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Synonyms: Baf A1
| Description | Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis. |
| Targets & IC50 | short circuit current:0.17 μM, V-ATPase:14 nmol /mg, Proteoglycan degradation (stimulated by IL-1):< 10 nM |
| In vitro | METHODS: Human pancreatic cancer cells Capan-1 were treated with Bafilomycin A1 (1-100 nM) for 72 h. Cell growth inhibition was detected using MTT. RESULTS: Bafilomycin A1 dose-dependently inhibited the growth of Capan-1 cells with an IC50 of 5 nM. [1] METHODS: Human osteosarcoma cells MG63 were treated with Bafilomycin A1 (1 μmol/L) for 6-24 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Bafilomycin A1 induced a significant increase in the levels of apoptosis-related proteins p53 and Beclin 1, a significant decrease in the expression of autophagy-related proteins p62 and LC3-I, and an increase in LC3-II. [2] METHODS: Human hepatocellular carcinoma cells BEL7402 and HepG2 were incubated with Bafilomycin A1 (5 nM) for 24 h, and the cell cycle was examined by Flow Cytometry. RESULTS: Bafilomycin A1 increased the percentage of BEL7402 and HepG2 cells in the G1 phase of the cell cycle, while cells in the G2/M phase decreased, indicating G1 phase arrest. [3] |
| In vivo | METHODS: To assay antitumor activity in vivo, Bafilomycin A1 (0.1-1 mg/kg) was intraperitoneally injected once daily for three days into NOD-SCID mice harboring the human acute lymphoblastic leukemia tumor B-ALL. RESULTS: Bafilomycin A1 prolonged the survival and improved the pathology of xenograft mice by targeting leukemia cells. [4] METHODS: To investigate the role of autophagy in chronic wound healing, Bafilomycin A1 (1 mg/kg) was administered as a single intraperitoneal injection to diabetic db/db mice. RESULTS: Bafilomycin A1 treatment significantly accelerated wound healing in db/db mice and exerted a favorable healing effect.Bafilomycin A1 may accelerate the healing of diabetic chronic refractory wounds by promoting cell proliferation, collagen production, and modulating inflammatory homeostasis. [5] |
| Synonyms | Baf A1 |
| Molecular Weight | 622.83 |
| Formula | C35H58O9 |
| Cas No. | 88899-55-2 |
| Smiles | 18[C@@]1(OC(=O)\C(OC)=C\C(\C)=C\[C@@H](C)[C@@H](O)[C@@H](C)C\C(C)=C\C=C\[C@@H]1OC)[C@@H](C)[C@@H](O)[C@H](C)[C@@]1(O)C[C@@H](O)[C@H](C)[C@H](O1)C(C)C |
| Relative Density. | 1.12 g/cm3 |
| Storage | Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 99 mg/mL (158.95 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 5% DMSO＋40% PEG300＋5% Tween 80＋50% Saline: 0.3 mg/mL (0.48 mM) Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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