influenza virus membrane proteins to the plasma membrane [ Nat Commun, 2025, 16(1):6271] PubMed: 40623997
The O-glycosyltransferase C1GALT1 promotes EWSR1::FLI1 expression and is a therapeutic target for Ewing sarcoma [ Nat Commun, 2025, 16(1):1267] PubMed: 39894896
S100P is a ferroptosis suppressor to facilitate hepatocellular carcinoma development by rewiring lipid metabolism [ Nat Commun, 2025, 16(1):509] PubMed: 39779666
Extracellular Histones as Exosome Membrane Proteins Regulated by Cell Stress [ J Extracell Vesicles, 2025, 14(2):e70042] PubMed: 39976275

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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