| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Macrolide
Bafilomycin C1 targets vacuolar-type H+-ATPases (V-ATPases), which are proton pumps responsible for acidifying intracellular organelles. The compound binds to the V0 subunit of the V-ATPase, specifically inhibiting proton translocation across membranes. By blocking V-ATPase activity, Bafilomycin C1 prevents the acidification of lysosomes and endosomes, leading to the inhibition of autophagic degradation and the accumulation of autophagosomes. The inhibition of V-ATPase also disrupts various cellular processes that depend on acidic pH, including receptor-mediated endocytosis, protein trafficking, and the activation of lysosomal enzymes. Bafilomycin C1 is a reversible inhibitor, meaning its effects can be reversed by removing the compound. |
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| ln Vitro |
In a time and dose-dependent manner, bafilomycin C1 (0.33-10 μM; 6 days) suppresses the growth and proliferation of HepG2 and SMMC7721 cells[2]. In both mRNA and protein expression, bafilomycin C1 (0.33-3.3 μM; 24 hours) reduces the expression of cyclin D3, cyclin E1, CDK2, CDK4, and CDK6 in SMMC7721 cells[2]. When compared to the vehicle, bafilomycin C1 (3.3–10 μM; 24 hours) results in morphological changes and a higher number of apoptotic cells when stained with Hoechst 33258 (HY-15558)[2].
Bafilomycin C1 has demonstrated potent in vitro activity against cancer cell lines. In hepatocellular carcinoma cell lines HepG2 and SMMC7721, Bafilomycin C1 (0.33-10 μM; 6 days) suppresses growth and proliferation in a time- and dose-dependent manner. The compound reduces the expression of cyclin D3, cyclin E1, CDK2, CDK4, and CDK6, which are key regulators of the cell cycle. Bafilomycin C1 induces cell apoptosis in hepatocellular carcinoma cells. The compound also exhibits antibacterial activity against gram-positive bacteria and antifungal activity. The half-maximal inhibitory concentration (IC50) for the inhibition of V-ATPase activity has not been detailed in the available literature, but the compound is described as a potent inhibitor. |
| ln Vivo |
Bafilomycin C1 (subcutaneous injection; 0.2 mg/kg; 20 days) in a model of naked mice slows the growth of tumors without causing any obvious side effects or unpleasant reactions[1].
Bafilomycin C1 has demonstrated in vivo antitumor activity in a xenograft mouse model. In a BALB/c nude mice model with SMMC7721 hepatocellular carcinoma tumor xenografts, subcutaneous injection of Bafilomycin C1 at a dose of 0.2 mg/kg for 20 days significantly retarded tumor growth without causing obvious adverse reactions or side effects. This finding suggests that Bafilomycin C1 has potential as an anticancer agent with a manageable safety profile at the tested dose. The compound’s in vivo activity is attributed to its inhibition of V-ATPase, which leads to the disruption of autophagic degradation and the induction of apoptosis in cancer cells. |
| Enzyme Assay |
The V-ATPase inhibitory activity of Bafilomycin C1 can be assessed using in vitro enzyme assays. In a typical assay, purified V-ATPase enzyme (from bovine brain or other sources) is reconstituted into liposomes or membrane vesicles. The enzyme is incubated with ATP and Bafilomycin C1 at varying concentrations, and the proton pumping activity is measured using a fluorescence-based assay with acridine orange or other pH-sensitive dyes. The decrease in fluorescence signal, which indicates the inhibition of proton translocation, is used to calculate the half-maximal inhibitory concentration (IC50). Alternatively, the ATPase activity of V-ATPase can be measured by quantifying the release of inorganic phosphate using a colorimetric assay. The reversibility of inhibition can be confirmed by dialysis or dilution experiments.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: SMMC7721 cell and HepG2 cell Tested Concentrations: 0.33 μM, 1.1 μM, and 3.3 μM for SMMC7721 1.1 μM, 3.3 μM, and 10.0 μM for HepG2 Incubation Duration: 6 days Experimental Results: Retarded the cell growth. Western Blot Analysis[2] Cell Types: SMMC7721 cells Tested Concentrations: 3.3 μM Incubation Duration: 24 hrs (hours) Experimental Results: Decreaed cyclin D3/E1,CDK2/4/6 protein expression and increased p21. Apoptosis Analysis[2] Cell Types: SMMC7721 and HepG2 cells Tested Concentrations: 3.3 μM; 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced apoptosis in SMMC7721 and HepG2 cells. The cellular activity of Bafilomycin C1 is assessed using hepatocellular carcinoma cell lines such as HepG2 and SMMC7721. Cells are seeded in 96-well plates and treated with escalating concentrations of Bafilomycin C1 (0.33-10 μM) for 24 to 144 hours. Cell viability is measured using MTT or CellTiter-Glo assays, and the half-maximal inhibitory concentration (IC50) values are calculated from dose-response curves. Apoptosis is assessed by flow cytometry using annexin V/propidium iodide staining or by measuring caspase-3/7 activity. The effects of Bafilomycin C1 on cell cycle regulators, such as cyclin D3, cyclin E1, CDK2, CDK4, and CDK6, are assessed by Western blotting. Autophagy is assessed by monitoring the accumulation of LC3-II (a marker of autophagosomes) by Western blotting. |
| Animal Protocol |
Animal/Disease Models: BALB/c nude mice (weighing 18-20 g) subcutaneous (sc)injected by SMMC7721 cell suspension (5×106 cells/100 μL)[2]
Doses: 0.2 mg/kg Route of Administration: subcutaneous (sc)injection; 20 days Experimental Results: Suppressed tumor growth of SMMC7721 tumor xenografts. Bafilomycin C1 has been evaluated in a xenograft mouse model of hepatocellular carcinoma. Female BALB/c nude mice are inoculated subcutaneously with SMMC7721 hepatocellular carcinoma cells. When tumors reach a palpable size, animals are randomized into treatment and control groups. Bafilomycin C1 is administered at a dose of 0.2 mg/kg by subcutaneous injection. The treatment is continued for 20 days. Tumor volumes are measured twice weekly using calipers, and tumor growth inhibition (TGI) is calculated. Body weights are monitored as a general indicator of toxicity. At the end of the study, tumors are excised, weighed, and processed for histopathological analysis and immunohistochemical staining to assess V-ATPase expression, apoptosis (TUNEL assay), and proliferation (Ki-67 staining). |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data for Bafilomycin C1 has been published in the available literature. As a macrolide antibiotic with a molecular weight of 720.89 g/mol, Bafilomycin C1 is likely to have poor oral bioavailability and may require parenteral administration for in vivo studies. The compound is soluble in DMSO. Further studies would be needed to characterize the absorption, distribution, metabolism, and excretion (ADME) properties of Bafilomycin C1, including plasma protein binding, clearance, half-life, and tissue distribution. The compound’s pharmacokinetic profile would be essential for determining appropriate dosing regimens for in vivo efficacy studies and for assessing its potential for clinical development.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for Bafilomycin C1 has been published in the available literature. In the xenograft mouse model, Bafilomycin C1 was reported to be well tolerated at a dose of 0.2 mg/kg, with no obvious adverse reactions or side effects. However, comprehensive toxicology studies would be required to evaluate the safety profile of Bafilomycin C1 for potential clinical development. The mechanism of action, which involves the inhibition of V-ATPase and disruption of lysosomal function, could lead to off-target effects in normal tissues that depend on V-ATPase activity. The compound’s antibacterial and antifungal activities also suggest that it could affect the microbiome.
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| References |
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| Additional Infomation |
Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. that functions as a potent, specific, and reversible inhibitor of vacuolar-type H+-ATPases (V-ATPases). It is used as a research tool to study the role of V-ATPases in autophagy, endocytosis, and other cellular processes. The compound inhibits the growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and has been used to study hepatocellular carcinoma. In a xenograft mouse model, subcutaneous injection of Bafilomycin C1 at 0.2 mg/kg for 20 days retarded tumor growth without causing obvious side effects. Bafilomycin C1 is available as a research compound from various suppliers.
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| Molecular Formula |
C39H60O12
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|---|---|
| Molecular Weight |
720.89
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| Exact Mass |
720.408
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| CAS # |
88979-61-7
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| PubChem CID |
129396804
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| Appearance |
White to off-white solid powder
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| Density |
1.18 g/cm3
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| Boiling Point |
844.4ºC at 760 mmHg
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| Flash Point |
248.9ºC
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| Index of Refraction |
1.544
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| LogP |
4.884
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
51
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| Complexity |
1350
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@H]1C/C(=C/C=C/[C@@H]([C@H](OC(=O)/C(=C/C(=C/[C@H]([C@H]1O)C)/C)/OC)[C@@H](C)[C@H]([C@H](C)[C@]2(C[C@H]([C@@H]([C@H](O2)C(C)C)C)OC(=O)/C=C/C(=O)O)O)O)OC)/C
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| InChi Key |
WUDBXVQNMOTFEE-ZXXPJKRZSA-N
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| InChi Code |
InChI=1S/C39H60O12/c1-21(2)36-26(7)31(49-33(42)16-15-32(40)41)20-39(46,51-36)28(9)35(44)27(8)37-29(47-10)14-12-13-22(3)17-24(5)34(43)25(6)18-23(4)19-30(48-11)38(45)50-37/h12-16,18-19,21,24-29,31,34-37,43-44,46H,17,20H2,1-11H3,(H,40,41)/b14-12+,16-15+,22-13+,23-18+,30-19-/t24-,25+,26-,27-,28-,29-,31+,34-,35+,36+,37+,39+/m0/s1
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| Chemical Name |
(E)-4-[(2R,4R,5S,6R)-2-hydroxy-2-[(2S,3R,4S)-3-hydroxy-4-[(2R,3S,4E,6E,9S,10S,11R,12E,14Z)-10-hydroxy-3,15-dimethoxy-7,9,11,13-tetramethyl-16-oxo-1-oxacyclohexadeca-4,6,12,14-tetraen-2-yl]pentan-2-yl]-5-methyl-6-propan-2-yloxan-4-yl]oxy-4-oxobut-2-enoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3872 mL | 6.9359 mL | 13.8717 mL | |
| 5 mM | 0.2774 mL | 1.3872 mL | 2.7743 mL | |
| 10 mM | 0.1387 mL | 0.6936 mL | 1.3872 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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