Bafilomycin A1 (Baf-A1)

製品コードS1413 バッチS141309

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 DMSO 100 mg/mL (160.55 mM)
Water Insoluble
Ethanol Insoluble
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
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
1.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.

溶剤液（一定の濃度）を調合する

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 is a toxic macrolide antibiotic derived from Streptomyces griseus. Bafilomycin A1 inhibits the short circuit current induced by the outer mantle epithelium (OME). The IC50 and maximum inhibition dose of Bafilomycin A1 are 0.17 μM and 0.5 μM, respectively. [2] In addition, Bilomycin A1 inhibits the acid influx with an IC50 value of 0.4 nM. Bafilomycin A1 inhibits the acidification dose-dependently resulting in a lower quenching, and thus a higher fluorescence. [3] Bafilomycin A1 prevents the vacuolization of Hela cells induced by H. pylori, with an inhibitory concentration giving 50% of maximal (ID50) of 4 nM. Bafilomycin A1 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. Bafilomycin not only dissipates the low endosomal pH but also blocks transport from early to late endosomes in HeLa cells. [5] Bafilomycin A1 at doses of 0.1-1 μM completely inhibits the acidification of lysosomes revealed by the incubation with acridine orange in BNL CL.2 and A431 cells. [6] When Bafilomycin A1 is added to Hanks' balanced salt solution, endogenous protein degradation is strongly inhibited and numerous autophagosomes accumulated in H-4-II-E cells. Bafilomycin A1 also prevents the appearance of endocytosed HRP in autophagic vacuoles. [7]
in vivo Bafilomycin A1 (1 μM and 0.1 μM) completely inhibits the resorptive activity of cultured osteoclasts. [8] Bafilomycin A1 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, 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 the specific V-ATPases inhibitor Bafilomycin A1.
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 inhibitor Bafilomycin 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 --

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：

Stress response silencing by an E3 ligase mutated in neurodegeneration [ Nature, 2024, 626(8000):874-880] PubMed: 38297121
ATG14 targets lipid droplets and acts as an autophagic receptor for syntaxin18-regulated lipid droplet turnover [ Nat Commun, 2024, 15(1):631] PubMed: 38245527
Gonococcal OMV-delivered PorB induces epithelial cell mitophagy [ Nat Commun, 2024, 15(1):1669] PubMed: 38396029
Heterogeneous ferroptosis susceptibility of macrophages caused by focal iron overload exacerbates rheumatoid arthritis [ Redox Biol, 2024, 69:103008] PubMed: 38142586
Pinacidil ameliorates cardiac microvascular ischemia-reperfusion injury by inhibiting chaperone-mediated autophagy of calreticulin [ Basic Res Cardiol, 2024, 119(1):113-131] PubMed: 38168863
LUBAC-mediated M1 Ub regulates necroptosis by segregating the cellular distribution of active MLKL [ Cell Death Dis, 2024, 15(1):77] PubMed: 38245534
Human YKT6 forms priming complex with STX17 and SNAP29 to facilitate autophagosome-lysosome fusion [ Cell Rep, 2024, 43(2):113760] PubMed: 38340317
Regulation of NCOA4-mediated iron recycling ameliorates paraquat-induced lung injury by inhibiting ferroptosis [ Cell Commun Signal, 2024, 22(1):146] PubMed: 38388414
RNA m6A modification regulates L1 retrotransposons in human spermatogonial stem cell differentiation in vitro and in vivo [ Cell Mol Life Sci, 2024, 81(1):92] PubMed: 38363375
PKCiota Inhibits the Ferroptosis of Esophageal Cancer Cells via Suppressing USP14-Mediated Autophagic Degradation of GPX4 [ Antioxidants (Basel), 2024, 13(1)114] PubMed: 38247539

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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