Bafilomycin A1
Bafilomycin A1(CAS 88899-55-2) is a selective inhibitor of vacuolar-type H⁺-ATPases (V-ATPases), enzymes responsible for proton translocation across organellar membranes. It inhibits V-ATPase enzymatic activity with established IC₅₀ values ranging from 4 to 400 nmol/mg protein, depending on the organismal source (plant, fungal, or animal origin). In vitro studies show Bafilomycin A1 completely blocks H⁺ transport through V-ATPases at concentrations as low as 10 nM. Additionally, this inhibitor is commonly employed in cell biology research to investigate roles of V-ATPases in intracellular pH regulation, lysosomal function, and osteoclast-mediated bone resorption.
References:
1. Bowman E J, Siebers A, Altendorf K. Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells[J]. Proceedings of the National Academy of Sciences, 1988, 85(21): 7972-7976.
2. Takami M, Suda K, Sahara T, et al. Involvement of vacuolar H+-ATPase in incorporation of risedronate into osteoclasts[J]. Bone, 2003, 32(4): 341-349.
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| Physical Appearance | A crystalline solid |
| Storage | Desiccate at -20°C |
| M.Wt | 622.84 |
| Cas No. | 88899-55-2 |
| Formula | C35H58O9 |
| Solubility | Soluble in DMSO |
| Chemical Name | (3Z,5E,7R,8S,9S,11E,13E,15S,16R)-16-[(2S,3R,4S)-4-[(2R,4R,5S,6R)-2,4-dihydroxy-5-methyl-6-propan-2-yloxan-2-yl]-3-hydroxypentan-2-yl]-8-hydroxy-3,15-dimethoxy-5,7,9,11-tetramethyl-1-oxacyclohexadeca-3,5,11,13-tetraen-2-one |
| SDF | Download SDF |
| Canonical SMILES | CC1CC(=CC=CC(C(OC(=O)C(=CC(=CC(C1O)C)C)OC)C(C)C(C(C)C2(CC(C(C(O2)C(C)C)C)O)O)O)OC)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
HeLa cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 20 nM |
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Applications |
Bafilomycin A1 dose-dependently inhibited the vacuolization of Hela cells induced by H. pylori, showing a 50% effect at 4 nM and a complete inhibition at 12.5 nM. In addition, Bafilomycin A1 also efficiently restored vacuolated cells to a normal appearance. |
| Animal experiment [2]: | |
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Animal models |
Young freshwater tilapias |
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Dosage form |
0 ~ 10-5 mol/L; 30 mins |
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Applications |
In young tilapias, Bafilomycin A1 dose-dependently inhibited the rate of Na+ uptake with a Ki value of 1.6 × 10-7 mol/L. The inhibitory effect (20%) was observed at a concentration as low as 10-8 mol/L and increased linearly up to a concentration of 10-6 mol/L, after which it remained at approximately 90 % inhibition. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Papini E, Bugnoli M, De Bernard M, Figura N, Rappuoli R, Montecucco C. Bafilomycin A1 inhibits Helicobacter pylori-induced vacuolization of HeLa cells. Mol Microbiol. 1993 Jan;7(2):323-7. [2]. Fenwick JC, Wendelaar Bonga SE, Flik G. In vivo bafilomycin-sensitive Na(+) uptake in young freshwater fish. J Exp Biol. 1999 Dec;202 Pt 24:3659-66. |
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| Description | Bafilomycin A1 is a selective and reversible inhibitor of vacuolar H+ ATPases (V-ATPases) with IC50 value of 4-400 nM. | |||||
| Targets | V-ATPases | |||||
| IC50 | 4-400 nM | |||||
Quality Control & MSDS
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