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Purity: ≥98%
Bafilomycin A1 (formerly known as NSC-381866; NSC381866; NSC 381866) is a novel, potent and selective inhibitor of vacuolar H+-ATPase (V-ATPases) with antibacterial activity. It inhibits vacuolar H+-ATPase (V-ATPases) with IC50 of 0.44 nM. It is a macrolide antibiotic isolated from the Streptomyces species. The inhibitory effect of bafilomycin A1 on vacuolar ATPases was determined by testing its influence on H+-pumping activity. H+ translocation was completely inhibited by 10 nM bafilomycin A1. Other study has shown that bafilomycin A1 strongly inhibited the pit-forming activity of osteoclasts. The subcellular localization of V-ATPase in osteoclasts was been treated with or without bafilomycin A1 by immunoelectron microscopy. Bafilomycin A1 triggers proliferative potential of senescent cancer cells in vitro and in NOD/SCID mice. Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways.
| ln Vitro |
Bafilomycin A1 is exposed to various membrane ATPases, exhibiting an I50 of 400 nmol/mg, 4 nmol/mg, and 50 nmol/mg for the vacuolar ATPases of a plant (Z. mays), an animal (bovine abrenal medulla), and a fungus (N. crassa). The 50% inhibition of ATPase activity expressed as μmol of Bafilomycin A1 per mg of protein is known as the I50 values[1]. By blocking both V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion, bafilomycin A1 ((-)-Bafilomycin A1) impairs autophagic flux[2]. Pediatric B-cell acute lymphoblastic leukemia cells are specifically and efficiently inhibited and killed by bafilomycin A1 at a low concentration (1 nM). It induces apoptosis without the need for caspase and targets mitochondria, the autophagy pathway, and both early and late stages of the pathway. Beclin 1 binds to Bcl-2 when bafilomycin A1 is present, further inhibiting autophagy and encouraging apoptotic cell death[5]. Bafilomycin A1 inhibits the growth of the HO-8910 ovarian cancer and BEL-7402 hepatocellular carcinoma cell lines as well as their ability to spread. Bafilomycin A1 is thought to cause apoptosis, according to tests using capsase-3 and -9 and transmission electron microscopy[6]. Whether or not they are transformed, NIH-3T3 fibroblasts, PC12 and HeLa cells, and golden hamster embryos are among the many cultured cells whose growth is dose-dependently inhibited by bafilomycin A1. When it comes to inhibiting cell growth, bafilomycin A1's IC50 ranges from 10 to 50 nM[7].
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| ln Vivo |
Low-dose Bafilomycin A1 (0.1 mg/kg) administered over an extended period of time modestly reduces the tumor volume, but the final tumor volume is not substantially different from the control. After 21 days, however, long-term administration of a high dose of Bafilomycin A1 (1 mg/kg) effectively slows tumor growth as compared to controls[8]. The survival of B-cell acute lymphoblastic leukemia (B-ALL) xenograft mice with advanced disease is prolonged by bafilomycin A1 (0.1 mg/kg or 1 mg/kg; intraperitoneally for 3 days)[9].
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| References |
[1]. Bowman EJ, et al. Bafilomycins: a class of inhibitors of membrane ATPases from microorganisms, animal cells, and plant cells. Proc Natl Acad Sci U S A. 1988;85(21):7972-7976.
[2]. Mauvezin C, et al. Bafilomycin A1 disrupts autophagic flux by inhibiting both V-ATPase-dependent acidification and Ca-P60A/SERCA-dependent autophagosome-lysosome fusion. Autophagy. 2015;11(8):1437-1438. [3]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015;100(3):345-356. [4]. Yoshimori T, et al. Bafilomycin A1, a specific inhibitor of vacuolar-type H(+)-ATPase, inhibits acidification and protein degradation in lysosomes of cultured cells. J Biol Chem. 1991;266(26):17707-17712 [5]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015 Mar;100(3):345-56. [6]. Lu X, et al. Bafilomycin A1 inhibits the growth and metastatic potential of the BEL-7402 liver cancer and HO-8910 ovarian cancer cell lines and induces alterations in their microRNA expression. Exp Ther Med. 2015 Nov;10(5):1829-1834. [7]. Ohkuma S, et al. Inhibition of cell growth by bafilomycin A1, a selective inhibitor of vacuolar H(+)-ATPase. In Vitro Cell Dev Biol Anim. 1993 Nov;29A(11):862-6. [8]. Ohta T, et al. Bafilomycin A1 induces apoptosis in the human pancreatic cancer cell line Capan-1. J Pathol. 1998 Jul;185(3):324-30. [9]. Cattani L, et al. Bafilomycin A1 and intracellular multiplication of Legionella pneumophila. Antimicrob Agents Chemother. 1997;41(1):212-214. [10]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015 Mar;100(3):345-56 |
| Molecular Formula |
C35H58O9
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| Molecular Weight |
622.83
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| CAS # |
88899-55-2
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| Related CAS # |
88899-56-3 (Bafilomycin B1)
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| SMILES |
O[ C@H]([ C@H](C)/C=C(C)/C=C1OC)[C@@H](C)C/C(C)=C/C=C\[ C@H](OC)C([C@@H](C)[ C@H]([C@@H]([C@@]2(O)C[C@@H](O)[ C@H](C)[C@@H]([ C@H](C)C)O2)C)O)OC/1=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6056 mL | 8.0279 mL | 16.0557 mL | |
| 5 mM | 0.3211 mL | 1.6056 mL | 3.2111 mL | |
| 10 mM | 0.1606 mL | 0.8028 mL | 1.6056 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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